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Publisher: Elsevier BV
Date: 11-1993
DOI: 10.1016/0306-3623(93)90434-Y
Abstract: 1. Hepatoprotective activity of hydro-methanolic extract of Artemisia scoparia (Compositae) was investigated against acetaminophen-induced hepatic damage. 2. Acetaminophen at a dose of 1 g/kg produced 100% mortality in mice while pretreatment of animals with plant extract (150 mg/kg) reduced the death rate to 20%. 3. Acetaminophen at a dose of 640 mg/kg produced liver damage in rats as manifested by the rise in serum levels of GOT and GPT to 1528 +/- 310 and 904 +/- 261 IU/l (n = 10) respectively, compared to respective control values of 80 +/- 11 and 38 +/- 09. 4. Pretreatment of rats with plant extract (150 mg/kg) lowered significantly the respective serum GOT and GPT levels to 85 +/- 11 and 23 +/- 06. 5. These results indicate that Artemisia scoparia contains hepatoprotective constituents and this study rationalizes the traditional use of this plant in hepatobiliary disorders.
Publisher: Springer Science and Business Media LLC
Date: 17-10-2011
Abstract: Origanum vulgare Linn has traditionally been used in the treatment of urolithiasis. Therefore, we investigated the crude extract of Origanum vulgare for possible antiurolithic effect, to rationalize its medicinal use. The crude aqueous-methanolic extract of Origanum vulgare (Ov.Cr) was studied using the in vitro and in vivo methods. In the in vitro experiments, supersaturated solution of calcium and oxalate, kidney epithelial cell lines (MDCK) and urinary bladder of rabbits were used, whereas, in the in vivo studies, rat model of urolithiasis was used for the study of preventive and curative effect. In the in vitro experiments, Ov.Cr exhibited a concentration-dependent (0.25-4 mg/ml) inhibitory effect on the slope of nucleation and aggregation and also decreased the number of calcium oxalate monohydrate crystals (COM) produced in calcium oxalate metastable solutions. It also showed concentration-dependent antioxidant effect against DPPH free radical and lipid peroxidation induced in rat kidney tissue homogenate. Ov.Cr reduced the cell toxicity using MTT assay and LDH release in renal epithelial cells (MDCK) exposed to oxalate (0.5 mM) and COM (66 μg/cm 2 ) crystals. Ov.Cr relaxed high K + (80 mM) induced contraction in rabbit urinary bladder strips, and shifted the calcium concentration-response curves (CRCs) towards right with suppression of the maximum response similar to that of verapamil, a standard calcium channel blocker. In male Wistar rats receiving lithogenic treatment comprising of 0.75% ethylene glycol in drinking water given for 3 weeks along with ammonium chloride (NH 4 Cl) for the first 5 days, Ov.Cr treatment (10-30 mg/kg) prevented as well as reversed toxic changes including loss of body weight, polyurea, crystalluria, oxaluria, raised serum urea and creatinine levels and crystal deposition in kidneys compared to their respective controls. These data indicating the antiurolithic activity in Ov.Cr, possibly mediated through inhibition of CaOx crystallization, antioxidant, renal epithelial cell protective and antispasmodic activities, rationalizes its medicinal use in urolithiasis.
Publisher: Bangladesh Journals Online (JOL)
Date: 14-10-2011
Publisher: Ovid Technologies (Wolters Kluwer Health)
Date: 05-01-2021
Abstract: In the past 3 decades, the arterial switch procedure has replaced the atrial switch procedure as treatment of choice for transposition of the great arteries. Although survival is superior after the arterial switch procedure, data on pregnancy outcomes are scarce and transposition of the great arteries after arterial switch is not yet included in the modified World Health Organization classification of maternal cardiovascular risk. The ROPAC (Registry of Pregnancy and Cardiac disease) is an international prospective registry of pregnant women with cardiac disease, part of the European Society of Cardiology EURObservational Research Programme. Pregnancy outcomes in all women after an arterial switch procedure for transposition of the great arteries are described. The primary end point was a major adverse cardiovascular event, defined as combined end point of maternal death, supraventricular or ventricular arrhythmias requiring treatment, heart failure, aortic dissection, endocarditis, ischemic coronary events, and thromboembolic events. Altogether, 41 pregnant women (mean age, 26.7±3.9 years) were included, and there was no maternal mortality. A major adverse cardiovascular event occurred in 2 women (4.9%): heart failure in one (2.4%) and ventricular tachycardia in another (2.4%). One woman experienced fetal loss, whereas no neonatal mortality was observed. Women after an arterial switch procedure for transposition of the great arteries tolerate pregnancy well, with a favorable maternal and fetal outcome. During counseling, most women should be reassured that the risk of pregnancy is low. Classification as modified World Health Organization risk class II seems appropriate.
Publisher: Springer Science and Business Media LLC
Date: 12-09-2023
Publisher: Springer Science and Business Media LLC
Date: 12-2014
Publisher: Wiley
Date: 03-2000
DOI: 10.1002/(SICI)1099-1573(200003)14:2<103::AID-PTR578>3.0.CO;2-P
Abstract: The seeds of Cuminum nigrum were screened phytochemically and were found to contain 8% flavonoids and 0.01% alkaloids. When studied for their effect on blood glucose levels, oral administration of the flavonoid contents of the plant caused a hypoglycaemic effect at a dose range of 0.5 to 1.5 g/kg, both in normal and alloxan-diabetic rabbits. The hypoglycaemic effect started 2 h after drug administration, reaching a maximum within 4-8 h and the blood glucose levels returned close to normal within 24 h of drug administration. The glibenclamide (5 mg/kg), produced a hypoglycaemic effect in the normal rabbits, whereas it had no effect on the blood glucose levels of alloxan-diabetic rabbits. The alkaloids isolated from C. nigrum seeds, however, failed to exert any significant hypoglycaemic effect in either the normal or diabetic rabbits. A 7 day acute toxicity study in rabbits did not produce any apparent adverse effect at doses as high as 5 g/kg orally. These data indicate that the total flavonoid contents of C. nigrum seeds exhibited considerable hypoglycaemic activity in rabbits and may therefore be responsible for the previously reported antidiabetic activity of the seeds. Furthermore, it is conceivable that the C. nigrum flavonoids possess insulin triggering and/or insulin-like properties.
Publisher: Bangladesh Journals Online (JOL)
Date: 20-05-2013
Publisher: Springer Science and Business Media LLC
Date: 07-03-2017
Publisher: Elsevier BV
Date: 12-2015
Publisher: Wiley
Date: 14-08-2006
DOI: 10.1002/PTR.1980
Abstract: The aqueous-ethanol extract of Calendula officinalis flowers (Co.Cr) was studied for its possible spasmolytic and spasmogenic effects in isolated gut preparations. In rabbit jejunum, Co.Cr caused a dose-dependent (0.03-3.0 mg/mL) relaxation of spontaneous and K+-induced contractions, suggestive of calcium channel blockade (CCB). In a few preparations, a mild non-reproducible spasmogenic effect was observed at lower doses, followed by relaxation. The CCB effect was confirmed when pretreatment of the jejunum preparations with Co.Cr produced a dose-dependent rightward shift in the Ca(++) dose-response curves, similar to that of verapamil. Activity-directed fractionation revealed that the spasmolytic activity of the plant was concentrated in its organic fractions. The aqueous fraction exhibited a marked atropine sensitive spasmogenic effect but was found to be devoid of any spasmolytic effect. These data indicate that the crude extract of Calendula officinalis flowers contains both spasmolytic and spasmogenic constituents, exhibiting these effects through calcium channel blocking and cholinergic activities and this study provides a scientific base for its traditional use in abdominal cr s and constipation.
Publisher: Elsevier BV
Date: 10-2000
DOI: 10.1016/S0944-7113(00)80064-1
Abstract: Daucus carota (carrot) has been used in traditional medicine to treat hypertension. Activity-directed fractionation of aerial parts of D. carota resulted in the isolation of two cumarin glycosides coded as DC-2 and DC-3. Intravenous administration of these compounds caused a dose-dependent (1-10 mg/kg) fall in arterial blood pressure in normotensive anaesthetised rats. In the in vitro studies, both compounds caused a dose-dependent (10-200 microg/ml) inhibitory effect on spontaneously beating guinea pig atria as well as on the K+ -induced contractions of rabbit aorta at similar concentrations. These results indicate that DC-2 and DC-3 may be acting through blockade of calcium channels and this effect may be responsible for the blood pressure lowering effect of the compounds observed in the in vivo studies.
Publisher: Elsevier BV
Date: 10-2013
Publisher: Cambridge University Press (CUP)
Date: 15-10-2021
DOI: 10.1017/S2040174420000896
Abstract: Preecl sia (PE) and gestational hypertension (GH) are pregnancy-specific diseases that occur in around 10% of pregnancies worldwide. Increasing evidence suggests that women whose pregnancies were complicated by PE or GH, and their offspring, are at increased risk of cardiovascular disease (CVD) later in life. We hypothesised that PE and GH would associate with CVD risk factors 8–10 years after the first pregnancy in the mother and child and that differences in cardiovascular risk profile would be seen between 8- and 10-year-old male and female children. This is a follow-up study of the Adelaide SCOPE pregnancy cohort where 1164 nulliparous women and their babies were recruited between 2005 and 2008. Haemodynamic function was assessed using non-invasive USCOMBP+ and USCOM1A devices. Microvascular function was assessed by post-occlusive reactive hyperaemia. Of the 273 mother–child pairs followed up, 38 women had PE and 20 had GH during pregnancy. Augmentation index (Aix) and suprasystolic pulse pressure (ssPP) were increased, whereas measures of microvascular function were decreased in children who were born to PE compared to uncomplicated pregnancies. Female children had decreased Aix and ssPP compared to male children after in utero exposure to PE. Women who developed GH during their first pregnancy had increased systolic, diastolic and mean arterial pressures compared to women who had uncomplicated pregnancy. Our data suggest that GH is associated with increased cardiovascular risk in women 8–10 years after first pregnancy and PE is associated with increased offspring risk at 8–10 years of age, highlighting differences between these two hypertensive disorders of pregnancy.
Publisher: Public Library of Science (PLoS)
Date: 21-07-2022
DOI: 10.1371/JOURNAL.PONE.0271722
Abstract: We aimed to assess women’s perceptions on the long-term risks for cardiovascular disease (CVD) after major pregnancy complications. Women who experienced major pregnancy complications and those who experienced uncomplicated pregnancies were invited to participate in a qualitative study. Focus group discussions (FGDs) and self-administered questionnaires were used to explore: The knowledge of long-term sequelae after experiencing a major pregnancy complication Importance of education on heart health The practicality of referral to a clinic after pregnancy complications Willingness for regular postpartum clinic visits after pregnancy complications. A thematic qualitative analysis was undertaken. 26 women participated in four FGDs. The majority of women did not know of the association between major pregnancy complications and CVD. The main views expressed were: Women who experience pregnancy complications should receive education on improving heart health An appointment for the first CVD risk screening visit needs to be made prior to discharge from the delivery suite Women will benefit by having the option to select between a hospital and a general-practitioner based model of follow up. These views are important in developing postpartum strategies to reduce CVD risk among women who experience pregnancy complications.
Publisher: Wiley
Date: 11-1995
Publisher: Hindawi Limited
Date: 13-07-2020
DOI: 10.1155/2020/7974835
Abstract: Ethnopharmacological Relevance . Natural products, like Flaxseed ( Linum usitatissimum ), have traditionally been used in inflammatory bowel disease (IBD). It is known to contain multiple constituents which may account for its effectiveness, as IBD is a multifaceted disease. Aim of the Study . In the current study, we aimed to assess pharmacological basis for the medicinal use of Flaxseed in IBD. Materials and Methods . Aqueous-methanolic crude extracts of Flaxseed (Fs.Cr) and Flaxseed oil were tested against 6% acetic acid- (AA-) induced colitis in BALB/c mice. Microscopic damage parameters of the hematoxylin and eosin-stained and periodic acid-Schiff-alcian blue-stained sections of the colon were scored to be assessed. Possible antispasmodic mechanism was studied on isolated rabbit jejunum, while antibacterial activity was assessed in vitro for microbes implicated in IBD. Results . In AA-induced colitis, Flaxseed oil was found to be more effective in reducing mortality and colonic ulcers than Fs.Cr at 500 mg/kg dose. Fs.Cr was more efficacious in increasing mucin content as compared to oil, exhibiting slightly greater anti-inflammatory effect (50% vs 35%) and reducing depth of lesion (55% vs 42.31%, respectively). Antispasmodic activity of Fs.Cr (0.03 and 0.1 mg/ml) was mediated by phosphodiesterase inhibitors (PDEI, possibly PDE-4 subtype) with a resultant increase in cAMP levels. Flaxseed oil PDEI activity was mild (1 and 3 mg/ml). Fs.Cr (0.1 and 0.3 mg/ml) was potent in exhibiting anticholinergic activity, similar to dicyclomine, whereas Flaxseed oil showed anticholinergic effect at 1 and 3 mg/ml. Flaxseed oil (9 and 14 µ g/ml) was bactericidal against enteropathogenic E.coli (EPEC), enterotoxigenic E.coli (ETEC), and enteroaggregative E.coli (EAEC), whereas Fs.Cr exhibited bactericidal effect against EPEC at 100 µ g/ml. Conclusions . Results of this study, taken together with previous studies, suggest that Flaxseed possesses anti-inflammatory, antibacterial, and antispasmodic action through multiple pathways and thus offers promising potential to be developed for IBD.
Publisher: Springer Science and Business Media LLC
Date: 11-2006
DOI: 10.1007/S00394-006-0620-0
Abstract: Rooibos tea (Aspalathus linearis) is commonly used for hyperactive gastrointestinal, respiratory and cardiovascular disorders. The aqueous extract of Rooibos tea (RT) was studied for the possible bronchodilator, antispasmodic and blood pressure lowering activities in an attempt to rationalize some of its medicinal uses. Isolated tissue preparations, such as rabbit jejunum, aorta and guinea-pig trachea and atria were set up in appropriate physiological salt solutions and aerated with carbogen. For in vivo studies rats were anesthetized with pentothal sodium and blood pressure was measured through carotid artery cannulation. In jejunum, RT caused a concentration-dependent relaxation of low K(+) (25 mM)-induced contractions, with mild effect on the contractions induced by high K(+) (80 mM). In presence of glibenclamide, the relaxation of low K(+)-induced contractions was prevented. Similarly, cromakalim caused glibenclamide-sensitive inhibition of low K(+), but not of high K(+), while verapamil did not differentiate in its inhibitory effect on contractions produced by the two concentrations of K(+). Like in jejunum, RT caused glibenclamide-sensitive relaxation of low K(+)-induced contractions in trachea and aorta, but with a 20 times higher potency in trachea. In atria, RT was least potent with weak inhibitory effect on atrial force and rate of contractions. RT caused a dose-dependent fall in arterial blood pressure in rats under anesthesia. Among the tested pure compounds of Rooibos, chrysoeriol showed selective bronchodilator effect. Chrysoeriol (luteolin 3'-methyl ether) is a bioactive flavonoid known for antioxidant, antiinflammatory, antitumor, antimicrobial, antiviral, and free radical scavenging activities. These results indicate that the bronchodilator, antispasmodic and blood pressure lowering effects of Rooibos tea are mediated predominantly through K(ATP) channel activation with the selective bronchodilatory effect. This study provides a sound mechanistic basis for the wide medicinal use of Rooibos tea, with the therapeutic potential to be developed for congestive respiratory ailments.
Publisher: Springer Science and Business Media LLC
Date: 20-08-2010
Abstract: The objective of present study was to provide the pharmacological basis for the medicinal use of Morinda citrifolia Linn in dyslipidemia using the aqueous-ethanolic extracts of its fruits (Mc.Cr.F), leaves (Mc.Cr.L) and roots (Mc.Cr.R). Mc.Cr.F, Mc.Cr.L and Mc.Cr.R showed antidyslipidemic effects in both triton (WR-1339) and high fat diet-induced dyslipidemic rat models to variable extents. All three extracts caused reduction in total cholesterol and triglyceride levels in triton-induced dyslipidemia. In high fat diet-induced dyslipidemia all these extracts caused significant reduction in total cholesterol, triglyceride, low density lipoprotein-cholesterol (LDL-C), atherogenic index and TC/HDL ratio. Mc.Cr.R extract also caused increase in high density lipoprotein-cholesterol (HDL-C). The Mc.Cr.L and Mc.Cr.R reduced gain in body weight with a reduction in daily diet consumption but Mc.Cr.F had no effect on body weight and daily diet consumption. These data indicate that the antidyslipidemic effect of the plant extracts was meditated through the inhibition of biosynthesis, absorption and secretion of lipids. This may be possibly due partly to the presence of antioxidant constituents in this plant. Therefore, this study rationalizes the medicinal use of Morinda citrifolia in dyslipidemia.
Publisher: MDPI AG
Date: 19-04-2019
Abstract: The aim of this study was to investigate the impact of bedside discharge education on activity levels and healthcare utilization for patients with acute coronary syndrome (ACS) in the first 30 days post-discharge. Knowledge recall and objective activity and location data were collected by global positioning systems (GPS). Participants were asked to carry the tracking applications (apps) for 30–90 days. Eighteen participants were recruited (6 metropolitan 12 rural) 61% ST elevation myocardial infarction (STEMI), mean age 55 years, 83% male. Recall of discharge education included knowledge of diagnosis (recall = 100%), procedures (e.g., angiogram = 40%), and comorbidities (e.g., hypertension = 60%, diabetes = 100%). In the first 30 days post-discharge, median steps per day was 2506 (standard deviation (SD) ± 369) steps (one participant completed 10,000 steps), 62% visited a general practitioner (GP) 16% attended cardiac rehabilitation, 16% visited a cardiologist, 72% a pharmacist, 27% visited the emergency department for cardiac event, and 61% a pathology service (blood tests). Adherence to using the activity tracking apps was 87%. Managing Big Data from the GPS and physical activity tracking apps was a challenge with over 300,000 lines of raw data cleaned to 90,000 data points for analysis. This study was an ex le of the application of objective data from the real world to help understand post-ACS discharge patient activity. Rates of access to services in the first 30 days continue to be of concern.
Publisher: Bangladesh Journals Online (JOL)
Date: 13-12-2019
Abstract: This study explores the pharmacological basis for the folk use of Fagonia indica in constipation using in vivo and in vitro assays. The crude extract of F. indica contained tannins, saponins, anthraquinones, alkaloids, flavonoids, glycosides and phenols. The administration of F. indica extract (100 and 300 mg/kg) to mice caused a partially atropine-sensitive 35 and 42.6% laxation, respectively, similar to ursolic acid which showed 22 and 36% laxation at 10 and 30 mg/kg, respectively. In loperamide-induced constipation mice, F. indica (27.3 and 34.6%) and ursolic acid (15 and 28%) also displayed laxative effects at the aforementioned doses. In mice and rats ileum, F. indica, its fractions (ethyl acetate, aqueous) and ursolic acid produced atropine-sensitive stimulatory effects, while in rats ileum, F. indica and aqueous fraction showed partially atropine-sensitive effects. F. indica and ursolic acid possess laxative and species-specific gut stimulant effects predominantly involving the activation of muscarinic receptor, thus eliciting its folk use in constipation. Video Clip of Methodology: 7 min 7 sec: Full Screen Alternate
Publisher: Elsevier BV
Date: 11-2014
Abstract: Almonds are reported to be protective against cardiovascular diseases (CVDs) however, the possible mode of action has only infrequently been explored. This study aimed at investigating the mechanistic basis for the benefits of almonds in atherosclerotic CVDs. Three studies in 3 groups of rats were designed with the use of tyloxapol (study 1), a high-fat diet (HFD study 2), and white-flour fructose (WFF study 3). In each of the studies, the first group acted as the control [administered saline in study 1 and fed a normal diet (ND) in studies 2 and 3] the second and third groups were treated with tyloxapol in study 1, an HFD in study 2, and WFF in study 3. The third group in each study was also fed almonds (3 g/kg) for 4 wk, after which blood was collected for biochemical evaluation. Livers and aortas were isolated from the rats in studies 1 and 2 for enzyme assays and vascular analysis, respectively. Almond supplementation significantly (P 0.05). Almonds partially restored the vascular reactivity of isolated aortas and prevented HFD-induced endothelial dysfunction by reducing inhibition of endothelial nitric oxide (NO) synthase and promoting NO release. The 70% decrease in HDL cholesterol that was observed in the WFF group was prevented by almond supplementation serum and LDL cholesterol were also normalized. The inhibition of de novo cholesterol synthesis, prevention of hepatic damage, and restoration of vascular function via the protection of endothelium and influence on the NO pathway are some of the mechanisms underlying the medicinal value of almonds in CVDs.
Publisher: Springer Science and Business Media LLC
Date: 18-01-2017
Publisher: Portland Press Ltd.
Date: 11-1998
DOI: 10.1042/BST026S342
Publisher: Ovid Technologies (Wolters Kluwer Health)
Date: 1999
Publisher: Elsevier BV
Date: 08-2015
Publisher: Elsevier BV
Date: 10-2002
DOI: 10.1016/S0031-9422(02)00190-5
Abstract: Two triterpenoids, 20beta-acetoxy-2alpha,3beta-dihydroxyurs-12-en-28-oic acid (guavanoic acid, 3), and 2alpha,3beta-dihydroxy-24-p-z-coumaroyloxyurs-12-en-28-oic acid (guavacoumaric acid, 7), along with six known compounds 2alpha-hydroxyursolic acid (1), jacoumaric acid (2), isoneriucoumaric acid (4), asiatic acid (5), ilelatifol D (6) and beta-sitosterol-3-O-beta-D-glucopyranoside (8), have been isolated from the leaves of Psidium guajava. Their structures were determined through spectroscopic methods. Compound 5 showed dose-dependent (10-500 microg/ml) spasmolytic activity in spontaneously contracting isolated rabbit jejunum preparations.
Publisher: Elsevier BV
Date: 09-2005
DOI: 10.1016/J.JEP.2005.05.010
Abstract: Crude extract of Valeriana wallichii rhizome (Vw.Cr) and its fractions were studied for possible antispasmodic and blood pressure lowering activities to rationalize some of the folkloric uses. In rabbit jejunum preparations, Vw.Cr (0.1-3.0 mg/mL) caused relaxation of spontaneous contractions. When tested against high K(+) (80 mM)-induced contractions it produced weak inhibitory effect, while caused complete relaxation of the contractions induced by low K(+) (20 mM). In the presence of glibenclamide (3 microM), the inhibitory effect of low K(+) was shifted to the right, similar to that produced by cromakalim while, verapamil caused no differentiation in its inhibitory effect against low and high K(+)-induced contractions. In guinea pig ileum, the plant extract produced similar results as in rabbit jejunum. Intravenous administration of Vw.Cr, produced fall in arterial blood pressure in normotensive anaesthetized rats and this effect was partially blocked by glibenclamide. In rabbit aortic preparations, plant extract also caused a selective and glibenclamide-sensitive relaxation of low K(+) (20 mM)-induced contractions. Activity-directed fractionation studies revealed that the observed activity was distributed both in the chloroform and aqueous fractions. These results indicate that the antispasmodic and hypotensive effects of Valeriana wallichii are mediated possibly through K(ATP) channel activation, which justify its use in gastrointestinal and cardiovascular disorders.
Publisher: Wiley
Date: 11-1995
Publisher: Elsevier BV
Date: 06-2021
Publisher: SAGE Publications
Date: 08-11-2016
Abstract: Polygonatum verticillatum has traditionally been used for various purposes. The present study was aimed to validate the antispasmodic and antidiarrheal properties of crude methanolic extract of rhizomes of P. verticillatum (PR). Isolated rabbit jejunum preparations were suspended in tissue baths to measure the isotonic responses using Power Lab data acquisition system for the antispasmodic activity of PR, while the antidiarrheal activity was conducted in vivo in mice. PR caused complete relaxation of the spontaneous contractions of isolated rabbit jejunum preparations in a dose-dependent mode. A complete inhibition was observed against low potassium (K + 25 mM)-induced contractions, while the plant extract partially inhibited the high K + (80 mM)-induced contractions. From a mechanistic point of view, the spasmolytic effect of PR against low K + was antagonized by glibenclamide similar to the effect of cromakalim, thus showing the presence of constituents in PR mediating spasmolytic activity predominantly through the activation of adenosine triphosphate-sensitive K + channels. When tested against castor oil-induced diarrhea in mice, oral administration of the plant extract manifested marked antidiarrheal activity at the doses of 500 and 1000 mg/kg similar to loperamide. This study provided a pharmacological basis for the medicinal use of PR in abdominal colic and diarrhea.
Publisher: Elsevier BV
Date: 06-2011
DOI: 10.1016/J.JEP.2011.03.064
Abstract: Areca catechu, commonly known as betel nut, is very famous for its medicinal use in multiple disorders. It is also popular as a remedy against inflammatory disorders in the Unani (Greco-Arab) system of medicine. This study was aimed at investigating the anti-inflammatory and analgesic activities of the crude extract of Areca catechu and its respective fractions. Paw edema, formalin-induced nociception and acetic acid-induced writhing assays were carried out in vivo. Free radical scavenging activity of the plant extract was performed in vitro. Preliminary experiments using a single dose (100 mg/kg) of Areca catechu and its respective fractions demonstrated an anti-inflammatory effect on carrageenan-induced edema in mice and rats, the aqueous fraction being distinctly more effective. When studied on prostaglandin E₂ (PGE₂), arachidonic acid, histamine, or serotonin (5HT)-induced edema in rats, Areca catechu and its aqueous fraction markedly repressed only the PGE₂ and arachidonic acid-induced inflammation. When studied for analgesic activity, the crude extract and its aqueous fraction produced a dose-dependent (10-100 mg/kg) inhibitory effect on formalin-induced nociception in mice and acetic acid-induced writhing in rats, similar to aspirin. In DPPH assay, Areca catechu and its aqueous fraction exhibited free radical scavenging activity with respective IC(50) values of 5.34 μg/ml (4.93-5.78, CI 95%, n=5) and 7.28 μg/ml (6.04-7.95, n=4), like that of rutin with IC(50) value of 4.75 μg/ml (3.89-5.42, n=4). These results indicate the anti-inflammatory and analgesic effects of Areca catechu and provide a rationale for its medicinal use in inflammatory disorders.
Publisher: Springer Science and Business Media LLC
Date: 19-07-2023
DOI: 10.1186/S13006-023-00571-3
Abstract: Breastfeeding is important for both mother and child in reducing risk of future cardiovascular disease. Therefore, it may be an effective method to improve cardio-metabolic health, particularly those who are exposed to pregnancy complications which increase later CVD risk for both mother and child. The aim of this study is to assess differences in cardiometabolic health at three years postpartum in mothers who breastfed for at least six months and their children compared to those who did not. Women and children from the Screening Tests to Predict Poor Outcomes of Pregnancy (STOP) study (2015–2017) were invited to attend a health check-up at three years postpartum. Women’s breastfeeding status at least six months postpartum was ascertained through their child health record. Anthropometric and hemodynamic measurements were taken from women and their children. A fasting blood s le was taken from women to measure blood glucose and lipids. A total of 160 woman-child dyads were assessed in this study. Women who breastfed for at least six months had significantly lower maternal BMI, systolic blood pressure, diastolic blood pressure, mean arterial pressure, central systolic blood pressure, and central diastolic blood pressure than those who did not and this did not change after adjusting for BMI and socioeconomic index in early pregnancy, prenatal smoking and maternal age in early pregnancy. Subgroup analysis on women who had one or more pregnancy complications during the index pregnancy (i.e. preecl sia, gestational hypertension, delivery of a small for gestational age infant, delivery of a preterm infant, and/or gestational diabetes mellitus) demonstrated that women who breastfed for at least six months had significantly lower maternal systolic and diastolic blood pressures, serum insulin and triglycerides, and higher HDL cholesterol. There were no differences in child anthropometric or hemodynamic variables at three years of age between those children who had been breastfed for at least six months and those who had not. Breastfeeding for at least six months may reduce some maternal cardiovascular risk factors in women at three years postpartum, in particular, in those who have experienced a complication of pregnancy. ACTRN12614000985684 (12/09/2014).
Publisher: Wiley
Date: 2005
DOI: 10.1002/PTR.1632
Abstract: The effect of a crude extract of the aerial parts of Artemisia vulgaris (Av.Cr) was investigated against D-galactosamine (D-GalN) and lipopolysaccharide (LPS) induced hepatitis in mice. Co-administration of D-GalN (700 mg[sol ]kg) and LPS (1 microg[sol ]kg) significantly (p < 0.05) raised the plasma levels of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) in mice in the toxin group compared with the values in the control group. Pre-treatment of mice with different doses of Av.Cr (150-600 mg[sol ]kg) significantly (p < 0.05) reduced the toxin-induced rise in plasma ALT and AST. The hepatoprotective effect was further verified by histopathology of the liver, which showed improved architecture, absence of parenchyma congestion, decreased cellular swelling and apoptotic cells, compared with the findings in the toxin group of animals. These findings scientifically validated the traditional use of Artemisia vulgaris for various liver disorders.
Publisher: Wiley
Date: 2005
DOI: 10.1002/PTR.1753
Abstract: Raphanus sativus, commonly known as radish, is a food plant known worldwide for its culinary and medicinal properties especially as a laxative and abortifacient. This study reports the gastrointestinal and uterine tone modulatory activities of the crude extract (Rl.Cr) of radish leaves. Rl.Cr, showing the presence of saponins and alkaloids, exhibited a spasmogenic effect (0.03-10 mg/mL) in isolated rabbit jejunum, rat stomach fundus and uterus which was partially blocked by atropine. In contrast, Rl.Cr was found to be devoid of any stimulatory effect in rat ileum, instead showed an inhibitory effect (0.1 mg/mL) on the ACh dose-response curves. A mild relaxant effect was also observed in rabbit jejunum at the lower doses (0.1-0.3 mg/mL) but not against K(+)-induced contractions, ruling out a calcium channel blocking effect. In guinea-pig ileum, Rl.Cr exhibited a stimulant effect resistant to atropine while sensitive to pyrilamine pretreatment. The aqueous fraction, showing a strong presence of saponins, was found to be more efficacious than the non-polar fractions in its spasmogenic effect. This study shows the presence of species-dependent gastrointestinal effects of radish mediated partially through cholinergic receptors in rabbit and rat tissues, but through histaminergic activation in the guinea-pig, providing a scientific basis for its use in gut and uterine affections while also giving a wider picture of the activity profile of radish by using different species of animals.
Publisher: F1000 Research Ltd
Date: 02-12-2021
DOI: 10.12688/F1000RESEARCH.74926.1
Abstract: PCAD possesses a public health challenge resulting in years of productive life lost and an escalating burden on health systems. Objective of this review is to compare modifiable and non-modifiable risk factors for PCAD compared to those without PCAD. This review will include all comparative observational studies conducted in adults aged 18 years with confirmed diagnosis of PCAD (on angiography) compared to those without PCAD. Databases to be searched include PubMed, CINAHL, Embase, Web of Science, and grey literature (Google Scholar). All identified studies will be screened for title and abstract and full-text against the inclusion criteria on Covidence software. Data relevant to exposures and outcomes will be extracted from all included studies. All studies selected for data extraction will be critically appraised for methodological quality. Meta-analysis using random-effects model will be performed using Review Manager 5.3. Effect sizes for categorical risk factors will be expressed as odds ratios with 95% confidence intervals. For risk factors measured in continuous form, mean difference (if units are consistent) otherwise standardized mean difference (if units are different across studies) will be reported. Heterogeneity between studies will be assessed using I 2 test statistics. GRADE will be used to assess the certainty of the findings. Systematic review registration number: PROSPERO Registration # CRD42020173216
Publisher: Elsevier BV
Date: 11-2014
Publisher: Elsevier BV
Date: 11-2014
Publisher: Science Alert
Date: 15-12-2006
Publisher: Informa UK Limited
Date: 1994
Publisher: Canadian Science Publishing
Date: 11-2008
DOI: 10.1139/Y08-084
Abstract: Paeonia emodi (peony) is a well known plant used medicinally to treat hypertension, palpitations, and asthma. Despite its popularity, there are few reports in the scientific literature examining its use in such conditions. We prepared a 70% ethanolic extract of peony root (Pe.Cr) and applied it to segments of guinea pig atria and trachea and rat aorta suspended separately in tissue baths. Activity against arachidonic acid (AA)-induced platelet aggregation was measured in human platelet-rich plasma. Airway relaxant effect was evaluated against acetylcholine (ACh)-induced airway contraction in mouse lung slices loaded with fluo-4. Pe.Cr (0.3–10 mg/mL) showed an atropine-resistant negative inotropic effect in atria. In rat aorta, an endothelium-independent vasodilatory effect (0.3–10 mg/mL) was seen in phenylephrine- and high-K + -induced contractions. Pe.Cr (0.01–1 mg/mL) also inhibited AA-induced platelet aggregation. In isolated trachea, Pe.Cr (0.3–10 mg/mL) relaxed carbachol- and histamine-induced contractions independently of β-adrenergic receptors. In mouse lung slices, Pe.Cr (0.3–1 mg/mL) inhibited ACh-induced airway narrowing and oscillations of intracellular Ca 2+ in airway smooth muscle cells. The results showed cardiosuppressant, vasodilatory, antiplatelet, and tracheal and airway relaxant activities of peony, providing potential justification for its medicinal use in different hyperactive cardiovascular and respiratory disorders.
Publisher: Elsevier BV
Date: 09-1998
Publisher: Research Square Platform LLC
Date: 30-03-2022
DOI: 10.21203/RS.3.RS-1300678/V1
Abstract: Background Microvascular angina (MVA) is increasingly recognized as an endotype of ischaemia with no obstructive coronary artery disease (INOCA), but assessment remains difficult while validated diagnostic investigation is invasive. This pilot study assessed the correlation between left ventricular contractile reserve (CR), measured via speckle-tracking imaging on low dose dobutamine stress echocardiography (DSE) and the invasive coronary microvascular function in patients with INOCA. Methods Forty-two patients with INOCA and abnormal coronary vasomotor dysfunction were prospectively screened at a single tertiary centre covering the Northern metropolitan area of South Australia, from February 2018 to December 2020 (ACTRN12618000149268). Forty patients were invited into to the DSE study after coronary angiography demonstrated NOCAD and abnormal coronary epicardial and microvascular function (n = 40). Results: Of the 40 participants undergoing DSE study, 30 were suitable to be included in the final analysis. Average age of 54.8 ± 10.8 years old and more female (76.2%) than male recruited. 92.1% of patients were of Caucasian ethnicity. 65.8% were considered obese. The study cohort demonstrating a degree of angina burden, with 73.7% experiencing once angina in a week. Weak positive association between CR with hyperaemic microvascular resistance (HMR) at 5mcg/kg/min, CR(absolute) (r=0.427, p-value=0.019) between 5 and 10 mcg/kg/min, CR(absolute) (r = 0.481, p-value = 0.007). The relationship between CR and HMR showed a trend of increase in CR at a DSE of 5mcg/kg/min, but a blunted response at the higher doses of 10 and 20mcg/kg/min (p=0.400). Weak positive association between CR with coronary flow reserve (CFR) at 5mcg/kg/min, CR(absolute) (r = 0.442, p-value = 0.015). The relationship between CR and CFR showed a trend of increase in CR at a DSE of 5mcg/kg/min, but a blunted response at the higher doses of 10 and 20mcg/kg/min (p=0.393). Conclusion: This pilot study has provided the possible utility of speckle tracking technique in assessment of INOCA with a MVA endotype.
Publisher: Wiley
Date: 16-06-2009
DOI: 10.1002/PTR.2859
Abstract: This study was aimed to provide a pharmacological basis to the medicinal use of Alstonia scholaris as an antidiarrhoeal and antispasmodic by using in vivo and in vitro techniques. In the in vivo study the crude extract of Alstonia scholaris (As.Cr), which tested positive for the presence of alkaloids, provided 31-84% protection against castor oil-induced diarrhoea in mice at 100-1000 mg/kg doses, similar to loperamide. In isolated rabbit jejunum preparation, the As.Cr caused inhibition of spontaneous and high K(+) (80 mm)-induced contractions, with respective EC(50) values of 1.04 (0.73-1.48) and 1.02 mg/mL (0.56-1.84 95% CI), thus showing spasmolytic activity mediated possibly through calcium channel blockade (CCB). The CCB activity was further confirmed when pretreatment of the tissue with the As.Cr (0.3-1 mg/mL) caused a rightward shift in the Ca(++) concentration-response curves similar to verapamil, a standard calcium channel blocker. Loperamide also inhibited spontaneous and high K(+) precontractions as well as shifted the Ca(++) CRCs to the right. These results indicate that the crude extract of Alstonia scholaris possesses antidiarrhoeal and spasmolytic effects, mediated possibly through the presence of CCB-like constituent(s) and this study provides a mechanistic base for its medicinal use in diarrhoea and colic.
Publisher: Wiley
Date: 29-12-2009
DOI: 10.1002/PTR.2979
Abstract: This study describes the gut, airways and cardiovascular modulatory activities of Zanthoxylum armatum DC. (Rutaceae) to rationalize some of its medicinal uses. The crude extract of Zanthoxylum armatum (Za.Cr) caused concentration-dependent relaxation of spontaneous and high K(+) (80 mM)-induced contractions in isolated rabbit jejunum, being more effective against K(+) and suggestive of Ca(++) antagonist effect, which was confirmed when pretreatment of the tissues with Za.Cr shifted Ca(++) concentration-response curves to the right, like that caused by verapamil. Za.Cr inhibited the castor-oil-induced diarrhea in mice at 300-1000 mg/kg. In rabbit tracheal preparations, Za.Cr relaxed the carbachol (1 microM) and high K(+)-induced contractions, in a pattern similar to that of verapamil. In isolated rabbit aortic rings, Za.Cr exhibited vasodilator effect against phenylephrine (1 microM) and K(+)-induced contractions. When tested in guinea pig atria, Za.Cr caused inhibition of both atrial force and rate of spontaneous contractions, like that caused by verapamil. These results indicate that Zanthoxylum armatum exhibits spasmolytic effects, mediated possibly through Ca(++) antagonist mechanism, which provides pharmacological base for its medicinal use in the gastrointestinal, respiratory and cardiovascular disorders.
Publisher: Elsevier BV
Date: 09-2016
DOI: 10.1016/J.INTIMP.2016.04.043
Abstract: New treatments for inflammatory bowel disease are of interest due to high rate of remission failure. Natural products have been effective in IBD therapeutics as they have multiple constituents. The aim of the present study was to evaluate the effect of Flaxseed extract (Fs.Cr) on ulcerative colitis and identify the possible mechanisms involved. Colitis was induced by intrarectal administration of 6% AA in BALB/c mice. Colonic mucosal damage was assessed after 24h by calculating disease activity index (DAI), macroscopic and histological damage scores, biochemical measurement of myeloperoxidase (MPO), malondialdehyde (MDA), superoxide dismutase (SOD), glutathione peroxidase (GPx), catalase (CAT), and total glutathione activities. Since cytokines are involved in exacerbating inflammatory cascade with emerging role of innate immune cytokines in IBD therapeutics, we hence assessed the effect on the levels of TNF-α, IFN-γ and IL-17, at 6, 12 and 24h by ELISA. Fs.Cr ameliorated the severity of AA colitis as evident by improved DAI, macroscopic damage and the histopathological scores along with restoration of goblet cells. Fs.Cr decreased MDA and MPO activities and enhanced antioxidant activity compared to the AA group. Finally, Fs.Cr in doses (300 and 500mg/kg) decreased TNF-α and IFN-γ levels at all time points with simultaneous increase in IL-17 levels at 24h as compared to the AA group. These results suggest that Fs.Cr ameliorates the severity of AA colitis by reducing goblet cell depletion, scavenging oxygen-derived free radicals, reduce neutrophil infiltration that may be attributed due to decreasing IFN-γ and TNF-α and increasing IL-17 levels.
Publisher: Wiley
Date: 26-11-2009
DOI: 10.1002/PTR.2980
Abstract: Three extracts of Valeriana wallichii DC (Valerianaceae) rhizome and fluoxetine were studied for antidepressant-like activity in two behavioral models, namely the forced swim test (FST) and the tail suspension test (TST). Fluoxetine as well as methanolic and aqueous extracts of V. wallichii induced monophasic dose-related decrements in immobility times in both tests. However, the aqueous-ethanolic fraction induced a biphasic dose-response profile since it produced a graded effect up to 200 mg/kg but the highest dose (250 mg/kg) was inactive in the FST. This extract also exhibited significantly reduced activity at 200 mg/kg compared to lower doses in the TST. The highest doses of aqueous-ethanolic extract also reduced locomotor activity which will have led to a negative functional interaction with antidepressant-like effects. Qualitative phytochemical analysis revealed that the aqueous-ethanolic extract of V. wallichii was the only separated rhizome fraction containing terpenoids. Furthermore, since the methanolic and aqueous extracts were active in the tests, it is suggested that the antidepressant-like action of this herbal plant is not contingent upon its terpenoid constituents.
Publisher: Elsevier BV
Date: 2005
DOI: 10.1016/J.JEP.2004.10.010
Abstract: The crude extract of Fumaria indica whole plant (Fi.Cr) and its fractions were studied in vitro for spasmogenic and spasmolytic effects to rationalize some of the traditional uses. Fi.Cr (1.0-5.0 mg/mL) caused a moderate degree of atropine-sensitive spasmogenic effect in guinea-pig ileum. In spontaneously contracting rabbit jejunum, Fi.Cr (0.03-0.3 mg/mL) caused a mild spasmogenicity followed by relaxation at the higher doses. In the atropinized preparations, Fi.Cr inhibited spontaneous and K(+)-induced contractions at the similar doses (0.1-1.0 mg/mL), which suggests calcium channel blockade (CCB). CCB effect was confirmed when pretreatment of the tissue with the Fi.Cr produced a dose-dependent shift in the Ca(2+) dose-response curves to the right, similar to that produced by verapamil. Activity-directed fractionation revealed that the spasmolytic effect is concentrated in the petroleum ether fraction, while dichloromethane fraction contains both spasmogenic and spasmolytic constituents. These data indicate that the presence of cholinergic and CCB constituents in Fi.Cr may explain the respective traditional use of Fumaria indica in constipation and diarrhoea.
Publisher: Elsevier BV
Date: 07-2015
DOI: 10.1016/J.JEP.2015.03.064
Abstract: This study was planned to assess pharmacological basis for the medicinal use of Flaxseed in constipation and diarrhea. The oil and mucilage of Flaxseeds were studied for their laxative, and antidiarrheal activities in mice. The mechanisms of laxative and antidiarrheal activities were further studied using the isolated tissue preparations (rabbit jejunum and guinea-pig ileum) immersed in Tyrode׳s solution maintained at 37°C and aerated with carbogen gas. Isotonic responses were measured on spontaneously contracting isolated jejunum and guinea-pig ileum preparations. Oral administration of Flaxseed oil (30 and 70mg/kg, orally) and mucilage (1 and 2.5g/kg, orally) caused dose-dependent increase in wet feces in mice. The spasmogenic effect of Flaxseed oil was partially blocked by pyrilamine (p<0.05) and atropine (p<0.01) in isolated rabbit jejunum whereas atropine completely blocked the effect of Flaxseed mucilage on isolated guinea-pig ileum. When studied for its antidiarrheal effect, Flaxseed oil reduced the castor oil-induced diarrheal score by 49.35% and 84.41% and intestinal secretions by 19% and 33.62% at the oral doses of 100 and 300mg/kg respectively. In isolated rabbit jejunum preparations, Flaxseed oil produced a dose-dependent inhibition of both spontaneous and low K(+) (25mM) -induced contractions in rabbit jejunum. The inhibitory effect against low K(+) was most sensitive to tetra-ethylammonium chloride, a non-specific K(+) channel blocker, followed by glibenclamide, a partial ATP-dependent K(+) channels blocker and 4-Aminopyridine, a voltage gated K(+)-channel blocker. Our results indicate that Flaxseed oil and mucilage exhibit laxative activity, mediated primarily through cholinergic pathway with weak histaminergic effect component evident in Flaxseed oil, which also showed antidiarrheal activity, mediated possibly through K(+) channels activation. Thus this study rationalizes the medicinal use of Flaxseed in both the constipation and diarrhea with sound mechanistic basis.
Publisher: Elsevier BV
Date: 05-2005
DOI: 10.1016/J.LFS.2004.12.021
Abstract: This study was carried out to provide scientific basis for the medicinal use of turmeric (Curcuma longa) in gastrointestinal and respiratory disorders. The crude extract of turmeric (Cl.Cr), relaxed the spontaneous and K+ (80 mM)-induced contractions in isolated rabbit jejunum as well as shifted the CaCl2 concentration-response curves. In rabbit tracheal preparation, Cl.Cr inhibited carbachol and K(+)-induced contractions. In anesthetized rats, Cl.Cr produced variable responses on blood pressure with a mixture of weak hypertensive and hypotensive actions. In rabbit aorta, Cl.Cr caused a weak vasoconstrictor and a vasodilator effect on K+ and phenylephrine-induced contractions. In guinea-pig atria, Cl.Cr inhibited spontaneous rate and force of contractions at 14-24 times higher concentrations. Activity directed fractionation revealed that the vasodilator and vasoconstrictor activities are widely distributed in the plant with no clear separation into the polar or non-polar fractions. When used for comparison, both curcumin and verapamil caused similar inhibitory effects in all smooth muscle preparations with relatively more effect against K(+)-induced contractions and that both were devoid of any vasoconstrictor effect and curcumin had no effect on atria. These data suggest that the inhibitory effects of Cl.Cr are mediated primarily through calcium channel blockade, though additional mechanism cannot be ruled out and this study forms the basis for the traditional use of turmeric in hyperactive states of the gut and airways. Furthermore, curcumin, the main active principle, does not share all effects of turmeric.
Publisher: Pakistan Journal of Botany
Date: 25-02-2019
Publisher: Springer Science and Business Media LLC
Date: 24-11-2012
Abstract: Although Group A beta hemolytic streptococcus (GABHS) can cause bacterial pharyngitis, the most common etiology is viral despite this viral etiology, antibiotics are commonly prescribed for this infection in industrialized countries. We investigated the prevalence of GABHS in adult pharyngitis patients from lower socioeconomic settings in Karachi, Pakistan, how often antibiotics are prescribed for pharyngitis and if appropriate agents were used in a developing world setting. Finally, we wanted to see the usefulness of modified McIsaac scores in predicting positive cultures. Adult patients were recruited from three local hospital outpatient dispensaries (OPDs). All patients aged 14–65 years who were suspected of having bacterial pharyngitis had throat swabs taken. Laboratory results for GABHS pharyngitis were then compared with their prescriptions. Appropriateness (using the World Health Organization’s definition) and type of antibiotic prescribed were assessed. Of 137 patients , 30 patients each were studied for scores of 0, 1, 2 and 3 17 patients were studied for score 4. Although 6 (4.4%) patients were GABHS +, for a prevalence of 43.8 per 1000 population, antibiotics were prescribed to 135 patients (98.5%). Of these, only 11.1% received appropriate antibiotics while 88.9 % received inappropriate antibiotics . Penicillins were prescribed most (34.1%), especially amoxicillin/clavulanate followed by macrolides (31.1%), especially the second-generation agents, and fluoroquinolones (14.8%). McIsaac scores were found to be 100% sensitive and 68.7% specific, giving a positive predictive value (PPV) of 12.7% and a negative predictive value (NPV) of 100%. Antibiotics were prescribed irrationally to adult pharyngitis patients, as most cultures were negative for bacterial infection. McIsaac modification of Centor scores related directly to culture results. We would therefore highly recommend its use to help family physicians make treatment decisions for adult pharyngitis patients.
Publisher: Springer Science and Business Media LLC
Date: 04-1995
DOI: 10.1007/BF02979146
Publisher: Oxford University Press (OUP)
Date: 04-1992
Abstract: A 69 year old woman was treated with sotalol (320 mg daily) for intermittent atrial fibrillation. Sotalol was initially well tolerated and reversion to sinus rhythm with sinus bradycardia occurred 4 weeks after initiation of therapy. Shortly thereafter, the patient developed recurrent syncope due to torsade de pointes. This was treated successfully with intravenous magnesium infusion and withdrawal of sotalol. Subsequently, the atrial fibrillation was adequately managed using amiodarone, with no recurrence of torsade de pointes. Development of bradycardia associated with reversion to sinus rhythm represents a potential cause of 'late' pro-arrhythmic effects of sotalol.
Publisher: Science Alert
Date: 15-06-2017
Publisher: Elsevier BV
Date: 05-2012
DOI: 10.1016/J.JEP.2012.03.001
Abstract: Helicobacter pylori infection is associated with gastritis, peptic ulcer, and gastric cancer. Due to its high global prevalence and uprising resistance to available antibiotics, efforts are now directed to identify alternative source to treat and prevent associated disorders. In the present study, effect of selected indigenous medicinal plants of Pakistan was evaluated on the secretion of interleukin-8 (IL-8) and generation of reactive oxygen species (ROS) in a bid to rationalize their medicinal use and to examine the anti-inflammatory and cytoprotective effects in gastric epithelial cells. AGS cells and clinically isolated Helicobacter pylori strain (193C) were employed for co-culture experiments. Anti-Helicobacter pylori activity and cytotoxic effects of the selected plants were determined by serial dilution method and DNA fragmentation assay respectively. ELISA and flow cytometry were performed to evaluate the effect on IL-8 secretion and ROS generation in Helicobacter pylori-infected cells. At 100μg/ml, extracts of Alpinia galangal, Cinnamomum cassia, Cinnamomum tamala, Mentha arvensis, Myrtus communis, Oligochaeta ramose, Polygonum bistorta, Rosa damascena, Ruta graveolens, Syzygium aromaticum, Tamarix dioica, and Terminalia chebula exhibited strong inhibitory activity against IL-8 secretion. Of these, four extracts of Cinnamomum cassia, Myrtus communis, Syzygium aromaticum, and Terminalia chebula markedly inhibited IL-8 secretion at both 50 and 100μg/ml. Cinnamomum cassia was further assessed at different concentrations against Helicobacter pylori and TNF-α stimulated IL-8 secretion, which displayed significant suppression of IL-8 in a concentration-dependent-manner. Among the plants examined against ROS generation, Achillea millefolium, Berberis aristata, Coriandrum sativum, Foeniculum vulgare, Matricaria chamomilla and Prunus domestica demonstrated significant suppression of ROS from Helicobacter pylori-infected cells (p<0.01). Results of the study revealed anti-inflammatory and cytoprotective effects of selected medicinal plants which could partially validate the traditional use of these plants in GI disorders particularly associated with Helicobacter pylori. Furthermore, results obtained may lead to possible future candidates of chemoprevention against peptic ulcer or gastric cancer.
Publisher: Bangladesh Journals Online (JOL)
Date: 10-06-2011
Publisher: Wiley
Date: 2002
DOI: 10.1002/PTR.886
Abstract: The crude extract of psyllium husk (ispaghula) and its active constituent (petroleum fraction) caused varying degrees of growth inhibition in three different species of Entamoeba, i.e. Entamoeba histolytica, E. invadens and E. dispar. The inhibitory effect of the crude extract was in the dose range of 1-10 mg/mL, whereas a similar inhibitory effect was obtained with the petroleum fraction at a much lower dose (0.1-1.0 mg/mL), indicating that the active chemical(s) is/are concentrated in the petroleum fraction. These data support the traditional use of psyllium husk in amoebic dysentery.
Publisher: Elsevier BV
Date: 05-2005
DOI: 10.1016/J.EJPHAR.2005.02.041
Abstract: Metabolic acidosis is associated with various clinical situations including diabetes mellitus and renal diseases. The aim of this study was to investigate the effects of acidosis on the resting as well as precontracted human left internal mammary artery. The vessels were obtained from the patients undergoing coronary artery bypass grafting surgery at The Aga Khan University Hospital, Karachi. Left internal mammary artery was cut into rings and isometric tension recording experiments were performed. Decrease in pH of the bathing solution from 7.4 to 6.8 had no effect on the resting tension of left internal mammary artery, whereas, acidic pH markedly relaxed the contractions to 24.8 mM KCl and 300 nM phenylephrine. Interestingly, when the KCl- or phenylephrine-contracted rings were treated with 3 microM glibenclamide an inhibitor of ATP-sensitive potassium (K(ATP)) channels, the relaxant effect of acidosis was abolished. Similarly, acidosis failed to cause relaxation of 100 nM endothelin-1-induced contraction in Ca2+-free bathing solution or in the presence of a voltage-dependent Ca2+ channel inhibitor, verapamil (10 microM), whereas, endothelin-1-induced contraction was attenuated by acidosis in Ca2+-containing normal solution. From all these data, it is concluded that under the acidic pH conditions, opening of K(ATP) channels occurs resulting in the hyperpolarization, decrease in Ca2+ influx via voltage-dependent Ca2+ channels and subsequent relaxation of human left internal mammary artery.
Publisher: Wiley
Date: 2000
DOI: 10.1002/1099-1573(200009)14:6<436::AID-PTR620>3.0.CO;2-C
Abstract: The crude aqueous extract of Piper betle leaves (Pb.Cr) was studied for the possible presence of cholinomimetic and calcium channel antagonist constituents. Pb.Cr at doses of 1-10 mg/mL caused a moderate spasmogenic effect in isolated guinea-pig ileum and this activity was concentrated in the aqueous fraction, which was found to be about 5 times more potent. Pretreatment of the tissue with atropine (1 microM) but not hexamethonium (100 microM) completely abolished the contractile effect of the aqueous fraction indicating a cholinergic (muscarinic) mechanism. In isolated rabbit jejunum preparations Pb.Cr did not produce a significant increase in the spontaneous contractions, but instead produced a dose-dependent (0.03-3.0 mg/mL) inhibition of spontaneous activity. Activity-directed fractionation revealed that the spasmolytic action was concentrated in the ethyl acetate fraction. When tested against K(+)-induced contractions, both Pb.Cr and its ethyl acetate fraction (Pb.EtAc) caused a dose-dependent inhibition, suggesting calcium channel blockade (CCB). The potent CCB effect of the crude extract and its ethyl acetate fraction was confirmed when pretreatment of the tissue with Pb.Cr or Pb.EtAc shifted the Ca(++) dose-response curves to the right in a dose-dependent manner. These data indicate that the plant contains cholinomimetic and possible calcium channel antagonist constituents, which are concentrated in the aqueous and ethyl acetate fractions respectively. It is suggested that some of the traditional uses of this plant may be explained on the basis of these activities.
Publisher: Wiley
Date: 15-08-2007
Publisher: Science Alert
Date: 08-2016
Publisher: Elsevier BV
Date: 07-2011
DOI: 10.1016/J.BRAINRES.2011.05.022
Abstract: Alzheimer's disease (AD) is a neurodegenerative disorder, which depicts features of chronic inflammatory conditions resulting in cellular death and has limited therapeutic options. We aimed to explore the effect of a curcuminoid mixture and its in idual components on inflammatory and apoptotic genes expression in AD using an Aβ+ibotenic acid-infused rat model. After 5 days of treatment with demethoxycurcumin, hippoc al IL-1β levels were decreased to 118.54 ± 47.48 and 136.67 ± 31.96% respectively at 30 and 10mg/kg, compared with the amyloid treated group (373.99 ± 15.28%). After 5 days of treatment, the curcuminoid mixture and demethoxycurcumin effectively decreased GFAP levels in the hippoc us. When studied for their effect on apoptotic genes expression, the curcuminoid mixture and bisdemethoxycurcumin effectively decreased caspase-3 level in the hippoc us after 20 days of treatment, where bisdemethoxycurcumin showed a maximal rescuing effect (92.35 ± 3.07%) at 3mg/kg. The curcuminoid mixture at 30 mg/kg decreased hippoc al FasL level to 70.56 ± 3.36% after 5 days of treatment and 19.01 ± 2.03% after 20 days. In the case of Fas receptor levels, demethoxycurcumin decreased levels after 5 days of treatment with all three doses showing a maximal effect (189.76 ± 15.01%) at 10mg/kg. Each compound was effective after 20 days in reducing Fas receptor levels in the hippoc us. This study revealed the important effect of curcuminoids on genes expression, showing that, each component of the curcuminoid mixture distinctly affects gene expression, thus highlighting the therapeutic potential of curcuminoids in AD.
Publisher: Georg Thieme Verlag KG
Date: 08-1994
Abstract: Coronavirus disease 2019 (COVID-19) disproportionately affects older people. Observational studies suggest indolent cardiovascular involvement after recovery from acute COVID-19. However, these findings may reflect pre-existing cardiac phenotypes. We tested the association of baseline cardiovascular magnetic resonance (CMR) phenotypes with incident COVID-19. We studied UK Biobank participants with CMR imaging and COVID-19 testing. We considered left and right ventricular (LV, RV) volumes, ejection fractions, and stroke volumes, LV mass, LV strain, native T1, aortic distensibility, and arterial stiffness index. COVID-19 test results were obtained from Public Health England. Co-morbidities were ascertained from self-report and hospital episode statistics (HES). Critical care admission and death were from HES and death register records. We investigated the association of each cardiovascular measure with COVID-19 test result in multivariable logistic regression models adjusting for age, sex, ethnicity, deprivation, body mass index, smoking, diabetes, hypertension, high cholesterol, and prior myocardial infarction. We studied 310 participants (n = 70 positive). Median age was 63.8 [57.5, 72.1] years 51.0% (n = 158) were male. 78.7% (n = 244) were tested in hospital, 3.5% (n = 11) required critical care admission, and 6.1% (n = 19) died. In fully adjusted models, smaller LV/RV end-diastolic volumes, smaller LV stroke volume, and poorer global longitudinal strain were associated with significantly higher odds of COVID-19 positivity. We demonstrate association of pre-existing adverse CMR phenotypes with greater odds of COVID-19 positivity independent of classical cardiovascular risk factors. Observational reports of cardiovascular involvement after COVID-19 may, at least partly, reflect pre-existing cardiac status rather than COVID-19 induced alterations.
Publisher: Springer Science and Business Media LLC
Date: 08-2007
DOI: 10.1007/BF02993965
Publisher: Science Alert
Date: 15-12-2006
Publisher: Elsevier BV
Date: 10-2004
Publisher: Portland Press Ltd.
Date: 04-1990
DOI: 10.1042/BST0180289
Publisher: Portland Press Ltd.
Date: 04-1990
DOI: 10.1042/BST0180288
Abstract: On terminally differentiated sperm cells, surface proteins are segregated into distinct surface domains that include the anterior and posterior head domains. We have analyzed the formation of the anterior and posterior head domains of guinea pig sperm in terms of both the timing of protein localization and the mechanism(s) responsible. On testicular sperm, the surface proteins PH-20, PH-30 and AH-50 were found to be present on the whole cell (PH-20) or whole head surface (PH-30, AH-50). On sperm that have completed differentiation (cauda epididymal sperm), PH-20 and PH-30 proteins were restricted to the posterior head domain and AH-50 was restricted to the anterior head domain. Thus these proteins become restricted in their distribution late in sperm differentiation, after sperm leave the testis. We discovered that the differentiation process that localizes these proteins can be mimicked in vitro by treating testicular sperm with trypsin. After testicular sperm were treated with 20 micrograms/ml trypsin for 5 min at room temperature, PH-20, PH-30, and AH-50 were found localized to the same domains to which they are restricted during in vivo differentiation. The in vitro trypsin-induced localization of PH-20 to the posterior head mimicked the in vivo differentiation process quantitatively as well as qualitatively. The quantitative analysis showed the process of PH-20 localization involves the migration of surface PH-20 from other regions to the posterior head domain. Immunoprecipitation experiments confirmed that there is protease action in vivo on the sperm surface during the late stages of sperm differentiation. Both the PH-20 and PH-30 proteins were shown to be proteolytically cleaved late in sperm differentiation. These findings strongly implicate proteolysis of surface molecules as an initial step in the mechanism of formation of sperm head surface domains.
Publisher: Portland Press Ltd.
Date: 04-1990
DOI: 10.1042/BST0180287
Publisher: Springer Science and Business Media LLC
Date: 10-2005
DOI: 10.1007/S10620-005-2957-2
Abstract: Ginger (rhizome of Zingiber officinale) has been widely used for centuries in gastrointestinal disorders, particularly dyspepsia, but its precise mode of action has yet to be elucidated. This study was undertaken to study the prokinetic action of ginger and its possible mechanism of action. Prokinetic activity of ginger extract (Zo.Cr) was confirmed in an in vivo test when it enhanced the intestinal travel of charcoal meal in mice. This propulsive effect of the extract, similar to that of carbachol, was blocked in atropine-pretreated mice, a standard cholinergic antagonist. Likewise, Zo.Cr showed an atropine-sensitive dose-dependent spasmogenic effect in vitro as well as in isolated rat and mouse stomach fundus tissues. In atropinized tissue, it showed spasmolytic activity as shown by the inhibition of 5-HT- and K+-induced contractions. A spasmolytic effect was also observed in other gut preparations either as noncompetitive inhibition of agonist dose-response curves, inhibition of high K+(80 mM)-induced contractions, or displacement of Ca2+ dose-response curves to the right, indicating a calcium antagonist effect. Phytochemical analysis revealed the presence of saponins, flavonoids, and alkaloids in the crude extract. These data indicate that Zo.Cr contains a cholinergic, spasmogenic component evident in stomach fundus preparations which provides a sound mechanistic insight for the prokinetic action of ginger. In addition, the presence of a spasmolytic constituent(s) of the calcium antagonist type may explain its use in hyperactive states of gut like colic and diarrhea.
Publisher: Wiley
Date: 18-11-2006
DOI: 10.1111/J.1472-8206.2005.00382.X
Abstract: In this study, we describe the hypotensive, cardio-modulatory and endothelium-dependent vasodilator actions of Raphanus sativus (radish) seed crude extract in an attempt to provide scientific basis for its traditional use in hypertension. The plant extract (Rs.Cr) was prepared in distilled water and was subjected to phytochemical screening using standard analytical procedures. In vivo blood pressure was monitored in anaesthetized normotensive rats. Isolated tissue preparations were suspended in tissue baths containing Kreb's solution while acute toxicity study was performed in mice for 24 h. Rs.Cr tested positive for the presence of saponins, flavonoids, tannins, phenols and alkaloids and caused a dose-dependent (0.1-3 mg/kg) fall in blood pressure and heart rate of rats that was mediated via an atropine-sensitive pathway. In isolated guinea-pig atria, Rs.Cr showed dose-dependent (0.03-3.0 mg/mL) inhibition of force and rate of contractions. In the atropine-treated tissues, the inhibitory effect was abolished and a cardiac stimulant effect was unmasked which was resistant to adrenergic and serotonergic receptor blockade. In the endothelium-intact rat aorta, Rs.Cr inhibited phenylephrine-induced contractions, which was blocked by atropine and Nomega-Nitro-L-arginine methyl ester hydrochloride while was also absent in the endothelium-denuded preparations. The extract was safe in mice up to the dose of 10 g/kg. The study shows that the cardiovascular inhibitory effects of the plant are mediated through activation of muscarinic receptors thus possibly justifying its use in hypertension.
Publisher: Hindawi Limited
Date: 2012
DOI: 10.1155/2012/596524
Abstract: Lepidium sativum is widely used in folk medicine for treatment of hyperactive airways disorders, such as asthma, bronchitis and cough. The crude extract of Lepidium sativum (Ls.Cr) inhibited carbachol (CCh, 1 μM-) and K + (80 mM-) induced contractions in a pattern similar to that of dicyclomine. Ls.Cr at 0.03 mg/mL produced a rightward parallel shift of CCh curves, followed by nonparallel shift at higher concentration (0.1 mg/mL), suppressing maximum response, similar to that caused by dicyclomine. Pretreatment of tissues with Ls.Cr (0.1–0.3 mg/mL) shifted Ca ++ concentration-response curves (CRCs) to right, as produced by verapamil. Ls.Cr at low concentrations (0.03–0.1 mg/mL) caused leftward shift of isoprenaline-induced inhibitory CRCs, like that caused by rolipram, a phosphodiesterase (PDE) inhibitor. These results indicate that bronchodilatory effect of Lepidium sativum is mediated through a combination of anticholinergic, Ca ++ antagonist and PDE inhibitory pathways, which provides sound mechanistic background for its medicinal use in the overactive airways disorders.
Publisher: American Chemical Society (ACS)
Date: 12-07-2000
DOI: 10.1021/NP9902340
Abstract: Phytochemical studies on the leaves of Eucalyptus camaldulensis var. obtusa have resulted in the isolation of a new triterpenoid camaldulin (3beta-formyloxyurs-11-en-28,13beta-olide) (1) along with ursolic acid lactone acetate (2), ursolic acid lactone (3), betulinic acid (4), and beta-sitosterol 3-O-beta-D-glucopyranoside (5). The structures were assigned on the basis of 1D and 2D NMR studies. Compounds 1-3 were tested for spasmolytic activity and were found to possess calcium antagonist activity.
Publisher: Science Alert
Date: 11-2012
Publisher: Oxford University Press (OUP)
Date: 10-2008
Abstract: Ginger rhizome (Zingiber officinale) has been used for centuries to treat dementia in South Asia. This study was undertaken to possibly justify its use. A 70% aqueous/methanolic extract of dried ginger (Zo.Cr) was used. Zo.Cr tested positive for the presence of terpenoids, flavonoids, secondary amines, phenols, alkaloids and saponins. When tested on isolated rat stomach fundus, Zo.Cr showed a spasmogenic effect (0.03–5.00 mg mL−1) it relaxed the tissue at concentrations ≥5 mg mL−1. The stimulant effect was resistant to blockade by hexamethonium and methysergide, but sensitive to atropine, indicating activity via muscarinic receptors. In atropinized (0.1 μM) preparations, Zo.Cr (0.3–3.0 mg mL−1) relaxed high K+ (80 mm)-induced contractions, indicating Ca++ antagonism in addition to the muscarinic effect. This possible Ca++ antagonist activity was investigated in Ca++-free conditions, with the inhibitory effect of the extract tested against contractions induced by externally administered Ca++. Zo.Cr (0.1–0.3 mg mL−1), similar to verapamil (0.03–0.10 μm), shifted the contractions induced by externally administered Ca++ to the right, thus suggesting an inhibitory interaction between Zo.Cr and voltage-operated Ca++ channels. Zo.Cr (0.1–3.0 μg mL−1) also potentiated acetylcholine peak responses in stomach fundus, similar to physostigmine, a cholinesterase inhibitor. Zo.Cr, in an in-vitro assay, showed specific inhibition of butyrylcholinesterase (BuChE) rather than acetylcholinesterase enzyme. Different pure compounds of ginger also showed spasmolytic activity in stomach fundus, with 6-gingerol being the most potent. 6-Gingerol also showed a specific anti-BuChE effect. This study shows a unique combination of muscarinic, possible Ca++ antagonist and BuChE inhibitory activities of dried ginger, indicating its benefit in dementia, including Alzheimer's disease.
Publisher: Mary Ann Liebert Inc
Date: 09-2023
Publisher: Elsevier BV
Date: 10-2002
DOI: 10.1016/S0306-9877(02)00260-8
Abstract: Herbs and minerals are the integral parts of traditional systems of medicine in many countries. Kushta is a form of herbo-mineral preparations used in traditional systems of medicine (Unani and Ayurvedic) of Indo-Pak subcontinent. These preparations have long been used and claimed to be the most effective and potent dosage form. However, there are only few scientific studies carried out on these products because of several reasons mainly being the lack of communication among traditional healers, physicians and scientists. The objective of this paper is to fill this gap by translating the old concepts in modern understanding, providing possible explanation and hypotheses. Some recommendations have also been given to provide the path to initiate research in this area of potential therapeutic value and public concern.
Publisher: Informa UK Limited
Date: 11-2022
DOI: 10.1080/14786410512331330567
Abstract: Keeping in view the interesting chemistry and pharmacological importance of harmine series of bases -- the beta-carboline alkaloids, a number of new derivatives of tetrahydroharmine and harmalol have been prepared and characterized through spectral studies. Some of these derivatives showed spasmolytic activity. It was observed that all the N-acyl tetrahydroharmine derivatives are stable, not labile and no ring opening occurs in these compounds, as reported recently.
Publisher: Science Alert
Date: 11-2015
Publisher: Wiley
Date: 02-01-2017
Publisher: Elsevier
Date: 2010
Publisher: Georg Thieme Verlag KG
Date: 12-1993
Publisher: Elsevier BV
Date: 09-1999
Publisher: Elsevier BV
Date: 12-1994
Publisher: Canadian Science Publishing
Date: 09-2007
DOI: 10.1139/Y07-079
Abstract: The aqueous-methanolic crude extract of Andropogon muricatus (Am.Cr) was investigated pharmacologically to determine some of its medicinal uses in cardiovascular and gastrointestinal disorders. A series of in vivo and in vitro studies were conducted to evaluate dose-dependent effects of Am.Cr on mean arterial pressure (MAP), cardiac and vascular contractions, and to further investigate the potential mechanism of action. Intravenous administration of Am.Cr (10–50 mg/kg) caused a fall (18%–56%) in MAP in normotensive rats under anesthesia. When tested in isolated guinea pig atria, Am.Cr (0.03–5.0 mg/mL) exhibited a cardiodepressant effect on the rate and force of spontaneous contractions. In isolated rabbit aorta, Am.Cr caused inhibition of K + (80 mmol/L)-induced contractions at a lower concentration than of phenylephrine. In isolated rabbit jejunum preparations, Am.Cr (0.01–0.10 mg/mL) caused relaxation of spontaneous and high K + (80 mmol/L)-induced contractions, suggesting that the spasmolytic effect is mediated possibly through calcium channel blockade (CCB). The CCB activity was confirmed when pretreatment of the tissue with Am.Cr (0.03–0.1 mg/mL) shifted the Ca 2+ dose–response curves to the right, similar to that caused by verapamil. These data indicate that the blood pressure-lowering and spasmolytic effects of Am.Cr are mediated possibly through a calcium channel blocking activity. Phytochemical screening of Am.Cr revealed the presence of phenols, saponins, tannins, and terpenes, which may be responsible for the observed vasodilator, cardiodepressant, and antispasmodic activities. This study shows potential with respect to its medicinal use in cardiovascular and gut disorders.
Publisher: Wiley
Date: 08-2005
DOI: 10.1002/PTR.1727
Abstract: The crude extract of Carthamus oxycantha (Co.Cr) and its fractions were studied in vitro for their possible spasmogenic and spasmolytic activities. Co.Cr (0.03-10 mg/mL) caused an atropine sensitive spasmogenic effect in guinea-pig ileum. In spontaneously contracting rabbit jejunum preparations, Co.Cr caused a dose-dependent (0.03-3.0 mg/mL) spasmogenic effect, followed by relaxation at the next higher doses of 5.0-10.0 mg/mL. In the presence of atropine, the spasmogenic effect was blocked and the relaxant effect was observed at lower doses (0.1-5.0 mg/mL), shifting the inhibitory dose-response curves to the left. Co.Cr also inhibited K(+) (80 mm)-induced contractions in atropinized preparations at similar doses, suggesting calcium channel blockade (CCB) activity. The CCB effect was further confirmed when pretreatment of the tissue with Co.Cr produced a dose-dependent shift in the Ca(++) dose-response curves to the right, similar to that caused by verapamil. Activity-directed fractionation revealed that the spasmolytic effect was concentrated in organic fractions in the following order of potency: hexane > ethylacetate > chloroform, while the aqueous fraction exhibited spasmogenic and weak spasmolytic effects. These results indicate that Carthamus oxycantha contains a combination of spasmogenic (cholinergic) and spasmolytic (calcium antagonist) constituents.
Publisher: Science Alert
Date: 05-2014
Publisher: BMJ
Date: 02-2022
DOI: 10.1136/BMJOPEN-2021-059160
Abstract: Chronic kidney disease (CKD) and cardiac disease are two significant health conditions that can impact a women’s pregnancy however, little is known about their prevalence and health impact within the population. These pregnancies are associated with significant risks of morbidity and mortality and propose a challenge to clinicians. The aim of this longitudinal cohort study is to prospectively record the incidence, prevalence, aetiology, outcomes and follow-up of maternal CKD and cardiac disease in the obstetric population of South Australia. This study is a state-wide multicentre prospective cohort study in South Australia that will begin recruitment in 2022 and is planned for at least 5 years. Pregnant women with chronic or acquired kidney or cardiac disease will be enrolled across the state’s major public obstetric hospitals. The data collected will focus on the chronic disease aetiology, peripartum interventions, delivery, obstetric and neonatal outcomes, progression of underlying disease and patient-related outcome measures. Women will have data collected each trimester during pregnancy and then at follow-up 6 weeks, 6 months and 12 months post partum. Clear inclusion and exclusion criteria have been developed which importantly includes new diagnosis of chronic disease in pregnancy. Approval was obtained from the local Health Network Human Research Ethics Committee. Summary data will be reviewed and reported in accordance with Strengthening the Reporting of Observational Studies in Epidemiology criteria 6 monthly and results will be published in peer-reviewed journals and presented at conferences. Findings will be presented to relevant local clinicians and hospitals at regular intervals. Consumer versions of research outputs will be developed in conjunction with the consumer reference group.
Publisher: Springer Science and Business Media LLC
Date: 11-07-2022
DOI: 10.1007/S00592-022-01914-Y
Abstract: Gestational diabetes mellitus (GDM) is thought to be associated with cardio-metabolic risk factor development in women and their children during the early postpartum period and early childhood. We hypothesized that these women and their children would exhibit increased abnormal cardio-metabolic risk factors three years after pregnancy. Women from the Screening Tests to Predict Poor Outcomes of Pregnancy study were invited to attend a follow-up with the child from their index pregnancy at 3 years postpartum. Women and children were assessed for anthropometric measures and haemodynamic function. Fasting blood s les were obtained from women to assess lipid and glucose status. A total of 281 woman-child dyads participated in the 3-year follow-up, with 40 women developing GDM during their index pregnancy. Fasting serum insulin was higher in women with GDM in index pregnancy compared to those with an uncomplicated pregnancy. However, this association was mediated by early pregnancy BMI and socioeconomic index (SEI). The rate of metabolic syndrome was higher in the GDM group than the uncomplicated pregnancy group. Maternal GDM was associated with elevated maternal fasting serum triglycerides at 3 years after adjustment for early pregnancy BMI and SEI. Children exposed to GDM in utero had higher waist circumference compared to children born after an uncomplicated pregnancy, but this is mediated the above covariates. Exposure to GDM is associated with elevated serum triglycerides in women at 3 years postpartum but other cardiometabolic outcomes in women and children appear to be mediated by early pregnancy BMI and SEI.
Publisher: Elsevier BV
Date: 09-1998
Abstract: The potential of protopine to inhibit microsomal drug metabolising enzymes (MDM E) and prevent paracetamol- and CCl4-induced hepatotoxicity was studied in rats. Paracetamol at the dose of 640 mg kg-1 produced hepatic damage in rats as manifested by the rise in serum levels of aspartate transaminase (AST) and alanine transaminase (ALT) to 972+/-186 and 624+/-131 IU (mean+/-sem n=10), respectively, compared to respective control values of 101+/-29 and 64+/-18 IU. Pretreatment of rats with protopine (11 mg kg-1, orally twice daily for 2 days) lowered significantly the respective serum AST and ALT levels (P<0.05) to 289+/-52 and 178+/-43 IU. The hepatotoxic dose of CCl4 (1.5 ml kg-1 orally) raised serum AST and ALT levels to 543+/-89 and 387+/-69 IU (mean+/-sem n=10), respectively, compared to respective control values of 98+/-28 and 56+/-17 IU. The same dose of protopine (11 mg kg-1) was able to prevent significantly (P<0.05), the CCl4-induced rise in serum enzymes and the estimated values of AST and ALT were 168+/-36 and 93+/-28 IU, respectively. Protopine caused prolongation (P<0.05) in pentobarbital (55 mg kg-1)-induced sleep as well as potentiated strychnine-induced toxicity in rats, suggestive of an inhibitory effect on MDME. These results indicate that protopine exhibits anti-hepatotoxic action which may be mediated through inhibition of MDME.
Publisher: Wiley
Date: 05-2013
DOI: 10.1111/IMJ.12035
Publisher: Springer Science and Business Media LLC
Date: 28-03-2013
Publisher: Public Library of Science (PLoS)
Date: 23-07-2021
DOI: 10.1371/JOURNAL.PONE.0255070
Abstract: Maternal and infant morbidities associated with pregnant women with cardiac conditions are a global issue contingent upon appropriate care. This study aimed to describe the clinical variables and their association with the adherence scores to perinatal guidelines for pregnant women with cardiac conditions. The clinical variables included cardiac, perinatal, and neonatal outcomes and complications. Using a retrospective cross-sectional medical record audit, data were abstracted and categorised as cardiac, obstetric, and neonatal predictors. Linear regression modelling was used to find the mean difference (MD) in adherence scores for each predictor, including a 95% confidence interval (CI) and a significance value for all the three categories’ clinical outcomes. This maternal cohort’s (n = 261) cardiac complications were primarily arrhythmias requiring treatment (29.9%), particularly SVT (28%), a new diagnosis of valvular heart disease and congenital heart disease (24%) and decompensated heart failure (HF) (16%). Women with HF had associated increased adherence scores (MD = 3.546, 95% CI: 1.689, 5.403) compared to those without HF. Elective LSCS mode of delivery was associated with a higher adherence score (MD = 5.197, 95% CI: 3.584, 6.811) than non-elective LSCS subgroups. Babies admitted to intensive /special care had greater adherence to the guidelines (MD = 3.581, 95% CI: 1.822, 5.340) than those not requiring the same care. Some pregnancy associated complications and morbidities were associated with higher adherence scores, reflecting that a diagnosis, identification of morbidities or risk factors, initiation of appropriate multidisciplinary involvement and adherence to guidelines were associated. Conversely, potentially avoidable major complications such as sepsis were associated with a low adherence score. ACTRN12617000417381 .
Publisher: Wiley
Date: 18-10-2011
DOI: 10.1002/PTR.3634
Abstract: Urginea indica Kunth. (Family Liliaceae) was studied for its gastrointestinal stimulant effect to rationalize the traditional medicinal uses as a digestive aid, stomachic and laxative. The crude aqueous-methanol extract of Urginea indica bulb (Ui.Cr) was tested on mice and isolated gut preparations. Ui.Cr, which was tested positive for alkaloids, tannins and coumarins, increased faecal output and accelerated charcoal meal transit in mice (6-12 mg/kg, p.o.), similar to that caused by carbachol (10 mg/kg). Ui.Cr (0.01-1 mg/mL) caused a spasmogenic effect in guinea-pig ileum that was reproduced in rabbit jejunum (0.01-0.3 mg/mL) followed by relaxation at a higher concentration. Like carbachol, the stimulant effect of Ui.Cr was blocked by atropine, suggesting the activation of muscarinic receptors mediating the prokinetic effect. Ui.Cr (0.01-5.0 mg/mL) also inhibited K(+) (80 mm)-induced contraction in rabbit jejunum and shifted the Ca(2+) concentration-response curves to the right, similar to verapamil, a standard calcium channel blocker. These data, indicating the presence of a gastrointestinal stimulant effect in Urginea indica possibly mediated through a cholinergic mechanism, provide a rationale for the use of Urginea indica in indigestion and constipation. The presence of a calcium antagonist effect in the plant may help to alleviate untoward effects of the plant that may result from an excessive increase in gut motility.
Publisher: Wiley
Date: 09-10-2008
DOI: 10.1002/PTR.2544
Abstract: This study describes the activity-guided isolation and purification of a novel antimicrobial protein from the seed of Croton tiglium Linn. Purification was carried out by (NH(4))(2)SO(4) precipitation, gel filtration and DEAE-cellulose ion-exchange chromatography. Antifungal and antibacterial activities were determined after each purification step. SDS-polyacrylamide gel electrophoresis revealed that the purified protein was a monomer with molecular mass of 50 kDa. This is a first report on purification of a protein from Croton tiglium, which possesses a strong and broad spectrum antimicrobial activity.
Publisher: Wiley
Date: 21-05-2013
DOI: 10.1002/PTR.4721
Abstract: The current study was undertaken to explore the antipyretic and anticonvulsant profile of the Polygonatum verticillatum in established pharmacological paradigms. The crude methanol extract of rhizomes (PR) and aerial parts (PA) of the plant were tested in Brewer's-yeast-induced pyrexia and pentylenetetrazole-induced convulsion test. PR and PA both evoked prominent antipyretic activity (p < 0.01) in a dose-dependent manner during all assessment times at the dose of 50, 100, and 200 mg/kg intraperitoneally. The protection elicited by PR (82.20%) at 200 mg/kg was comparable with aspirin (88.48%) as a standard drug at 100 mg/kg. However, PA was less potent, and maximum protection was 64% at 200 mg/kg. Both PR and PA were devoid of any anticonvulsant activity. Our results demonstrated prominent evidence of antipyretic activity of P. verticillatum that is consistent with the folk uses of the plant. In addition from a bio ersity point of view, PA of the plant can also be used as an alternate of PR.
Publisher: Wiley
Date: 12-2008
DOI: 10.1002/PTR.2550
Abstract: Commercially available Aztec marigold (Tagetes erecta) flower extract (Af.Cr) was evaluated for the in vitro antioxidant activity and in vivo analgesic effect on acetic-acid-induced abdominal writhing. The results revealed the presence of pronounced antioxidant potential in Aztec marigold flowers and a dose-dependent (100 and 300 mg/kg) analgesic effect. The antioxidant and analgesic activities obtained seem to be in good accordance with the medicinal uses of Aztec marigold as an anti-inflammatory and analgesic.
Publisher: Elsevier BV
Date: 06-2022
Publisher: Springer Science and Business Media LLC
Date: 15-09-2021
Publisher: Bentham Science Publishers Ltd.
Date: 31-01-2018
Publisher: Oxford University Press (OUP)
Date: 05-05-2005
Abstract: To estimate the proportion of pharmacies meeting licensing requirements and to identify factors associated with these pharmacies in urban Rawalpindi, Pakistan. Cross-sectional questionnaire survey conducted during July-September 2001, of 311 pharmacies selected from a drug company list of 506. Free-standing licensed and unlicensed pharmacies in urban Rawalpindi. A pharmacist or (if unavailable) the most experienced drug seller. The proportion of pharmacies meeting licensing requirements was 19.3% [95% C.I (confidence interval): 15.1, 24.2], with few qualified persons (22%). Only 10% had a temperature-monitoring device and 4% an alternative power supply for refrigerators (present in 76% of pharmacies). Associated with pharmacies meeting licensing requirements was the knowledge of not giving co-trimoxazole, a prescription drug, without prescription [OR (odds ratio) = 2.0 95% CI: 1.1, 3.6], knowledge of the temperature range for vaccines (OR = 2.6 95% CI: 1.4, 4.8), availability of vaccines (OR = 2.8 95% CI: 2.8, 18.4), and alternative power supply for the refrigerator (OR = 6.0 95% CI: 1.5, 23.7). The practice of selling drugs without prescription was not found to have a significant association (OR = 1.1 95% CI: 0.5, 2.3) however, it did show a trend indicating discrepancy between knowledge and practice. Most drug sellers had fragmentary knowledge regarding drug dispensing and storage, and improper dispensing practices. There is a need to enforce existing legislation with training programmes directed towards drug sellers and to involve the pharmaceutical industry, which plays an important role in influencing pharmacy knowledge and practices.
Publisher: Elsevier BV
Date: 08-2005
DOI: 10.1016/J.JEP.2005.06.001
Abstract: The use of plants, plant extracts or plant-derived pure chemicals to treat disease is a therapeutic modality, which has stood the test of time. Indeed today many pharmacological classes of drugs include a natural product prototype. Aspirin, atropine, ephedrine, digoxin, morphine, quinine, reserpine and tubocurarine are a few ex les of drugs, which were originally discovered through the study of traditional cures and folk knowledge of indigenous people. There is a revival of interest in herbal products (botanicals) at a global level and the conventional medicine is now beginning to accept the use of botanicals once they are scientifically validated. Ispaghula, Garlic, Ginseng, Ginger, Ginkgo, St. John's Wort, and Saw palmetto are a few ex les of botanicals which are gaining popularity amongst modern physicians and this trend is likely to continue partly due to high cost involved in the development of patentable chemical drugs. There is growing evidence to show that medicinal plants contain synergistic and/or side-effects neutralizing combinations. Ethnopharmacology has already played important role in the development of conventional medicine and is likely to play more significant role in the years to come. A team work amongst ethnobotanists, ethnopharmacologists, physicians and phytochemists is essential for the fruitful outcome on medicinal plants research. While the ethnopharmacologists have a greater role to play in the rationalization of combination of activities, the phytochemist's role will slightly shift towards standardization of botanicals.
Publisher: Elsevier BV
Date: 08-2005
DOI: 10.1016/J.BBRC.2005.06.086
Abstract: The withanolides 1-3 and 4-5 isolated from Ajuga bracteosa and Withania somnifera, respectively, inhibited acetylcholinesterase (AChE, EC 3.1.1.7) and butyrylcholinesterase (BChE, EC 3.1.1.8) enzymes in a concentration-dependent fashion with IC50 values ranging between 20.5 and 49,2 microm and 29.0 and 85.2 microm for AChE and BChE, respectively. Lineweaver-Burk as well as Dixon plots and their secondary replots indicated that compounds 1, 3, and 5 are the linear mixed-type inhibitors of AChE, while 2 and 4 are non-competitive inhibitors of AChE with K(i) values ranging between 20.0 and 45.0 microm. All compounds were found to be non-competitive inhibitors of BChE with K(i) values ranging between 27.7 and 90.6 microm. Molecular docking study revealed that all the ligands are completely buried inside the aromatic gorge of AChE, while compounds 1, 3, and 5 extend up to the catalytic triad. A comparison of the docking results showed that all ligands generally adopt the same binding mode and lie parallel to the surface of the gorge. The superposition of the docked structures demonstrated that the non-flexible skeleton of the ligands always penetrates the aromatic gorge through the six-membered ring A, allowing their simultaneous interaction with more than one subsite of the active center. The affinity of ligands with AChE was found to be the cumulative effects of number of hydrophobic contacts and hydrogen bonding. Furthermore, all compounds also displayed dose-dependent (0.005-1.0 mg/mL) spasmolytic and Ca2+ antagonistic potentials in isolated rabbit jejunum preparations, compound 4 being the most active with an ED50 value of 0.09 +/- 0.001 mg/mL and 0.22 +/- 0.01 microg/mL on spontaneous and K+ -induced contractions, respectively. The cholinesterase inhibitory potential along with calcium antagonistic ability and safe profile in human neutrophil viability assay could make compounds 1-5 possible drug candidates for further study to treat Alzheimer's disease and associated problems.
Publisher: Elsevier BV
Date: 09-1996
DOI: 10.1016/0306-3623(95)02140-X
Abstract: 1. The hepatoprotective activity of an aqueous-methanolic extract of Fumaria parviflora was investigated against paracetamol- and CCI4-induced hepatic damage. 2. Paracetamol (1 g/kg orally) produced 100% mortality in mice pretreatment of animals with the plant extract (500 mg/kg orally) reduced the death rate to 50%. 3. Pretreatment of rats with plant extract (500 mg/kg, orally twice daily for 2 days) prevented (P 0.05) the CCI4-induced rise in serum enzyme levels. 4. Posttreatment with 3 successive doses of the extract (500 mg/kg, 6 hourly) also restricted the paracetamol-induced hepatic damage. 5. The plant extract (500 mg/kg orally) caused significant prolongation in pentobarbital (75 mg/ kg)-induced sleep as well as increased strychnine-induced lethality in mice (P < 0.05), suggestive of an inhibitory effect on microsomal drug metabolizing enzymes (MDME). 6. It is conceivable therefore, that Fumaria parviflora extract exhibits a selective protective effect against paracetamol-induced hepatotoxicity, probably mediated through MDME inhibition.
Publisher: Elsevier BV
Date: 03-1995
DOI: 10.1016/0031-9422(94)00729-D
Abstract: Six new and three synthetically known glycosides have been isolated from the leaves of Moringa oleifera, employing a bioassay-directed isolation method on the ethanolic extract. Most of these compounds, bearing thiocarbamate, carbamate or nitrile groups, are fully acetylated glycosides, which are very rare in nature. Elucidation of the structures was made using chemical and spectroscopic methods, including 2D NMR techniques. Thiocarbamates showed hypotensive activity.
Publisher: Elsevier BV
Date: 04-2015
DOI: 10.1016/J.CTIM.2015.01.008
Abstract: To compare the clinical efficacy of Black seeds and Turmeric alone and its co-administration in lower doses among patients with metabolic syndrome (MetS). Double-blind-randomized-controlled trial. Hijrat colony, Karachi, Pakistan. Apparently healthy males (n=250), who screened positive for MetS, were randomized to either Black seeds (1.5g/day), Turmeric (2.4g/day), its combination (900mg Black seeds and 1.5g Turmeric/day) or placebo for 8 weeks. body-mass-index (BMI), body-fat-percent (BF%), waist-circumference (WC), hip-circumference (HC), blood pressure (BP), lipid-profile (cholesterol, HDL-cholesterol, LDL-cholesterol and TG), fasting blood glucose (FBG) and c-reactive protein (CRP). At 4 weeks, compared to baseline, Black seed and Turmeric alone showed improvement in BMI, WC and BF%. Combination improved all parameters except HDL-cholesterol with lower FBG and LDL-cholesterol as compared to placebo. At 8 weeks, compared to placebo, Black seeds reduced lipids and FBG, while Turmeric reduced LDL-cholesterol and CRP. Interestingly, combination group with 60% dose of the in idual herbs showed an improvement in all parameters from baseline. When compared to placebo, it reduced BF%, FBG, cholesterol, TG, LDL-cholesterol, CRP and raised HDL-cholesterol. Turmeric and Black seeds showed improvement in all parameters of metabolic syndrome, when co-administered at 60% of doses of in idual herbs with enhanced efficacy and negligible adverse-effects. The combination of Black seeds and Turmeric can therefore, be recommended with lifestyle modification as a starting point for patients with MetS to halt its future complications and progression.
Publisher: Elsevier BV
Date: 11-2000
DOI: 10.1016/S0378-8741(00)00288-9
Abstract: The aqueous crude extract (PPL.Cr) of peach leaves (Prunus persica) was studied for the possible presence of gut stimulatory constituent(s) to rationalize the folkloric use of the plant in constipation. PPL.Cr at the dose of 1-10 mg/ml caused a moderate degree of spasmogenic effect in isolated guinea-pig ileum. Pretreatment of the tissue with atropine (1 M) completely abolished the contractile effect of the plant extract similar to that of acetylcholine which is suggestive of a cholinergic mechanism. In isolated rabbit jejunum preparations, PPL.Cr produced a week spasmogenic effect followed by relaxation of the spontaneous contractions at higher doses. Bioassay-directed fractionation revealed that the spasmogenic activity was separated in the aqueous fraction, while the spasmolytic activity was concentrated in the ethyl acetate fraction. When tested against K(+)-induced contraction, both PPL.Cr and its ethyl acetate fraction (PPL.EtAc) caused a dose-dependent inhibition, suggesting calcium channel blockade (CCB). The presence of CCB in peach leaves was confirmed when pretreatment of the tissue with PPL.EtAc caused a dose-dependent rightward shift in the Ca(2+) dose-response curves, similar to that produced by verapamil. These data indicate that the plant contains spasmogenic (cholinomimetic) and spasmolytic (calcium antagonist) constituents, which are concentrated in the aqueous and ethyl acetate fractions, respectively. Furthermore, the laxative effect of the plant reported in the traditional system of medicine may be partially due to the cholinergic action, which was dominant over the spasmolytic component.
Publisher: Wiley
Date: 18-10-2011
DOI: 10.1002/PTR.3642
Abstract: This study was aimed to provide the pharmacological basis for the medicinal use of Lepidium sativum in diarrhea using in vivo and in vitro assays. The seed extract of Lepidium sativum (Ls.Cr) at 100 and 300 mg/kg inhibited castor oil-induced diarrhea in rats. In isolated rat ileum, Ls.Cr (0.01-5 mg/mL) reversed carbachol (CCh, 1 µM) and K(+) (80 mM)-induced contractions with higher potency against CCh, similar to dicyclomine. Preincubation of rat ileum with a lower concentration of Ls.Cr (0.03 mg/mL) caused a rightward parallel shift in the concentration-response curves (CRCs) of CCh without suppression of the maximum response, while at the next higher concentration (0.1 mg/mL), it produced a non-parallel rightward shift with suppression of the maximum response, similar to that of dicyclomine. Ls.Cr shifted the CRCs of Ca(++) to the right with suppression of the maximum response, similar to verapamil. These data suggest that Lepidium sativum seed extract possesses antidiarrheal and spasmolytic activities mediated possibly through dual blockade of muscarinic receptors and Ca(++) channels, though additional mechanism(s) cannot be ruled out and this study explains its medicinal use in diarrhea and abdominal cr s.
Publisher: Elsevier BV
Date: 05-1998
Publisher: Wiley
Date: 31-10-2006
DOI: 10.1111/J.1742-7843.2006.PTO_507.X
Abstract: Rooibos tea has been widely used for abdominal spasm and diarrhoea. The aim of the present study was to explore the possible mechanism for its use in such ailments. Its aqueous extract (RT) at 0.3-10 mg/ml produced relaxation of spontaneous and low K(+) (25 mM)-induced contractions of rabbit jejunum, with weak effect on high K(+) (80 mM)-induced contractions. In the presence of glibenclamide, relaxation of low K(+)-induced contractions was prevented. Cromakalim inhibited contractions induced by low K(+), but not high K(+), while verapamil did not differentiate in its inhibitory effect on contractions produced by the two concentrations of K(+). RT also exhibited antidiarrhoeal and antisecretory activities in mice. The spasmolytic effect was concentrated in organic fractions. Its constituents, chrysoeriol, orientin and vitexin showed a similar pattern of spasmolytic effects to the extract, while rutin was more like verapamil. So Rooibos tea possesses a combination of dominant K(ATP) channel activation and weak Ca(++) antagonist mechanisms and hence justifies its use in hyperactive gastrointestinal disorders.
Publisher: Informa UK Limited
Date: 2005
DOI: 10.1080/09637480500539420
Abstract: Olive (Olea europea) is used in traditional medicine as a remedy for hypertension. The aqueous-methanolic crude extract of O. europea fruit (OeF.Cr) was studied in anaesthetized rats and its possible mechanism was elucidated using isolated cardiovascular preparations. Intravenous administration of OeF.Cr produced a dose-dependent (30-100 mg/kg) fall in arterial blood pressure in normotensive anaesthetized rats. This effect remained unaltered in atropinized animals. In the in vitro studies OeF.Cr (0.1-3.0 mg/ml) inhibited spontaneously beating guinea-pig atria. Moreover, it relaxed K+ and/or phenylephrine-induced contractions of rabbit aortic preparations over a dose range of 0.1-3.0 mg/ml, suggesting calcium channel blockade (CCB). The CCB effect was confirmed when pretreatment of the vascular preparations with OeF.Cr produced a dose-dependent rightward shift of the Ca2+ dose-response curves, similar to verapamil. These results suggest that the blood pressure lowering effect of olive is mediated through CCB, justifying its use in hypertension.
Publisher: Wiley
Date: 29-10-2013
DOI: 10.1002/PTR.4860
Abstract: Polygonatum verticillatum is commonly used for the treatment of asthma and inflammation. The current study was aimed to scrutinize the pharmacological profile of methanolic extract of the aerial parts (PA). Isolated tracheal preparations were used for the evaluation of bronchodilatory activity, whilst the in vivo carrageenan-induced paw oedema test and an in vitro lipoxygenase (LOX) inhibitory assay were used for the assessment of the anti-inflammatory profile of PA. When tested against carbachol and K⁺ (80 mM)-induced contractions, PA caused complete inhibition of isolated rabbit tracheal preparations in a dose-dependent mode, similar to verapamil. While elucidating possible mechanism, PA shifted the Ca²⁺ concentration-response curves to the right, analogous to that produced by verapamil, confirming a Ca²⁺ channel blocker-like activity. PA provoked profound reduction in paw oedema with a maximum protection of 60.87% at 200 mg/kg i.p. in a dose-dependent manner which was augmented by its prominent LOX inhibitory activity (IC₅₀ : 125 µg/mL). These findings authenticated its therapeutic potential in the treatment of asthmatic and inflammatory conditions.
Publisher: Ovid Technologies (Wolters Kluwer Health)
Date: 07-2009
Publisher: Springer Science and Business Media LLC
Date: 11-09-2009
DOI: 10.1038/HR.2009.148
Abstract: The objective of this study was to investigate the possible mode(s) of action for the medicinal use of Orchis mascula (OM) (family Orchidaceae) in hypertension and dyslipidemia. In spontaneously hypertensive rats (SHRs), OM significantly (P<0.05) reduced systolic blood pressure to 174.2+/-9.63 vs. 203.4+/-7.13 mm Hg (mean+/-s.e.m. n=7-10) and improved endothelial dysfunction by increasing acetylcholine-induced relaxation. In normotensive anesthetized rats, the crude extract of OM (Om.Cr) at 10 and 30 mg kg(-1) caused a dose-dependent attenuation of mean arterial pressure. OM also decreased serum triglycerides to 29.28+/-6.99 vs. 93.84+/-5.7 mg per 100 ml (P<0.001), low-density lipoprotein-cholesterol to 5.99+/-1.27 vs. 21.9+/-3.5 mg per 100 ml (P<0.05) and atherogenic index to 0.096+/-0.017 vs. 0.36+/-0.08 mg per 100 ml (P<0.05). OM significantly reduced lipid levels in tyloxapol and high fat diet-induced hyperlipidemia. In a second model, OM also reduced gain in body weight with a reduction in daily diet consumption. In isolated rabbit aorta, Om.Cr caused concentration-dependent relaxation of both phenylephrine and high K(+) (80 mM)-induced contractions and a rightward shift of the calcium concentration-response curves similar to the effect seen with verapamil. In conclusion, OM shows antihypertensive and endothelial-modulating effects mediated through multiple pathways that include direct vasodilation by calcium channel blockade and reduction of plasma lipids by inhibition of biosynthesis, absorption and secretion. This study rationalizes the medicinal use of OM in hypertension and dyslipidemia. However, further studies are required to identify the active constituents of this plant.
Publisher: The Japan Institute of Heterocyclic Chemistry
Date: 1995
DOI: 10.3987/COM-94-6862
Publisher: Hindawi Limited
Date: 13-09-2021
DOI: 10.1155/2021/5583372
Abstract: Background. Grewia asiatica Linn, or phalsa, is a commonly consumed fruit in Pakistan. The fruit is employed in the traditional medicine practice of Pakistan as a smooth muscle relaxant in different gastrointestinal (GI) and cardiovascular diseases. In this investigation, we show the antispasmodic and vasorelaxant actions of Grewia asiatica fruit extract. Methods. A 70% methanolic crude extract of the plant material was prepared (Ga.Cr). Different isolated GI tissue preparations and endothelium-intact aortas from rats were utilized to observe the pharmacological actions of the extract. Results. Ga.Cr, in increasing concentrations, inhibited the spontaneously contracting rabbit jejunum. In an effort to determine the mechanism of this relaxant action, contractions were induced in jejunum and ileum tissues with K+ (80 mM). Ga.Cr was able to only partially inhibit these induced contractions indicating that the mechanism might not be completely through a blockade of Ca2+ channels (CCB). When tested on low K+-(25 mM) sustained contractions, Ga.Cr cumulatively suppressed these contractions (0.1–10 mg/ml), indicating an opening of K+ channels (KCO) as the mechanism. Cromakalim, a standard KCO, was also more specific in blocking low K+-induced contractions. For the effect in aorta tissues, Ga.Cr suppressed the agonist-induced contractions from 0.3 mg/ml to 10 mg/ml. Upon challenge with L-NAME, a nitric oxide (NO) blocker, the extract response curve shifted right, indicating vasodilation was mediated via endothelial NO. Conclusion. This study shows that GI antispasmodic and vasodilator activities of Ga.Cr may be mediated via a KCO mechanism in the GI tract and through the release of NO from vascular endothelium.
Publisher: Springer Science and Business Media LLC
Date: 2006
DOI: 10.1007/BF02977465
Publisher: Georg Thieme Verlag KG
Date: 04-1998
Abstract: Hypotensive activity of the ethanolic and aqueous extracts of Moringa oleifera whole pods and their parts, namely, coat, pulp, and seed was investigated. The activity of the ethanolic extract of both the pods and the seeds was equivalent at the dose of 30 mg/kg. The ethyl acetate phase of the ethanolic extract of pods was found to be the most potent fraction at the same dose. Its bioassay-directed fractionation led to the isolation of thiocarbamate and isothiocyanate glycosides which were also the hypotensive principles of the pods as observed in case of Moringa leaves. Two new compounds, O-[2'-hydroxy-3'-(2"-heptenyloxy)]-propyl undecanoate (1) and O-ethyl-4-[(alpha-L-rhamnosyloxy)-benzyl] carbamate (2) along with the known substances methyl p-hydroxybenzoate (3) and beta-sitosterol have also been isolated in the present studies. The latter two compounds and p-hydroxybenzaldehyde showed promising hypotensive activity. Structures of all these compounds have been deduced by spectroscopy and chemical reactions.
Publisher: Springer Science and Business Media LLC
Date: 15-04-2010
DOI: 10.1007/S10787-010-0038-4
Abstract: The current study was aimed to evaluate Acacia modesta for analgesic, anti-inflammatory, and anti-platelet activities. The analgesic and anti-inflammatory effects were assessed in rodents using acetic acid and formalin-induced nociception, hot plate and carrageenan-induced rat paw oedema tests. The intraperitoneal (i.p.) administration of the methanolic extract (50 and 100 mg/kg) produced significant inhibition (P\\0.01) of the acetic acid-induced writhing in mice and suppressed formalin-induced licking response of animals in both phases of the test. In the hot plate assay the plant extract (100 mg/kg) increased pain threshold of mice. Naloxone (5 mg/kg i.p.) partially reversed the analgesic effect of the extract in formalin and hot plate tests.A. modesta (100 and 200 mg/kg i.p.) exhibited sedative effect in barbiturate-induced hypnosis test similar to that produced by diazepam (10 mg/kg i.p.). The plant extract(50-200 mg/kg i.p.) produced marked anti-inflammatory effect in carrageenan-induced rat paw oedema assay comparable to diclofenac and produced a dose-dependent(0.5-2.5 mg/mL) inhibitory effect against arachidonic acid induced platelet aggregation. These data suggest that A. modesta possesses peripheral analgesic and antiinflammatory properties, with analgesic effects partially associated with the opioid system.
Publisher: Informa UK Limited
Date: 10-2006
DOI: 10.1179/OEH.2006.12.4.362
Abstract: Children in Central Asia and the Middle East bear disproportionate environmental threats to health, of which the most widespread and serious result from poverty, malnutrition, lack of access to safe drinking water and food, and exposures to toxic chemicals. Their psychological health is threatened in several parts of this region by internal wars and strife. Many, or even most, children are regularly exposed to environmental tobacco smoke. In many of these countries, children constitute very high percentages of the population. Because children constitute the future, it is critical that these threats to their health be addressed and reduced to the greatest extent possible through both provision of safe and adequate drinking water and nutrition and reduction of exposures to environmental contaminants.
Publisher: Elsevier BV
Date: 04-2014
DOI: 10.1016/J.JEP.2014.02.024
Abstract: Carissa carandas Linn. commonly known as "Karaunda" (Apocynaceae) is a popular medicinal herb widely distributed in different parts of Pakistan. In addition to other medicinal uses, Carissa carandas is popular in indigenous system of medicine for its medicinal use in gut motility disorders like, constipation and diarrhea. This study was planned to provide pharmacological basis to the medicinal use of Carissa carandas in constipation and diarrhea. The crude extract of the leaves of Carissa carandas (Cc.Cr) was prepared in methanol and its fractionation was carried out with ethylacetate, petroleum ether and n-butanol. In-vivo studies were conducted on mice, while isolated rabbit jejunum and guinea-pig ileum preparations were used for the in-vitro experiments. The spasmogenic and spasmolytic responses of gut tissues were recorded using isotonic transducers coupled with PowerLab data acquisition system. The HPLC fingerprints of Cc.Cr, its petroleum (Cc.Pef), ethylacetate (Cc.Eaf) and n-butanol (Cc.Baf) fractions showed the presence of oleanolic acid, ursolic acid, stigmasterol and β-sitosterol. Oral administration of Cc.Cr to mice increased fecal output at lower doses (30 and 50 mg/kg), while it showed protection against castor oil-induced diarrhea at higher doses (300 and 600 mg/kg). In isolated guinea-pig ileum and rabbit jejunum, Cc.Cr and Cc.Baf exhibited stimulatory effect at 0.003-3 mg/ml, which was partially sensitive to atropine or pyrillamine or partially/fully sensitive to atropine+pyrillamine, followed by relaxation at higher tested concentrations, being more potent in rabbit tissues. The ethylacetate fraction (0.1-5 mg/ml) exhibited fully atropine-sensitive contractions in both guinea-pig and rabbit tissues, being more potent in guinea-pig while more efficacious in rabbit tissues. However, the petroleum fraction (0.003-1.0 mg/ml) showed only spasmolytic activity in spontaneously contracting rabbit tissues, similar to nifedipine. In guinea-tissue, Cc.Pef did not cause any stimulant effect. When studied against high K(+) (80 mM)-induced contraction, the crude extract and its fractions caused a dose-dependent inhibition, with the following order of potency: Cc.Pef>Cc.Eaf>Cc.Cr≥Cc.Baf, similar to nifedipine indicating Ca(++) channel antagonist like activity, which was further confirmed when the plant extract displaced Ca(++) curves to the right with suppression of maximum effect similar to that of nifedipine. This study demonstrates that the crude extract of Carissa carandas possesses a gut-stimulatory effect mediated primarily through the activation of muscarinic and histaminergic receptors while its spasmolytic effect was mediated possibly through Ca(++) antagonist pathway. Thus, this study provides a clear evidence for the dual effectiveness of Carissa carandas in constipation and diarrhea, thus validating its medicinal use.
Publisher: Springer Science and Business Media LLC
Date: 12-2013
Publisher: Wiley
Date: 04-12-2008
DOI: 10.1002/PTR.2322
Abstract: The present study was undertaken in normotensive anaesthetized male rats that received a continuous perfusion of a chrysin glucoside isolated from the flowers and leaves of Calycotome villosa subsp intermedia at a dose of 2.5 mg/kg, or furosemide (control diuretic) at a dose of 0.5 mg/kg. Compared with the control rats receiving NaCl (0.9%), the urine flow, glomerular filtration and electrolyte excretion (Na+, K+) increased significantly in rats treated with chrysin glucoside (p < 0.001). A similar effect was observed in the rats perfused with furosemide. Intravenous injections of bolus doses (1-3 mg/kg) of the chrysin glucoside to anaesthetized rats elicited an immediate and dose-dependent decrease in mean arterial blood pressure (MABP). Pretreatment of the rats with the nitric oxide synthase inhibitor, l-NOArg (10 mg/kg), reduced partially, but significantly (p < 0.01), the maximal decrease in MABP elicited by chrysin glucoside. In the rat isolated aorta preparation, chrysin glucoside (10-100 microm) inhibited in a concentration-dependent manner the noradrenaline (1 microm) induced contractions (IC(50) = 52 microm). This relaxant activity of chrysin glucoside was significantly reduced by incubation of the endothelium-intact rings with l-NOArg (100 microm), (80 +/- 4.7% vs 48 +/- 5.06% in the absence of L-NOArg). In conclusion, these results demonstrate a diuretic and hypotensive action of a chrysin glucoside from Calycotome villosa in anaesthetized rats and indicating an action on renal function, and an active vascular relaxation mediated partially through nitric oxide release.
Publisher: Elsevier BV
Date: 2011
DOI: 10.1016/J.JEP.2010.11.023
Abstract: This study was aimed at providing the possible mechanisms for the medicinal use of Phyllanthus emblica in diarrhea. The in vivo studies were conducted in mice, while isolated rabbit jejunum and guinea-pig ileum were used for the in vitro experiments. The crude extract of Phyllanthus emblica (Pe.Cr), which tested positive for alkaloids, tannins, terpenes, flavonoids, sterols and coumarins, caused inhibition of castor oil-induced diarrhea and intestinal fluid accumulation in mice at 500-700 mg/kg. In isolated rabbit jejunum, Pe.Cr relaxed carbachol (CCh) and K(+) (80 mM)-induced contractions, in a pattern similar to that of dicyclomine. The preincubation of guinea pig-ileum with Pe.Cr (0.3 mg/mL), caused a rightward parallel shift in the concentration-response curves (CRCs) of acetylcholine without suppression of the maximum response. While at the next higher concentration (1 mg/mL), it produced a non-parallel rightward shift with suppression of the maximum response, similar to that of dicyclomine, suggesting anticholinergic and Ca(2+) channel blocking (CCB)-like antispasmodic effect. The CCB-like activity was further confirmed when pretreatment of the tissue with Pe.Cr, shifted the CRCs of Ca(2+) to the right with suppression of the maximum response, similar to nifedipine or dicyclomine. The activity-directed fractions of Pe.Cr showed a combination of Ca(2+) antagonist and anticholinergic like components in all fractions but with varying potency. These results indicate that the Phyllanthus emblica fruit extract possesses antidiarrheal and spasmolytic activities, mediated possibly through dual blockade of muscarinic receptors and Ca(2+) channels, thus explaining its medicinal use in diarrhea.
Publisher: Elsevier BV
Date: 1997
DOI: 10.1016/S0024-3205(96)00691-1
Abstract: The ability of the alkaloid, ebeinone, isolated from Fritillaria imperialis, to act at muscarinic M2 and M3 acetylcholine receptors was investigated. In functional studies with guinea-pig left atrium, ebeinone was found to be ca. 10-fold more active as an antagonist of responses to carbachol (CCh) than in either guinea-pig ileum or trachea. Estimates of dissociation constants (KB values) in the three tissues were 77.3, 931.1 and 547.0 nM, respectively. Inhibition binding studies in rat atria with the non-selective antagonist [3H]N-methylscopolamine ([3H]NMS) showed ebeinone to have a KI value of 80.9 nM. Comparison of ebeinone with pancuronium, another steroid-like compound with a similar KB value at the muscarinic M2 receptor, found both compounds able to retard the dissociation rate of [3H]NMS in atria, indicating an allosteric mode of interaction at the M2 receptor. It is concluded that ebeinone exhibited a higher affinity for muscarinic M2 receptors than for M3 receptors in the guinea-pig and that it interacted allosterically at rat atrial M2 receptors.
Publisher: Wiley
Date: 02-1993
Publisher: Elsevier BV
Date: 03-2008
DOI: 10.1016/J.JEP.2008.01.006
Abstract: The present investigation was carried out to provide the pharmacological basis for the medicinal use of Terminalia bellerica in hyperactive gastrointestinal and respiratory disorders. Crude extract of Terminalia bellerica fruit (Tb.Cr) was studied in in vitro and in vivo. Tb.Cr caused relaxation of spontaneous contractions in isolated rabbit jejunum at 0.1-3.0mg/mL. Tb.Cr inhibited the carbachol (CCh, 1microM) and K(+) (80mM)-induced contractions in a pattern similar to that of dicyclomine, but different from nifedipine and atropine. Tb.Cr shifted the Ca(++) concentration-response curves to right, like nifedipine and dicyclomine. In guinea-pig ileum, Tb.Cr produced rightward parallel shift of acetylcholine-curves, followed by non-parallel shift at higher concentration with the suppression of maximum response, similar to dicyclomine, but different from nifedipine and atropine. Tb.Cr exhibited protective effect against castor oil-induced diarrhea and carbachol-mediated bronchoconstriction in rodents. In guinea-pig trachea, Tb.Cr relaxed the CCh-induced contractions, shifted CCh-curves to right and inhibited the contractions of K(+). Anticholinergic effect was distributed both in organic and aqueous fractions, while CCB was present in the aqueous fraction. These results indicate that Terminalia bellerica fruit possess a combination of anticholinergic and Ca(++) antagonist effects, which explain its folkloric use in the colic, diarrhea and asthma.
Publisher: Ovid Technologies (Wolters Kluwer Health)
Date: 11-2008
Publisher: Wiley
Date: 27-07-2007
DOI: 10.1002/PTR.2216
Abstract: During the course of screening of medicinal plants of Pakistan for the isolation and structure elucidation of bioactive natural products, it was found that the methanol extract of the Rhododendron collettianum showed analgesic and spasmolytic activities. The methanol extract was then extracted with chloroform. Nine pentacyclic triterpenes were isolated from the chloroform extract and their structures were elucidated as erythrodiol (1), betulinic acid (2), maslinic acid (3), 2alpha,3alpha,23-trihydroxyolean-12-en-28-oic acid (4), bayogenin (5), arjunilic acid (6), methyl arjunolate (7), arjungenin (8) and 3beta, 23, 24-trihydroxyolean-12-en-28-oic acid (9). Among the triterpenes (1-9) tested, arjunilic acid (6) was found to be most potent. Their structure-activity relationship (SAR) showed that if the configuration of the -OH group at C-2 is changed from alpha to beta the potency is decreased. In most of the compounds the position and configuration of the -OH group was found to be important for the inhibitory potency against the enzyme tyrosinase. For the comparison, the standard tyrosinase inhibitors kojic acid (IC50=16.67 microm) and L-mimosine (IC50=3.68 microm) were used as controls.
Publisher: Wiley
Date: 03-12-2011
DOI: 10.1002/SYN.20876
Abstract: Curcuminoids are vital constituent of turmeric, with therapeutic potential in the treatment of Alzheimer's disease. Electrically, stimulus train-elicited plastic changes in hippoc al CA1 excitability were used as an experimental paradigm to study the effects of curcuminoid mixture and in idual components on functional failure induced by Aβ peptide in vitro. Electrical stimulation was applied on Schaffer collaterals, and population spikes (PS) were recorded from stratum pyramidale. To induce long-term potentiation (LTP) of PS, primed burst stimulation (PBs) was used. Aβ peptide inhibited PS LTP induction. Sinking PS LTP due to Aβ peptide was rescued when curcuminoid mixture was applied before PBs only at lower dose (0.1 μM) resulting in PS potentiation to 127.42% ± 1.83% at 5 min and 123.98% ± 1.06% at 60-min post-PBs. Similarly, when bisdemethoxycurcumin was applied, PS LTP was induced and lasted only at a single dose (0.1 μM). Demethoxycurcumin was effective at a middle dose (1 μM), so that the PS litude was changed to 140.15% ± 2.68% and 129.82% ± 0.44% at 5 and 60 min, respectively. PS LTP was effectively induced in the presence of curcumin at middle and high doses (1 and 30 μM) with resultant PS LTP to 155.68% ± 1.23% and 127.72% ± 1.23%, respectively, at 60-min post-PBs. These results showed that curcuminoids can restore susceptibility for plastic changes in CA1 excitability that is injured by exposure to Aβ peptide and rescue sinking PS LTP in Aβ-peptide-exposed hippoc al CA1 neurons.
Publisher: Wiley
Date: 20-09-2011
DOI: 10.1002/PTR.3303
Abstract: Achillea millefolium Linn. (Asteraceae) is used in folk medicine for the treatment of overactive cardiovascular and respiratory ailments. This study describes its hypotensive, cardio-depressant, vasodilatory and bronchodilatory activities. The crude extract of Achillea millefolium (Am.Cr) caused a dose-dependent (1-100 mg/kg) fall in arterial blood pressure of rats under anaesthesia. In spontaneously beating guinea-pig atrial tissues, Am.Cr exhibited negative inotropic and chronotropic effects. In isolated rabbit aortic rings, Am.Cr at 0.3-10 mg/mL relaxed phenylephrine (PE, 1 µm) and high K(+) (80 mm)-induced contractions, as well as suppressed the PE (1 µm) control peaks obtained in Ca(++) -free medium, like that caused by verapamil. The vasodilator effect of Am.Cr was partially blocked by N(ω) -nitro-l-arginine methyl ester in endothelium intact preparations. In guinea-pig tracheal strips, Am.Cr inhibited carbachol (CCh, 1 µm) and K(+) -induced contractions. These results indicate that Achillea millefolium exhibits hypotensive, cardiovascular inhibitory and bronchodilatory effects, thus explaining its medicinal use in hyperactive cardiovascular and airway disorders, such as hypertension and asthma.
Publisher: Wiley
Date: 2003
DOI: 10.1002/PTR.1251
Abstract: The in vitro effect of aqueous extract of Nigella sativa seeds on nitric oxide (NO) production by murine macrophages was studied. Murine peritoneal macrophages were pre-incubated with the extract and then activated with Escherichia coli lipopolysaccharride. NO production was measured after 24 hours by spectrophotometry. The plant extract caused a dose-dependent decrease in NO production. Dialyzed preparation of the extract did not affect NO production. However, the boiled fraction of the extract resulted in a dose-dependent inhibition of NO apparently comparable to that of the whole extract. These results indicate that the aqueous extract of N. sativa seeds exhibits an inhibitory effect on nitric oxide production by murine macrophages and the active component(s) is/are non-protein in nature. In view of the fact that nitric oxide is a pro-inflammatory mediator, this study validates the traditional use of the Nigella sativa seeds for the treatment of rheumatism.
Publisher: Hindawi Limited
Date: 2007
DOI: 10.1155/2007/730785
Abstract: Neuropathic pain (NeP), generated by disorders of the peripheral and central nervous system, can be particularly severe and disabling. Prevalence estimates indicate that 2% to 3% of the population in the developed world suffer from NeP, which suggests that up to one million Canadians have this disabling condition. Evidence-based guidelines for the pharmacological management of NeP are therefore urgently needed. Randomized, controlled trials, systematic reviews and existing guidelines focusing on the pharmacological management of NeP were evaluated at a consensus meeting. Medications are recommended in the guidelines if their analgesic efficacy was supported by at least one methodologically sound, randomized, controlled trial showing significant benefit relative to placebo or another relevant control group. Recommendations for treatment are based on degree of evidence of analgesic efficacy, safety, ease of use and cost-effectiveness. Analgesic agents recommended for first-line treatments are certain antidepressants (tricyclics) and anticonvulsants (gabapentin and pregabalin). Second-line treatments recommended are serotonin noradrenaline reuptake inhibitors and topical lidocaine. Tramadol and controlled-release opioid analgesics are recommended as third-line treatments for moderate to severe pain. Recommended fourth-line treatments include cannabinoids, methadone and anticonvulsants with lesser evidence of efficacy, such as lamotrigine, topiramate and valproic acid. Treatment must be in idualized for each patient based on efficacy, side-effect profile and drug accessibility, including cost. Further studies are required to examine head-to-head comparisons among analgesics, combinations of analgesics, long-term outcomes, and treatment of pediatric and central NeP.
Publisher: Wiley
Date: 17-03-2016
DOI: 10.1002/PTR.5610
Abstract: The crude ethanolic extract of Chrozophora prostrata (Cp.Cr) was tested using in vivo and ex vivo assays for its possible bronchodilatory effects in order to validate its medicinal use in respiratory disorders, like asthma and cough. Cp.Cr exhibited dose-dependent inhibition of carbachol (CCh)-induced bronchospasm in anesthetized rats, similar to aminophylline. When tested on guinea-pig tracheal preparations, Cp.Cr caused relaxation of both CCh (1 μM) and high K(+) (80 mM)-induced contractions with comparable potencies, similar to papaverine, a dual inhibitor of phosphodiesterse (PDE) and Ca(+2) influx. Pre-treatment of the tracheal tissues with Cp.Cr resulted in potentiation of the inhibitory effect of isoprenaline on CCh-induced contractions, like that caused by papaverine indicative of PDE inhibitory activity, which was confirmed when Cp.Cr concentration dependently (1 and 3 mg/mL) increased intracellular cAMP levels of the tracheal preparations, like papaverine. Cp.Cr shifted concentrationresponse curves of Ca(+2) constructed in guinea-pig tracheal preparation towards right with suppression of the maximum response, similar to both verapamil and papaverine. These data indicate bronchodilator activity of Chrozophora prostrata mediated possibly through dual inhibition of PDE and Ca(+2) influx, thus, showing therapeutic potential in asthma with effect enhancing and side-effect neutralizing potential Copyright © 2016 John Wiley & Sons, Ltd.
Publisher: Springer Science and Business Media LLC
Date: 06-10-2022
DOI: 10.1186/S13098-022-00916-8
Abstract: Maternal complications of pregnancy, including hypertensive disorders of pregnancy, gestational diabetes mellitus, intrauterine growth restriction, preterm labour, and placental abruption, are associated with increased risk of future cardiometabolic disease. Lifestyle interventions that focus on preventative strategies for this young, high-risk population of women may assist in cardiometabolic disease risk reduction. The aim of this preliminary registry analysis was to observe the change in maternal metabolic syndrome status after receiving a nurse practitioner-led lifestyle intervention delivered soon after a complicated pregnancy. This preliminary analysis included 64 eligible women who had attended both baseline (approximately 6 months postpartum) and review (approximately eighteen months postpartum) appointments at the postpartum lifestyle clinic after an index pregnancy complicated by at least one maternal complication of pregnancy. Metabolic syndrome status at both appointments was assessed. At the baseline appointment, 22 (34.4%) women met the criteria for metabolic syndrome. This number reduced at the review appointment to 19 (29.7%). This difference was not statistically significant. There were some modest improvements in the in idual cardiometabolic risk factors, as well as marked improvements in the women who had recovered from metabolic syndrome over twelve months. There was a high percentage of metabolic syndrome present early in the postpartum period. The results of this preliminary analysis highlight the importance of continuing preventative care and ongoing research for this group of high-risk women.
Publisher: Wiley
Date: 04-07-2013
DOI: 10.1002/PTR.4761
Abstract: Desmostachya bipinnata, despite of its popular medicinal uses, has not been widely studied for its effect in diarrhea, indigestion, and asthma. The aim of the present investigation was to provide scientific rationale for these applications. The crude aqueous-methanolic extract of D. bipinnata (Db.Cr) was evaluated through in vivo and in vitro experiments. Db.Cr (100-500 mg/kg) protected mice against castor oil-induced diarrhea, similar to loperamide. When tested on gut preparations, Db.Cr produced an atropine-sensitive spasmogenic effect in rabbit jejunum up to 5 mg/mL, followed by a partial relaxation at 10 mg/mL. With atropine preincubation, a verapamil-like inhibitory effect was evident against spontaneous and high K(+) (80 mM)-induced contractions. The maximum stimulant effect was comparable with the acetylcholine-induced maximum contraction and was similarly reproducible in guinea pig ileum. Db.Cr inhibited carbachol (1 μM)-induced contraction in rabbit trachea but caused an atropine-sensitive accentuation of high K(+) -induced contraction at 0.003-0.3 mg/mL followed by inhibition at 1-5 mg/mL. On activity-directed fractionation, inhibitory effect was concentrated on organic and stimulant effect in aqueous fraction. This study, suggesting the presence of calcium antagonist activity, possibly underlying its medicinal effect in hyperactive gut and respiratory disorders, and cholinergic activity, possibly underlying its digestive effect, provides rationale for these therapeutic uses of D. bipinnata.
Publisher: Springer Science and Business Media LLC
Date: 27-07-2011
DOI: 10.1007/S11418-011-0566-2
Abstract: Swertia chirata is used in folk medicine for the treatment of constipation, colic, diarrhea, and asthma. This study was carried out in order to provide a pharmacological basis for its medicinal use in gastrointestinal and respiratory disorders. Crude extract of Swertia chirata (Sc.Cr) and its fractions were studied using rabbit isolated tissue preparations. In jejunum, Sc.Cr, which tested positive for alkaloids, flavonoids, saponins, tannins, and terpenes, caused stimulation at concentrations of 0.01-1.0 mg/mL, followed by a relaxant effect at higher concentrations. In the presence of atropine, the contractile effect was blocked and only relaxation occurred. Sc.Cr inhibited high K(+) (80 mM)-induced contractions at 0.01-10 mg/mL and shifted Ca(2+) concentration-response curves to the right, similar to that caused by verapamil. In trachea, Sc.Cr relaxed the carbachol (1 μM) and high K(+)-induced contractions, in a pattern similar to that of verapamil. Bioassay directed fractionation revealed the separation of spasmogenic and spasmolytic components in aqueous and organic fractions, respectively. The chloroform fraction exhibited a concentration-dependent (0.1-3.0 mg/mL) bronchodilator effect. These results indicate that Swertia chirata exhibits gut excitatory and inhibitory effects, mediated through cholinergic and Ca(2+) antagonist mechanisms, respectively, as well as bronchodilatation, via Ca(2+) channel blockade. Thus, this study provides a sound mechanistic background for the therapeutic application of Swertia chirata in gut motility disorders, such as constipation, colic, and diarrhea, and airways hyperactivity disease, such as asthma.
Publisher: BMJ
Date: 07-06-2010
DOI: 10.1136/BMJ.C2641
Publisher: Science Alert
Date: 02-2014
Publisher: Science Alert
Date: 02-2015
Publisher: Springer Science and Business Media LLC
Date: 29-07-2013
Publisher: Springer Science and Business Media LLC
Date: 27-03-2013
Abstract: The present study was aimed to provide ethnopharmacological basis for the medicinal use of Viola betonicifolia whole plant in indigestion and constipation. Mice were used in in-vivo prokinetic and laxative studies while in-vitro experiments were conducted on isolated tissues of rabbit and guinea-pig gut preparations suspended in a tissue bath to measure isotonic contractions. The crude methanolic extract of Viola betonicifolia (VBME) showed partially atropine-sensitive prokinetic (50 and 100 mg/kg) and laxative (30 and 100 mg/kg) activities in mice. When tested in isolated rabbit jejunum and guinea-pig ileum, VBME caused dose-dependent contractions at 0.01-0.3 mg/mL and 0.03-5 mg/mL, respectively. The spasmogenic effect was partially sensitive to atropine, while the presence of pyrilamine, SB203186 or hexamethonium had no effect in both gut preparations. VBME partially inhibited acetylcholinesterase enzyme (19%) in the in-vitro assay. The spasmodic effect of VBME was more efficacious in guinea-pig ileum than rabbit jejunum preparation. The phytochemical analysis of the crude methanolic extract for total alkaloids and saponins revealed that the VBME is a rich source of alkaloids and saponins. This study showed the prokinetic and laxative effects of Viola betonicifolia in mice, partially mediated through cholinergic action. The in-vitro spasmodic effect of the plant extract was also partially sensitive to atropine indicating more than one mechanisms in the gut stimulant effect. This study provides a rationale for the medicinal use of Viola betonicifolia in indigestion and constipation.
Publisher: Elsevier BV
Date: 2022
Publisher: Wiley
Date: 2006
DOI: 10.1002/PTR.1897
Abstract: The crude extract of Achillea millefolium (Am.Cr) was studied for its possible hepatoprotective effect against d-galactosamine (d-GalN) and lipopolysaccharide (LPS) induced hepatitis in mice and antispasmodic effect in isolated gut preparations to rationalize some of the folklore uses. Co-administration of d-GalN (700 mg/kg) and LPS (25 microg/kg) produced 100% mortality in mice. Pre-treatment of animals with Am.Cr (300 mg/kg) reduced the mortality to 40%. Co-administration of d-GalN (700 mg/kg) and LPS (1 microg/kg) significantly raised the plasma alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels compared with values in the control group (p < 0.05). Pre-treatment of mice with Am.Cr (150-600 mg/kg) significantly prevented the toxins induced rise in plasma ALT and AST (p < 0.05). The hepatoprotective effect of Am.Cr was further verified by histopathology of the liver, which showed improved architecture, absence of parenchymal congestion, decreased cellular swelling and apoptotic cells, compared with the toxin group of animals. In isolated rabbit jejunum preparations, Am.Cr caused a concentration-dependent (0.3-10 mg/mL) relaxation of both spontaneous and K(+)-induced contractions as well as shifting the Ca(++) concentration-response curves (CRCs) to the right, similar to that caused by verapamil. These results indicate that the crude extract of Achillea millefolium exhibits a hepatoprotective effect, which may be partly attributed to its observed calcium channel blocking activity.
Publisher: Ovid Technologies (Wolters Kluwer Health)
Date: 2005
DOI: 10.1097/00005344-200501000-00013
Abstract: Ginger (Zingiber officinale Roscoe), a well-known spice plant, has been used traditionally in a wide variety of ailments including hypertension. We report here the cardiovascular effects of ginger under controlled experimental conditions. The crude extract of ginger (Zo.Cr) induced a dose-dependent (0.3-3 mg/kg) fall in the arterial blood pressure of anesthetized rats. In guinea pig paired atria, Zo.Cr exhibited a cardiodepressant activity on the rate and force of spontaneous contractions. In rabbit thoracic aorta preparation, Zo.Cr relaxed the phenylephrine-induced vascular contraction at a dose 10 times higher than that required against K (80 mM)-induced contraction. Ca2+ channel-blocking (CCB) activity was confirmed when Zo.Cr shifted the Ca2+ dose-response curves to the right similar to the effect of verapamil. It also inhibited the phenylephrine (1 microM) control peaks in normal-Ca2+ and Ca2+-free solution, indicating that it acts at both the membrane-bound and the intracellular Ca2+ channels. When tested in endothelium-intact rat aorta, it again relaxed the K-induced contraction at a dose 14 times less than that required for relaxing the PE-induced contraction. The vasodilator effect of Zo.Cr was endothelium-independent because it was not blocked by L-NAME (0.1 mM) or atropine (1 microM) and also was reproduced in the endothelium-denuded preparations at the same dose range. These data indicate that the blood pressure-lowering effect of ginger is mediated through blockade of voltage-dependent calcium channels.
Publisher: Elsevier BV
Date: 03-2010
DOI: 10.1016/J.VETPAR.2009.11.005
Abstract: This paper describes the in vivo anthelmintic activity of Azadirachta indica seeds to justify their use in South-Asia by traditional animal healers. Seeds of A. indica were administered as crude powder (CP), crude aqueous (CAE) and crude methanolic extracts (CME) at the doses of 1 and 3g/kg of body weight to sheep naturally infected with mixed species of gastrointestinal nematodes. The study design also included untreated as well as treated controls. Faecal egg count reduction and larval counts from coprocultures were performed pre- and post-treatments to assess the anthelmintic activity. Crude powder and CME did not show significant activity (P>0.05) at the lower dose used but were found effective at 3g/kg and the maximum anthelmintic effect was observed at the 15 days post-treatment with both crude powder and CME (P<0.01) with a maximum reduction of 29.3% and 40.2%, respectively in eggs per gram of faeces. Haemonchus contortus and Trichostrongylus species were found susceptible (P<0.01) to higher doses of CP and CME of A. indica. However, CAE did not exhibit any considerable reduction in EPG as well as larval counts. Levamisole (7.5mg/kg), a standard anthelmintic agent, exhibited 99.2% reduction in EPG (P<0.001). Though of low efficacy compared with levamisole, the use of A. indica seeds against gastrointestinal nematodes may be justified in some situations, depending on the nature and intensity of the helminth infections.
Publisher: Elsevier BV
Date: 06-2006
DOI: 10.1016/J.JEP.2005.12.031
Abstract: This paper describes the anthelmintic activity of Zingiber officinale Roscoe (family Zingiberaceae) rhizome, commonly known as ginger, to justify its traditional use in veterinary medicine. Crude powder (CP) and crude aqueous extract (CAE) of dried ginger (1-3 g/kg) were administered to sheep naturally infected with mixed species of gastrointestinal nematodes. Both CP and CAE exhibited a dose- and a time-dependent anthelmintic effect with respective maximum reduction of 25.6% and 66.6% in eggs per gram (EPG) of faeces on day 10 of post-treatment. Levamisole (7.5 mg/kg), a standard anthelmintic agent, exhibited 99.2% reduction in EPG. This study shows that ginger possesses in vivo anthelmintic activity in sheep thus justifying the age-old traditional use of this plant in helminth infestation.
Publisher: Elsevier BV
Date: 06-1995
Publisher: Elsevier BV
Date: 2009
DOI: 10.1016/J.VPH.2008.09.003
Abstract: The present investigation was aimed at providing the pharmacological basis for the medicinal use of a polyherbal formulation (POL-10) in hypertension and dyslipidemia. In spontaneously hypertensive rats, POL-10 significantly (p<0.05) reduced blood pressure to 183.2+/-2.97 vs 198.1+/-5.2 mmHg (Mean+/-S.E.M n=7-10), improved endothelial dysfunction (p<0.01) by increasing acetylcholine-induced relaxation up to 46.0+/-6.7% vs 24.6+/-3.8% (n=5-10) and decreased serum triglycerides (TG) to 54.5+/-3.3 vs. 93.84+/-5.7 mg/dl (p<0.001). In high fat diet-induced hypercholesterolemia, POL-10 caused reduction in total cholesterol (TC), low density lipoproteins (LDL) levels and the atherogic index (TC-HDL/HDL). It decreased TG levels in tyloxapol-induced hyperlipidemia and increased high-density lipoprotein cholesterol (HDL-C) and reduced atherogenic index in normotensive rats. It exhibited strong antioxidant activity in different in vitro assays. In isolated smooth muscle preparation, POL-10 exhibited calcium channel blocking (CCB) activity by inhibition of high K(+)- induced contractions and rightward shift of Ca(++) concentration-response curves similar to that of verapamil. In conclusion, these findings rationalize the medicinal use of POL-10 in cardiovascular disorders which are mediated through multiple pathways such as, antioxidant, CCB, inhibition of lipid biosynthesis and absorption.
Publisher: Elsevier
Date: 2016
Publisher: Bangladesh Journals Online (JOL)
Date: 22-07-2014
Publisher: Wiley
Date: 25-08-2017
DOI: 10.1002/PTR.5907
Abstract: Achyranthes aspera L. is traditionally used to relieve constipation, diarrhea, and asthma. Its crude extract (Aa.Cr) was evaluated through in vivo and ex vivo experiments to rationalize these medicinal uses of A. aspera and to provide their scientific basis. Aa.Cr, at 3 and 10 mg/kg, increased fecal output, similar to castor oil, whereas at 30, 100, 300, and 700 mg/kg, it protected against castor oil-induced diarrhea in mice when administered orally. Aa.Cr caused spasmogenic effect on rabbit jejunum and guinea pig ileum preparations, which was partially inhibited by atropine while completely blocked by cyproheptadine preincubation. Aa.Cr also relaxed high K
Publisher: Wiley
Date: 25-09-2013
DOI: 10.1002/PTR.4819
Abstract: The aim of this study was to see if the crude extract of Lepidium sativum (Ls.Cr) exhibits species specificity in its antidiarrheal and antispasmodic activities along with insight into the underlying mechanisms using the in‐vivo and in‐vitro experiments. Ls.Cr inhibited castor oil‐induced diarrhea in mice at doses (300 and 1000 mg/kg) three times higher dose than for rats. In isolated rat ileum and jejunum, Ls.Cr completely inhibited carbachol (CCh), low K + (25 mM) and high K + (80 mM)‐induced contractions, while in guinea‐pig tissues, Ls.Cr caused complete inhibition of only CCh‐induced contraction. In rabbit tissues, Ls.Cr completely inhibited CCh and low K + ‐induced contractions sensitive to K + channel antagonists. Pretreatment of guinea‐pig and rat tissues with Ls.Cr caused a rightward shift in CCh‐induced contractions in a pattern similar to dicyclomine, while in rabbit and rat tissues, Ls.Cr shifted isoprenaline curves to the left similar to papaverine. These data indicate that the antidiarrheal and antispasmodic activities of L. sativum are species dependent, mediating its antispasmodic effect through combinations of multiple pathways including activation of K + channels, and inhibition of muscarinic receptors, Ca ++ channels and PDE enzyme. Rat tissues showed the highest potency. Based on the results, we recommend using multiple species to know the real pharmacological profile of medicinal products. Copyright © 2012 John Wiley & Sons, Ltd.
Publisher: Proceedings of the National Academy of Sciences
Date: 26-05-1998
Abstract: Cardiac myocytes have been shown to express constitutively endothelial nitric oxide synthase (eNOS) (nitric oxide synthase 3), the activation of which has been implicated in the regulation of myocyte L-type voltage-sensitive calcium channel current (I Ca-L ) and myocyte contractile responsiveness to parasympathetic nervous system signaling, although this implication remains controversial. Therefore, we examined the effect of the muscarinic cholinergic agonist carbachol (CCh) on I Ca-L and contractile litude in isoproterenol (ISO)-prestimulated ventricular myocytes isolated from adult mice, designated eNOS null mice, with targeted disruption of the eNOS gene. Although both eNOS null and wild-type (WT) ventricular myocytes exhibited similar increases in I Ca-L in response to ISO, there was no measurable suppression of I Ca-L by CCh in cells from eNOS null mice, in contrast to cells from WT mice. These results were reflected in the absence of an effect of CCh on the positive inotropic effect of ISO in eNOS null myocytes. Also, unlike myocytes from WT animals, eNOS null myocytes failed to exhibit an increase in cGMP content in response to CCh. Nevertheless, the pharmacologic nitric oxide donors 3-morpholino-sydnonimine and S-nitroso-acetyl-cystein increased cGMP generation and suppressed ISO-augmented I Ca-L in eNOS null cells, suggesting that the signal transduction pathway(s) downstream of eNOS remained intact. Of importance, activation of the acetylcholine-activated K + channel by CCh was unaffected in atrial and ventricular eNOS null myocytes. These results confirm the obligatory role of eNOS in coupling muscarinic receptor activation to cGMP-dependent control of I Ca-L in cardiac myocytes.
Publisher: Elsevier BV
Date: 07-2019
Publisher: Elsevier BV
Date: 12-1992
Publisher: Elsevier BV
Date: 07-2005
DOI: 10.1016/J.BBRC.2005.05.068
Abstract: The alkaloid juliflorine (1) from Prosopis juliflora inhibited acetylcholinesterase (AChE, EC 3.1.1.7) and butyrylcholinesterase (BChE, EC 3.1.1.8) enzymes in a concentration-dependent fashion with IC50 values 0.42 and 0.12 microM, respectively. Lineweaver-Burk as well as Dixon plots and their secondary replots indicated that the nature of inhibition was purely of non-competitive type with Ki values 0.4 and 0.1 microM, against AChE and BChE, respectively. By molecular docking studies compound 1 was found to be ideally spaced inside the aromatic gorge of AChE with rings A/B remaining at the top and rings C/D penetrating deep into the gorge, that might be due to the greater hydrophobicity of rings C/D as compared to rings A/B, allowing their simultaneous interaction with the peripheral anionic and quaternary ammonium-binding sites. The 1-AChE complex was found to be stabilized by hydrophobic contacts, hydrogen bonding, and pi-pi stacking between the compound 1 and amino acid residues of the aromatic gorge of AChE. Amino acid residues Tyr70, Asp72, Tyr121, Trp279, and Tyr334 of the peripheral anionic site (PAS) of AChE were found to be exclusively involved in the hydrophobic contacts with compound 1 that might be responsible for the competitive mode of inhibition. Compound 1 also showed dose-dependent (30-500 microg/mL) spasmolytic and Ca2+-channel blocking activities in isolated rabbit jejunum preparations. The cholinesterase inhibitory potential along with calcium-channel blocking activity of compound 1 and safe profile in human neutrophils viable assay could make it a possible drug candidate for Alzheimer's disease.
Publisher: Elsevier BV
Date: 07-2011
Publisher: Informa UK Limited
Date: 30-05-2020
Publisher: Wiley
Date: 14-11-2011
DOI: 10.1002/PTR.3600
Abstract: In continuation of our work on Indian celery (Seseli diffusum (Roxb. ex Sm.) Santapau & Wagh Umbelliferae), the fractionation of the 80% MeOH-H(2) O extract of the seeds was performed to identify the principles responsible for its folk use as an antispasmodic and diuretic. Several compounds were isolated as active components: seselin (1) and anthriscinol methyl ether (4) showed a selective cytotoxicity to some yeast strains. Compound 1 also showed spasmolytic activity. On the other hand, isopimpinellin (3) and isorutarin (5) exhibited a spasmogenic effect on the smooth muscle preparations. Compound 5 was also found to have antioxidant activity. Among them, compound 4 was isolated for the first time from this plant.
Publisher: MDPI AG
Date: 12-03-2012
DOI: 10.3390/IJMS13033291
Publisher: Ovid Technologies (Wolters Kluwer Health)
Date: 15-11-1995
DOI: 10.1161/01.CIR.92.10.2855
Abstract: Background N -acetylcysteine (NAC) has been shown to potentiate the effects of nitroglycerin (NTG) and to have antioxidant activity. This is the first study to assess the safety and effect of NAC in the treatment of evolving acute myocardial infarction (AMI). Methods and Results Patients with AMI received either 15 g NAC infused over 24 hours (n=20) or no NAC (n=7), combined with intravenous NTG and streptokinase. Peripheral venous plasma malondialdehyde (MDA), reduced (GSH) and oxidized (GSSG) glutathione concentrations, and rate of reperfusion (using continuous ST-segment analysis) were measured. Cardiac catheterization was performed between days 2 and 5. No significant adverse events occurred. Less oxidative stress occurred in patients treated with NAC than in patients not receiving NAC (GSH to GSSG ratio 44±25 versus 19±13 at 4 hours, P .05). NAC concentration (mean 172±79 μmol/L at 4 hours) was correlated to GSH concentration ( P =.006). MDA concentrations were lower ( P =.001) over the first 8 hours of treatment with NAC. There was a trend toward more rapid reperfusion (median 58 minutes, 95% confidence interval [CI] 48 to 98 minutes versus median 95 minutes, 95% CI 59 to 106 minutes P =.17) and better preservation of left ventricular function (cardiac index 3.4±0.8 versus 2.6±0.27 L · min · m 2 , P =.009) with NAC treatment. Conclusions NAC in combination with NTG and streptokinase appeared to be safe for the treatment of evolving AMI and was associated with significantly less oxidative stress, a trend toward more rapid reperfusion, and better preservation of left ventricular function.
Publisher: Elsevier BV
Date: 2021
Publisher: Springer Science and Business Media LLC
Date: 12-2014
Publisher: Science Alert
Date: 15-09-2015
Publisher: Wiley
Date: 1998
DOI: 10.1002/(SICI)1099-1573(1998)12:1+<S63::AID-PTR252>3.0.CO;2-7
Publisher: Wiley
Date: 08-1995
Publisher: Elsevier BV
Date: 02-2000
DOI: 10.1016/S0367-326X(99)00098-2
Abstract: Berberis aristata is an edible plant employed in the South Asian Traditional Medicine, particularly its fruits being used as a tonic remedy for liver and heart. In this investigation, berberine, a known compound from this plant, was studied for its possible antihepatotoxic action in rats. Pretreatment of animals with berberine (4 mg/kg orally twice daily for 2 days) prevented the acetaminophen- or CCl4-induced rise in serum levels of alkaline phosphatase (ALP) and aminotransaminases (AST and ALT), suggestive of hepatoprotection. Post-treatment with three successive oral doses of berberine (4 mg/kg every 6 h) reduced the hepatic damage induced by acetaminophen, while CCl4-induced hepatotoxicity was not modified, suggesting a selective curative effect against acetaminophen. Pretreatment of animals with a single oral dose of berberine (4 mg/kg) induced prolongation of the pentobarbital (60 mg/kg, i.p.)-induced sleeping time as well as increased strychnine (0.3 mg/kg i.p.)-induced toxicity, suggestive of inhibitory effect on microsomal drug metabolizing enzymes, cytochrome P450s (CYPs).
Publisher: Elsevier BV
Date: 02-2009
DOI: 10.1016/J.PBB.2008.09.010
Abstract: Curcuminoids (a mixture of curcumin, bisdemethoxycurcumin and demethoxycurcumin) share vital pharmacological properties possessed by turmeric, a well known curry spice, considered useful in Alzheimer's disease (AD). The aim of this study was to evaluate if curcuminoids possess acetylcholinesterase (AChE) inhibitory and memory enhancing activities. The in-vitro and ex-vivo models of AChE inhibitory activity were used along with Morris water maze test to study the effect on memory in rats. Curcuminoids inhibited AChE in the in-vitro assay with IC(50) value of 19.67, bisdemethoxycurcumin 16.84, demethoxycurcumin 33.14 and curcumin 67.69 microM. In the ex-vivo AChE assay, curcuminoids and its in idual components except curcumin showed dose-dependent (3-10 mg/kg) inhibition in frontal cortex and hippoc us. When studied for their effect on memory at a fixed dose (10 mg/kg), all compounds showed significant (p<0.001) and comparable effect in scopolamine-induced amnesia. These data indicate that curcuminoids and all in idual components except curcumin possess pronounced AChE inhibitory activity. Curcumin was relatively weak in the in-vitro assay and without effect in the ex-vivo AChE model, while equally effective in memory enhancing effect, suggestive of additional mechanism(s) involved. Thus curcuminoids mixture might possess better therapeutic profile than curcumin for its medicinal use in AD.
Publisher: Science Alert
Date: 15-02-2007
DOI: 10.3923/PJBS.2007.792.796
Abstract: Hydro-ethanolic crude extract of Hypericum perforatum Linn. family hypericaceae (St. John's Wort) aerial parts (Hp. Cr) was studied for its possible antinociceptive effect against acetic acid-induced abdominal constriction assay in mice. Hp. Cr (10-20 mg kg(-1)), opium (10-30 mg kg(-1)), morphine (0.75-3.0 mg kg(-1)) and aspirin (50-100 mg kg(-1)) showed dose-dependent antinociceptive effect. In animals treated with naloxone (0.5 mg kg(-1)), the antinociceptive effect of Hp. Cr was significantly reduced similar to that of opium, while effect of aspirin remained unchanged. These results suggest that the antinociceptive effect of Hypericum perforatum may be mediated through activation of opioid receptors.
Publisher: Informa UK Limited
Date: 30-04-2015
DOI: 10.3109/10641963.2014.913602
Abstract: In current study, we describe blood pressure (BP)-lowering, endothelium-dependent, and independent vasodilator and cardio-modulatory actions of Carum roxburghianum seed. The crude extract of C. roxburghianum seed (Cr.Cr) induced dose-dependent (10-100 mg/kg) fall in arterial BP of anaesthetized rats. In isolated rabbit aorta, Cr.Cr (0.3-10 mg/mL) inhibited high K+ (80 mM) and phenylephrine (PE, 1 µM)-induced contractions, like verapamil and papaverine. In endothelium-intact rat aortic preparations, Nω-nitro-L-arginine methyl ester hydrochloride-sensitive vasodilator activity was observed with Cr.Cr, which also relaxed endothelium-denuded aorta tissues. In guinea-pig atria, Cr.Cr initially caused mild cardiac stimulation, followed by inhibition, as shown by papaverine. These results reveal that cardiovascular effects of C. roxburghianum seed extract are mediated possibly through combination of Ca++ antagonist, nitric oxide modulating and phosphodiesterase inhibitory mechanisms, though further in-depth studies are required for elucidating precise mode of action.
Publisher: Wiley
Date: 12-09-2013
DOI: 10.1002/PTR.4821
Abstract: This study was aimed to provide pharmacological basis for the medicinal use of Phyllanthus emblica fruit in indigestion and constipation using the in‐vivo and in‐vitro assays. The crude extract of the dried fruits of Phyllanthus emblica (Pe.Cr) and its fractions were tested positive for alkaloids, saponins, tannins, terpenes, flavonoids, sterols and coumarins. Pe.Cr at the doses of 100 and 300 mg/kg exhibited the prokinetic and laxative activities in mice, which were found partially sensitive to atropine. In isolated guinea‐pig ileum and rabbit jejunum, the crude extract and its aqueous fraction (Pe.Aq) caused concentration‐dependent and partially atropine‐sensitive stimulatory effects followed by relaxation at higher tested concentrations, being more efficacious in guinea pig, while more potent in rabbit tissues. The petroleum fraction (0.003–0.1 mg/mL) exhibited fully atropine‐sensitive contractions in both guinea‐pig and rabbit tissues. However, the ethyl acetate and chloroform fractions (0.003–1.0 mg/mL) showed only spasmolytic activity when studied in spontaneously contracting rabbit jejunum. This study showed that the Phyllanthus emblica possesses prokinetic and laxative activities in mice along with spasmodic effect in the isolated tissues of guinea pig and rabbit, mediated partially through activation of muscarinic receptors thus, this study provides a rationale for the medicinal use of Phyllanthus emblica fruits in indigestion and constipation. Copyright © 2012 John Wiley & Sons, Ltd.
Publisher: Bangladesh Journals Online (JOL)
Date: 10-2016
Abstract: This study was aimed to investigate the effect of the extract of em Mentha longifolia /em on blood pressure and the possible mechanisms. In anesthetized rats, the crude extract of em M. /em longifolia and aqueous and chloroform fractions caused a dose-dependent fall in mean arterial pressure. Atropine pretreatment abolished the effect of extract and aqueous fraction but did not change that of chloroform fraction. In rabbit aortic rings, crude extract relaxed phenylephrine (1 µM) and high K sup + /sup (80 mM) pre-contractions. Chloroform fraction was more potent against high K sup + /sup , similar to verapamil and caused a rightward shift in the Ca sup ++ /sup concentration-response curves. Aqueous fraction partially relaxed high K sup + /sup pre-contractions. In rat aortic rings, crude extract and aqueous fraction-induced endothelium-dependent atropine-sensitive vasodilator effect. Extract and fractions also relaxed high K sup + /sup precontractions. In guinea-pig atrial strips, crude extract and chloroform fraction suppressed force and rate of contractions, similar to verapamil. In conclusion, em M. /em longifolia lowers blood pressure through Ca sup ++ /sup channel blockade and atropine-sensitive-NO pathway. strong Video Clip: /strong a href="/Fz0MrZ6q2WI" Experiment using aorta: /a 2 min 35 sec
Publisher: Science Alert
Date: 15-06-2017
Publisher: Public Library of Science (PLoS)
Date: 20-01-2023
DOI: 10.1371/JOURNAL.PONE.0280451
Abstract: We aimed to compare risk factors for CVD 10 years postpartum among women who had ≥ 1 compared to no cardio metabolic risk factor in early first pregnancy. Women of the SCOPE (Screening fOr Pregnancy Endpoints) study from Adelaide, South Australia were invited to participate in a cardiovascular risk assessment 10 years after the delivery of the first child. Data from 141 women who completed all the assessments are included in the analyses. Compared to women who did not have any cardio metabolic risk factor at 15 ± 1 weeks’ gestation during the first pregnancy, those who had ≥ 1 risk factor were 5.5 times more likely to have metabolic syndrome 10 years postpartum (aOR = 5.5, 95% CI 1.8–17.3, p = 0.004). Women who had ≥ 1cardio metabolic risk factor during the first pregnancy were more likely to be obese (p = 0.001), have high total cholesterol levels (p .001) or have increased insulin resistance (p .001) 10 years later compared to women who had no risk factor during the first pregnancy. 63.5% of the women with no cardio metabolic risk factor compared to 39% of women who had ≥ 1 risk factor in first pregnancy, had neither a complicated first pregnancy nor was diagnosed with MetS 10 years postpartum (p = 0.023). Cardio metabolic risk factors at the booking visit in the first pregnancy may be useful in identifying young women at risk of future CVD.
Publisher: Springer Science and Business Media LLC
Date: 10-2012
Abstract: The aqueous-methanolic extract of Amaranthus spinosus ( A. spinosus Linn.,) whole plant, was studied for its laxative, spasmolytic and bronchodilator activities to validate some of its medicinal uses. The crude extract of A. spinosus was studied in-vivo for bronchodilator and laxative activities and in-vitro using isolated tissue preparations which were mounted in tissue baths assembly containing physiological salt solutions, maintained at 37°C and aerated with carbogen, to assess the spasmolytic effect and to find out the possible underlying mechanisms. In the in-vivo experiments in mice, the administration of A. spinosus increased fecal output at doses of 100 and 300 mg/kg showing laxative activity. It also inhibited carbachol-induced bronchospasm in anesthetized rats at 1, 3, 10 and 30 mg/kg indicative of bronchodilator activity. When tested on isolated gut preparations, the plant extract showed a concentration-dependent (0.01-10.0 mg/ml) spasmogenic effect in spontaneously contracting rabbit jejunum and guinea-pig ileum. The spasmogenic effect was partially blocked in tissues pretreated with atropine (0.1 μM). When tested on K + (80 mM)-induced sustained contractions in isolated rabbit jejunum, the plant extract caused complete relaxation and also produced a shift in the Ca ++ concentration-response curves (CRCs) towards right, similar to diltiazem. In rabbit trachea, the plant extract completely inhibited K + (80 mM) and carbachol (CCh, 1 μM)-induced contractions at 1 mg/ml but pretreatment of tissue with propranolol (1 μM), caused around 10 fold shift in the inhibitory CRCs of the plant extract constructed against CCh-induced contraction. The plant extract (up to 0.3 mg/ml) also increased both force and rate of spontaneous contractions of isolated guinea-pig atria, followed by relaxation at higher concentration (1.0-5.0 mg/ml). The cardio-stimulant effect was abolished in the presence of propranolol, similar to that of isoprenaline. Activity-directed fractionation revealed that the spasmolytic component(s) was separated in the organic fraction, whereas the spasmogenic component was concentrated in the aqueous fraction. These results indicate that A. spinosus possesses laxative activity partially mediated through cholinergic action. The spasmolytic effect was mediated through calcium channel blocking (CCB), while bronchodilator activity through a combination of β-adrenergic and CCB pathways, which may explain the traditional uses of A. spinosus in gut and airways disorders.
Publisher: Elsevier BV
Date: 12-2007
DOI: 10.1016/J.JEP.2007.08.032
Abstract: In this study, we investigated the crude extract of Borago officinalis leaves (Bo.Cr) for its antispasmodic, bronchodilator, vasodilator and cardio-depressant activities to rationalize some of the traditional uses. Bo.Cr was studied using different isolated tissue preparations including rabbit jejunum, trachea, aorta, and guinea-pig atria. Bo.Cr which was tested positive for flavonoids, coumarins, sterols and tannins produced a concentration-dependent relaxation of spontaneous and K+ (80mM)-induced contractions in isolated rabbit jejunum preparations, suggestive of Ca++ antagonist effect, which was confirmed when pretreatment of the tissue with Bo.Cr produced a rightward shift in the Ca++ concentration-response curves like that caused by verapamil. In rabbit tracheal preparations, Bo.Cr relaxed the carbachol (1microM) and K+-induced contractions. Verapamil also produced non-specific inhibitory effect. In rabbit aorta preparations, Bo.Cr exhibited vasodilator effect against phenylephrine and K+-induced contractions similar to verapamil. When tested in guinea-pig atria, Bo.Cr caused inhibition of both atrial force and rate of contractions. These results suggest that the spasmolytic effects of Bo.Cr are mediated possibly through Ca++ antagonist mechanism, which might explain the traditional use of Borago officinalis in hyperactive gastrointestinal, respiratory and cardiovascular disorders.
Publisher: Portico
Date: 2008
DOI: 10.1358/MF.2008.30.4.1186075
Abstract: This study describes the hypotensive, cardiosuppressant and vasodilator activities of Hyoscyamus niger crude extract (Hn.Cr). Hn.Cr, which tested positive for alkaloids, coumarins, flavonoids, sterols, tannins and terpenes, caused a dose-dependent (10-100 mg/kg) fall in the arterial blood pressure (BP) of rats under anesthesia. In guinea-pig atria, Hn.Cr exhibited a cardiodepressant effect on the rate and force of spontaneous atrial contractions. In isolated rabbit aorta, Hn.Cr (0.01-1.0 mg/ml) relaxed the phenylephrine (PE, 1 microM) and K(+) (80 mM)-induced contractions and suppressed PE (1 microM) control peaks obtained in Ca(++)-free medium similar to that caused by verapamil. The vasodilator effect of Hn.Cr was endothelium-independent as it was not opposed by N (omega)-nitro-L-arginine methyl ester in endothelium-intact rat aortic preparations and also occurred at a similar concentration in endothelium-denuded tissues. These data indicate that Hyoscyamus niger lowers BP through a Ca(++)-antagonist mechanism.
Publisher: Science Alert
Date: 02-2015
Publisher: Elsevier BV
Date: 11-1998
Publisher: Springer Science and Business Media LLC
Date: 10-01-2012
Abstract: This study was undertaken to provide pharmacological basis for the medicinal use of Viola odorata Linn. in hypertension and dyslipidemia using the in vivo and in vitro assays. Viola odorata leaves extract (Vo.Cr), which tested positive for alkaloids, saponins, tannins, phenolics, coumarins and flavonoids, caused a dose-dependent (0.1-1.0 mg/kg) decrease in mean arterial blood pressure in anaesthetized rats. In isolated guinea-pig atria, Vo.Cr equally inhibited force and rate of spontaneous atrial contractions. On the baseline of rat thoracic aortae (endothelium-intact and denuded), the plant extract caused phentolamine-sensitive vasoconstriction. When tested on phenylephrine (PE, 1 μM) and K + (80 mM)-induced vasoconstriction, Vo.Cr caused a concentration-dependent relaxation and also caused a rightward shift of Ca ++ concentration-response curves as well as suppression of PE (1 μM) control peaks in Ca ++ -free medium, similar to that caused by verapamil. In the presence of L-NAME, the relaxation curve of Vo.Cr was partially inhibited showing involvement of Nitric oxide (NO) mediated pathway. In Tyloxapol-induced dyslipidemia, Vo.Cr caused reduction in total cholesterol and triglyceride levels. In high-fat diet-induced dyslipidemia model, the plant extract caused a significant decrease in total cholesterol, LDL-C, atherogenic index and prevented the increase in average body weights, while it increased HDL-C. These data indicate that the vasodilator effect of the plant extract is mediated through multiple pathways like inhibition of Ca ++ influx via membranous Ca ++ channels, its release from intracellular stores and NO-mediated pathways, which possibly explain the fall in BP. The plant also showed reduction in body weight and antidyslipidemic effect which may be due to the inhibition of synthesis and absorption of lipids and antioxidant activities. Thus, this study provides a pharmacologic rationale to the medicinal use of Viola odorata in hypertension and dyslipidemia.
Publisher: Wiley
Date: 04-2009
DOI: 10.1002/PTR.2659
Abstract: This aim of this study was to investigate the crude extract of Buddleja crispa (Bc.Cr) and its active constituent(s) for their antihypertensive and antispasmodic activities. The Bc.Cr caused a dose-dependent (3-10 mg/kg) fall in mean arterial pressure in rats under anesthesia. In rabbit aorta preparations, Bc.Cr (0.03-1 mg/mL) caused inhibition of high K(+) (80 mM) precontractions. The Bc.Cr (0.03-1 mg/mL) also inhibited spontaneous and high K(+) precontractions in rabbit jejunum preparations, suggestive of calcium channel blocking (CCB) activity. CCB activity was further confirmed when pretreatment of the tissues with Bc.Cr (0.03-0.10 mg/mL) caused a rightward shift in Ca(++) concentration response curves, similar to verapamil. Among the pure compounds, BdI-H3 was more potent against the high K(+) than spontaneous contractions and was around eight times more potent than Bc.Cr against the spontaneous contractions while the other two compounds, BdI-2 and BH-3 were inactive. Activity-directed fractionation revealed that the hexane fraction was more potent against K(+) precontractions. These data indicate that Bc.Cr possesses a blood-pressure lowering effect, mediated possibly through CCB, though additional mechanism(s) cannot be ruled out. Among the pure compounds, Bdl-H3 is likely to be the active compound involved in the spasmolytic and possibly BP lowering effect of the parent crude extract.
Publisher: Elsevier BV
Date: 10-2001
DOI: 10.1016/S0024-3205(01)01347-9
Abstract: We investigated the combined effect of 5-hydroxytryptamine (5-HT, serotonin) and calcium ionophore (A23187) on human platelet aggregation. Aggregation, monitored at 37 degrees C using a Dual-channel Lumi-aggregometer, was recorded for 5 min after challenge by a change in light transmission as a function of time. 5-HT (2-200 microM) alone did not cause platelet aggregation, but markedly potentiated A23187 (low dose) induced aggregation. Inhibitory concentration (IC50) values for a number of compounds were calculated as means +/- SEM from dose-response determinations. Synergism between 5-HT (2-5 microM) and A23187 (0.5-2 microM) was inhibited by 5-HT receptor blockers, methysergide (IC50 = 18 microM) and cyproheptadine (IC50 = 20 microM), and calcium channel blockers (verapamil and diltiazem, IC50 = 20 microM and 40 microM respectively). Interpretation of the effects of these blockers is complicated by their lack of specificity. Similarly, U73122, an inhibitor of phospholipase C (PLC), blocked the synergistic effect at an IC50 value of 9.2 microM. Wortmannin, a phosphatidylinositide 3-kinase (PI 3-K) inhibitor, also blocked the response (IC50 = 2.6 microM). However, neither genistein, a tyrosine-specific protein kinase inhibitor, nor chelerythrine, a protein kinase C inhibitor, affected aggregation at concentrations up to 10 microM. We conclude that the synergistic interaction between 5-HT and ionophore may be mediated by activation of PLC/Ca2+ and PI 3-kinase signalling pathways, but definitive proof will require other enzyme inhibitors with greater specificity.
Publisher: Oxford University Press (OUP)
Date: 08-1994
Publisher: Bentham Science Publishers Ltd.
Date: 15-07-2016
Publisher: Hindawi Limited
Date: 2011
DOI: 10.1155/2011/304960
Abstract: Valeriana hardwickii is indigenous to Pakistan, Burma and Ceylon, where it is traditionally being used as an antispasmodic and antidiarrheal, besides its culinary use as spice. The aim of this paper was to provide pharmacological validation to these medicinal uses. The crude aqueous-methanolic extract of Valeriana hardwickii rhizome (Vh.Cr) was studied on isolated rabbit jejunum and castor oil-induced diarrhea in mice for spasmolytic and antidiarrheal properties, respectively. Vh.Cr caused concentration-dependent (0.01–1 mg/mL) relaxation of spontaneous contractions in isolated rabbit jejunum and inhibited K + -induced contractions (0.01–0.3 mg/mL), similar to verapamil, suggestive of calcium channel blockade (CCB). The CCB effect was confirmed when pretreatment of the jejunum preparations with Vh.Cr produced a concentration-dependent (0.03–0.1 mg/mL) rightward shift in the Ca ++ concentration-response curves, as caused by verapamil. Vh.Cr exhibited dose-dependent (100–300 mg/kg) protection against castor oil-induced diarrhea in mice. Loperamide, a standard antidiarrheal drug, similarly prevented the diarrhea. These data indicate the presence of CCB effect in the extract of Valeriana hardwickii rhizome, possibly mediating its antispasmodic and antidiarrheal activities and provide a scientific base for its traditional use in hyperactive gut disorders.
Publisher: Informa UK Limited
Date: 1999
Publisher: Frontiers Media SA
Date: 08-04-2022
Abstract: Sex and gender differences in presentation and characteristics of out-of-hospital cardiac arrest (OHCA) are established in cohorts with presumed cardiac aetiology but not non-cardiac etiology. This study investigated the effect of sex on incidence and outcome of OHCA according to presumed and adjudicated aetiology within a local health network. Population-based observational cohort study of emergency medical services (EMS) attended OHCAs within an Australian local health network. Cases identified from an EMS registry between 2012-2016 were linked to a hospital registry. Age-standardised incidence and baseline characteristics were stratified by sex for EMS-treated OHCA, non-EMS witnessed presumed cardiac and obvious non-cardiac sub-cohorts, and hospitalised cases. Logistic regression was used to explore the primary outcome of survival to hospital discharge. We identified 2,024 EMS-attended and 780 EMS-treated OHCAs. The non-EMS witnessed sub-cohorts comprised 504 presumed cardiac and 168 obvious non-cardiac OHCAs. Adjudicated aetiology was recorded in 123 hospitalised cases. Age-standardised incidence for women was almost half that of men across all groups. Across cohorts, women were generally older and arrested with a non-shockable initial rhythm in an area of low socioeconomic status. There was no sex difference in the primary outcome for the main EMS-treated cohort or in the non-cardiac sub-cohorts. The sex difference in outcome in the presumed cardiac sub-cohort was not present after multivariable adjustment. There are sex differences in incidence and outcome of EMS-treated OHCA that appear to be driven by differences in susceptibility to cardiac arrhythmias and underlying etiology, rather than treatment delays or disparities.
Publisher: Elsevier
Date: 2016
Publisher: Springer Science and Business Media LLC
Date: 30-05-2007
Publisher: Elsevier BV
Date: 12-2003
DOI: 10.1016/J.LFS.2003.06.039
Abstract: The potency, structure-activity relationship, and mechanism of vasorelaxation of a series of flavonoids, representing different subclasses (flavonols: fisetin, rutin, quercetin flavones: chrysin, flavone, baicalein flavanones: naringenin, naringin isoflavones: diadzein and flavanes: epigallo catechin gallate), were examined in the isolated rat aorta. Most of the flavonoids tested showed concentration dependent relaxant effects against K+ (80 mM) and phenylephrine (PE, 0.1 microM)-induced contractions with a greater inhibition of the responses to the alpha1-adrenoceptor agonist. The relaxant effects of most of the flavonoids involve in part the release of nitric oxide and prostaglandins from the endothelium as pretreatment with L-NAME and indomethacin attenuated the responses. In addition, the relaxant action of the flavonoids includes inhibition of Ca+2 influx and release of Ca+2 from intracellular stores. A structure-activity relationship amongst the flavonoids was suggested.
Publisher: Elsevier
Date: 2016
Publisher: Elsevier BV
Date: 07-2000
DOI: 10.1016/S0378-8741(99)00198-1
Abstract: Lavandula stoechas L. (Lamiaceae) has been used for a long time in traditional medicine as an anticonvulsant and antispasmodic. The aqueous-methanolic extract of L. stoechas flowers (LS) was studied for its possible anticonvulsant and antispasmodic activities. When tested in mice, LS (600 mg/kg) significantly reduced the severity and increased the latency of convulsions induced by pentylene tetrazole (PTZ). LS likewise reduced PTZ's lethality. LS up to a dose of 600 mg/kg was found devoid of any hypnotic effect in mice, however, animals were found to be dull, calm and relaxed. The sedative effect of the plant extract was confirmed, as it prolonged the pentobarbital sleeping time in mice similar to that of diazepam. In isolated rabbit jejunum preparations, LS caused a dose-dependent (0.1-1.0 mg/ml) relaxation of spontaneous contractions. LS also inhibited K(+)-induced contractions in a similar dose range, thereby suggesting calcium channel blockade. This effect was confirmed when pretreatment of the jejunum preparation with LS produced a dose-dependent shift of the Ca(2+) dose-response curve to the right, similar to the effect of verapamil, a standard calcium channel blocker. These data indicate that the plant extract exhibits anticonvulsant and antispasmodic activities. Its calcium channel blocking property may be mechanistically related to these activities. Its usefulness in folk medicine appears thus to be based on a sound mechanistic background.
Publisher: Cambridge University Press (CUP)
Date: 19-02-2020
DOI: 10.1017/S2040174420000094
Abstract: Preecl sia (PE) is now recognised as a cardiovascular risk factor for women. Emerging evidence suggests that children exposed to PE in utero may also be at increased risk of cardiovascular disease (CVD) in later life. In iduals exposed to PE in utero have higher systolic and diastolic blood pressure and higher body mass index (BMI) compared to those not exposed to PE in utero . The aim of this review is to discuss the potential mechanisms driving the relationship between PE and offspring CVD. Exposure to an adverse intrauterine environment as a consequence of the pathophysiological changes that occur during a pregnancy complicated by PE is proposed as one mechanism that programs the fetus for future CVD risk. Consistent with this hypothesis, animal models of PE where progeny have been studied demonstrate causality for programming of offspring cardiovascular health by the preecl tic environment. Shared alleles between mother and offspring, and shared lifestyle factors between mother and offspring provide alternate pathways explaining associations between PE and offspring CVD risk. In addition, adverse lifestyle habits can also act as second hits for those programmed for increased CVD risk. PE and CVD are both multifactorial diseases and, hence, identifying the relative contribution of PE to offspring risk for CVD is a very complex task. However, considering the emerging strong association between PE and CVD, those exposed to PE in utero may benefit from targeted primary CVD preventive strategies.
Publisher: Elsevier BV
Date: 11-2018
Publisher: Informa UK Limited
Date: 07-08-2009
Publisher: Springer Science and Business Media LLC
Date: 03-2007
DOI: 10.1007/BF02977610
Publisher: Springer Science and Business Media LLC
Date: 10-2015
DOI: 10.1016/J.PHAREP.2015.03.002
Abstract: The excessive production of reactive oxygen species in nervous tissues is considered one of the major risk factors of neurodegenerative diseases. During the last two decades, much attention has been paid to the antioxidant and anti-inflammatory activity of natural products and compounds isolated from natural products which are often characterized by high efficacy and low adverse effects. Berberine is an isoquinoline alkaloid, widely present in different medicinal herbs, especially in the genus Berberis. It is mainly used as antidiarrhoeal, antibacterial, antifungal, and antiprotozoal agent. However, current research has focused on its beneficial role in neurodegenerative diseases, mainly due to its powerful antioxidant effect. The therapeutic potential of Berberine in different neurodegenerative diseases such as Alzheimer, Parkinson and Huntington disease has been brought to evidence by numerous studies. However, a limited number of reviews focus on the beneficial role of Berberine against neurodegeneration. The main objective of this review is to discuss the role of oxidative stress in neurodegeneration and the potential role of antioxidant compounds, in particular Berberine which is analyzed in its chemical structure, source, bioavailability, therapeutic potential, with special attention to its mechanism of action at a molecular level.
Publisher: Elsevier BV
Date: 10-1998
DOI: 10.1016/S0006-2952(98)00094-X
Abstract: The Cinchona bark contains alkaloids like quinine, quinidine, cinchonine and cinchonidine. These agents are effective antimalarial drugs and have been used clinically in malaria caused by Plasmodium falciparum. Previous studies show that quinine and quinidine exert effects on cardiovascular system. This study was conducted to examine the effect of cinchonine on human platelet aggregation. The results show that cinchonine inhibited platelet aggregation mediated by platelet agonists, epinephrine (200 microM), ADP (4.3 microM), platelet activating factor (PAF 800 nM) and collagen (638 nM) but had no effect on arachidonic acid (AA 0.75 mM). Cinchonine was most effective in inhibiting aggregation induced by platelet activating factor and epinephrine with IC50 values of 125 and 180 microM respectively, however, higher concentrations of cinchonine were required to inhibit aggregation mediated by ADP or collagen (IC50 300 microM). Pretreatment of platelets with cinchonine inhibited aggregation caused by Ca2+ ionophore, A-23187 (6 microM), in a dose-dependent manner (IC50 300 microM) indicating an inhibitory effect on Ca2+-signaling cascade. This was supported by measuring [Ca2+]i in platelets loaded with Fura-2AM where cinchonine inhibited the rise in cytosolic Ca2+ mediated by A-23187 (6 microM) or collagen (638 nM). Results show that cinchonine (20 microM) also inhibited aggregation when platelets were pretreated with protein kinase C (PKC) activator, phorbol myristate acetate (PMA 0.1 microM) in combination with low doses of platelet activating factor (80 nM). Cinchonine, however, had no effect on AA-induced platelet aggregation and thromboxane A2 (TXA2) synthesis in platelets. These results suggest that antiplatelet effects of cinchonine are mediated mainly through inhibition of Ca2+-influx and protein kinase C pathways in platelets.
Publisher: Elsevier BV
Date: 06-1994
Publisher: Springer Science and Business Media LLC
Date: 30-11-2023
Publisher: Elsevier BV
Date: 10-2012
DOI: 10.1016/J.JEP.2012.08.039
Abstract: In the Greco-Arab (Unani) traditional medicine, Fumaria parviflora Linn. is widely used in hypreractive gut and respiratory disorders including diarrhea, abdominal cr s, indigestion and asthma but scientific studies to provide rational for these medicinal uses are sparse. This study was therefore undertaken to provide ethnopharmacological basis for its medicinal use in diarrhea, abdominal cr s and asthma. The in vivo studies were conducted in mice and rats while isolated gut and tracheal preparations of rat, guinea-pig and rabbit were suspended in respective tissue baths to measure the isotonic and isometric responses, using Power Lab electronic recorder. The aqueous-methanol extract of Fumaria parviflora (Fp.Cr) protected against diarrhea caused by castor oil in rats and mice, similar to loperamide and dicyclomine, and bronchospasm caused by carbachol (CCh) in rats, similar to aminophylline. In the in vitro studies, Fp.Cr relaxed CCh and isotonic high K(+) physiological salts solutions-induced contractions in jejunum, ileum and tracheal preparations of rat, guinea-pig and rabbit. Fp.Cr was predominately more potent against CCh than isotonic high K(+) solutions-induced contractions, similar to dicyclomine, suggesting the presence of anticholinergic and calcium channel blocking (CCB) activities, which were confirmed when Fp.Cr shifted the CCh and Ca(2+) concentration-response curves, constructed in rat ileum and trachea, towards right. Among intestinal preparations from various species, both anticholinergic and CCB effects of Fp.Cr were exhibited at lower concentrations in rat than the other species. In tracheal preparations, Fp.Cr was the most potent in its CCB effect in rabbit. Within species, CCB effect of Fp.Cr was produced at lower concentrations in rat jejunum than ileum and trachea, whereas, anticholinergic effect was produced at higher concentration in rat trachea than intestine. This study, showing the presence of antidiarrheal, antispasmodic and bronchodilator activities in Fumaria parviflora possibly mediated through dual blockade of muscarinic receptors and Ca(2+) channels, provides sound basis for its medicinal uses in diarrhea, abdominal cr s and may be used as bronchodilator in asthma. Species and tissue-dependency of these effects underscores the importance of utilizing multiple tissues and species to get more meaningful results.
Publisher: Informa UK Limited
Date: 25-04-2007
Publisher: Wiley
Date: 10-06-2010
DOI: 10.1002/JSFA.4021
Abstract: The aim of the present study was to appraise variation in the chemical composition, and antimicrobial and cytotoxic activities of essential oils from the leaves of four Mentha species-M. arvensis, M. piperita, M. longifolia and M. spicata-as affected by harvesting season. Disc diffusion and broth microdilution susceptibility assays were used to evaluate the antimicrobial activity of Mentha essential oils against a panel of microorganisms. The cytotoxicity of essential oils was tested on breast cancer (MCF-7) and prostate cancer (LNCaP) cell lines using the MTT assay. The essential oil contents of M. arvensis, M. piperita, M. longifolia and M. spicata were 17.0, 12.2, 10.8 and 12.0 g kg(-1) from the summer and 9.20, 10.5, 7.00 and 9.50 g kg(-1) from the winter crops, respectively. Gas chromatographic-mass spectrometric analysis revealed that mostly quantitative rather than qualitative variation was observed in the oil composition of each species. The principal chemical constituents determined in M. arvensis, M. piperita, M. longifolia and M. spicata essential oils from both seasons were menthol, menthone, piperitenone oxide and carvone, respectively. The tested essential oils and their major components exhibited notable antimicrobial activity against most of the plant and human pathogens tested. The tested essential oils also exhibited good cytotoxicity potential. Of the Mentha essential oils tested, M. arvensis essential oil showed relatively better antimicrobial and cytotoxic activities. A significant variation in the content of most of the chemical components and biological activities of seasonally collected s les was documented.
Publisher: Wiley
Date: 20-01-2011
DOI: 10.1002/PTR.3369
Abstract: Polygonatum verticillatum All. is used traditionally as an analgesic and plant diuretic. The methanol extract of aerial parts of Polygonatum verticillatum (PA) was assessed in various experimental paradigms. The pain threshold in the form of abdominal constriction induced by acetic acid was significantly (p < 0.01) inhibited by PA at test doses (50, 100 and 200 mg/kg). In the formalin test, PA elicited a significant (p < 0.01) analgesic activity in both phases and strongly attenuated the formalin-induced flinching behaviour. The hot plate test was used to evaluate central involvement in the analgesic profile of PA. The PA significantly relieved thermal-induced pain. From a mechanistic point of view, the central antihyperalgesic activity was tested for antagonism with naloxone, but no antagonism was observed. The current investigations suggest that the active constituent(s) in PA has an analgesic profile with predominant peripheral activity which is augmented by an opioid independent central effect. In the diuretic assay, PA (300 and 600 mg/kg) showed mild insignificant diuretic activity. Our study rationalized the traditional use of Polygonatum verticillatum in the treatment of painful conditions.
Publisher: Wiley
Date: 08-1995
Abstract: The influence of caffeine (60 mg) was studied on the pharmacokinetic characteristics of acetaminophen (500 mg single dose) in ten healthy male human volunteers in a complete cross-over design. A high-performance liquid chromatography (HPLC) method was used to analyse serum drug concentrations. Caffeine caused a highly significant (p < 0.01) increase in AUC and AUMC, a significant (p < 0.05) increase in Cmax, and a significant (p < 0.05) decrease in clearance (C1/F) of acetaminophen. We conclude that caffeine taken in doses commonly available commercially or in a cup of coffee can significantly potentiate the therapeutic potential of acetaminophen in man.
Publisher: Bangladesh Journals Online (JOL)
Date: 26-04-2014
Publisher: Science Alert
Date: 11-2014
Publisher: Wiley
Date: 13-10-2018
DOI: 10.1002/EHF2.12211
Publisher: Elsevier BV
Date: 12-2002
DOI: 10.1016/S0367-326X(02)00217-4
Abstract: Rutin, a well-known flavonoid was investigated for its possible protective effect against paracetamol- and CCl(4)-induced hepatic damage. Paracetamol produced 100% mortality at the dose of 1 g/kg in mice while pre-treatment of animals with rutin (20 mg/kg) reduced the death rate to 40%. Oral administration of a sub-lethal dose of paracetamol (640 mg/kg) produced liver damage in rats as manifested by the rise in serum level of transaminases (AST and ALT). Pre-treatment of rats with rutin (20 mg/kg) prevented the paracetamol-induced rise in serum enzymes. The hepatotoxic dose of CCl(4) (1.5 ml/kg orally) also raised the serum AST and ALT levels. The same dose of rutin (20 mg/kg) was able to prevent the CCl(4)-induced rise in serum enzymes. Rutin also prevented the CCl(4)-induced prolongation in pentobarbital sleeping time confirming its hepatoprotectivity. These results indicate that rutin possesses hepatoprotective activity and the presence of this compound in Artemisia scoparia may explain the folkloric use of the plant in liver damage.
Publisher: Wiley
Date: 1991
Publisher: Elsevier BV
Date: 2011
DOI: 10.1016/J.EJPHAR.2010.10.076
Abstract: Berberine is an isoquinoline alkaloid, occurring in nature as the main constituent of several plants with medicinal use in kidney stone disease. This work was undertaken to evaluate its antiurolithic potential and explore the possible underlying mechanism(s). Berberine was tested in vitro for the antioxidant effect and in vivo for diuretic and antiurolithic effects on an animal model of calcium oxalate urolithiasis. Berberine exhibited concentration-dependent (50-150μg/ml) antioxidant effect against ferrous-ascorbate induced lipid peroxidation in rat kidney homogenate with potency slightly higher than the reference antioxidant, butylated hydroxytoluene. In Wistar rats, berberine (5-20mg/kg) increased urine output accompanied by increased pH and Na(+) and K(+) excretion and decreased Ca(2+) excretion, similar to hydrochlorothiazide. In an animal model of calcium oxalate urolithiasis developed in male Wistar rats by adding 0.75% ethylene glycol in drinking water, berberine (10mg/kg) prevented as well as eliminated calcium oxalate crystal deposition in renal tubules and protected against deleterious effects of lithogenic treatment including weight loss, impaired renal function and oxidative stress, manifested as increased malondialdehyde and protein carbonyl contents, depleted GSH and decreased antioxidant enzyme activities of the kidneys. In naïve rats, berberine (10mg/kg) increased urine volume and pH and decreased Ca(2+) excretion. Results of this study suggest the presence of antiurolithic effects in berberine against calcium oxalate stones mediated through a combination of antioxidant, diuretic, urinary alkalinizing and hypocalciuric effects. These data invite future studies on berberine to establish its efficacy for clinical use.
Publisher: Wiley
Date: 17-06-2019
DOI: 10.1002/PTR.6411
Abstract: We have reported the antidyslipidemic, antihypertensive, and Ca
Publisher: Informa UK Limited
Date: 1992
Publisher: Wiley
Date: 28-07-2010
DOI: 10.1002/PTR.3263
Abstract: Mentha longifolia has a reputation in traditional medicine in the indications of diarrhoea and gut spasm. This study was carried out to provide a possible pharmacological basis for its medicinal use in hyperactive gut disorders. In a castor oil induced diarrhoeal model, the crude extract of Mentha longifolia (Ml.Cr), at doses of 100-1000 mg/kg, provided 31-80% protection, similar to loperamide. In isolated rabbit jejunum preparations, Ml.Cr caused inhibition of spontaneous and high K(+)-induced contractions, with respective EC50 values of 1.80 (1.34-2.24 n = 6-8) and 0.60 mg/mL (0.37-0.85 n = 6-8), which suggests spasmolytic activity, mediated possibly through calcium channel blockade (CCB). The CCB activity was further confirmed when pretreatment of the tissue with Ml.Cr (0.3-1 mg/mL) caused a rightward shift in the Ca(++) concentration-response curves (CRCs), similar to verapamil. Loperamide also inhibited spontaneous and high K(+)-induced contractions and shifted the Ca(++) CRCs to the right. Activity-directed fractionation revealed that the petroleum spirit fraction was more potent than the parent crude extract and aqueous fraction. These data indicate that the antidiarrhoeal and spasmolytic effects of the crude extract of Mentha longifolia are mediated through the presence of CCB-like constituent(s), concentrated in the petroleum spirit fraction and this study provides indirect evidence for its medicinal use in diarrhoea and spasm.
Publisher: Elsevier BV
Date: 02-2006
DOI: 10.1016/J.FITOTE.2005.11.013
Abstract: Seeds of Butea monosperma administered as crude powder (CP) at doses of 1, 2 and 3 g/kg to sheep naturally infected with mixed species of gastrointestinal nematodes exhibited a dose and a time-dependent anthelmintic effect. The maximum reduction of 78.4% in eggs per gram of feces (EPG) was recorded on day 10 after treatment with 3 g/kg. Levamisole (7.5 mg/kg), a standard anthelmintic agent, exhibited 99.1% reduction in EPG.
Publisher: Wiley
Date: 07-1993
Publisher: Oxford University Press (OUP)
Date: 10-2008
Abstract: Ginger rhizome (Zingiber officinale) has been used for centuries to treat dementia in South Asia. This study was undertaken to possibly justify its use. A 70% aqueous/methanolic extract of dried ginger (Zo.Cr) was used. Zo.Cr tested positive for the presence of terpenoids, flavonoids, secondary amines, phenols, alkaloids and saponins. When tested on isolated rat stomach fundus, Zo.Cr showed a spasmogenic effect (0.03-5.00 mg mL(-1)) it relaxed the tissue at concentrations > or =5 mg mL(-1). The stimulant effect was resistant to blockade by hexamethonium and methysergide, but sensitive to atropine, indicating activity via muscarinic receptors. In atropinized (0.1 microM) preparations, Zo.Cr (0.3-3.0 mg mL(-1)) relaxed high K(+) (80 mM)-induced contractions, indicating Ca(++) antagonism in addition to the muscarinic effect. This possible Ca(++) antagonist activity was investigated in Ca(++)-free conditions, with the inhibitory effect of the extract tested against contractions induced by externally administered Ca(++). Zo.Cr (0.1-0.3 mg mL(-1)), similar to verapamil (0.03-0.10 microM), shifted the contractions induced by externally administered Ca(++) to the right, thus suggesting an inhibitory interaction between Zo.Cr and voltage-operated Ca(++) channels. Zo.Cr (0.1-3.0 microg mL(-1)) also potentiated acetylcholine peak responses in stomach fundus, similar to physostigmine, a cholinesterase inhibitor. Zo.Cr, in an in-vitro assay, showed specific inhibition of butyrylcholinesterase (BuChE) rather than acetylcholinesterase enzyme. Different pure compounds of ginger also showed spasmolytic activity in stomach fundus, with 6-gingerol being the most potent. 6-Gingerol also showed a specific anti-BuChE effect. This study shows a unique combination of muscarinic, possible Ca(++) antagonist and BuChE inhibitory activities of dried ginger, indicating its benefit in dementia, including Alzheimer's disease.
Publisher: Elsevier BV
Date: 07-2013
Publisher: Pharmaceutical Society of Japan
Date: 2007
DOI: 10.1248/JHS.53.151
Publisher: Bangladesh Journals Online (JOL)
Date: 10-06-2011
Publisher: Informa UK Limited
Date: 2006
DOI: 10.1080/09637480600656074
Abstract: This study describes the prokinetic actions of the aqueous extract of ginger (Zingiber officinale). Ginger extract (Zo.Cr), which tested positive for saponins, terpenes, phenols, flavonoids and alkaloids, showed a spasmogenic effect in isolated guinea-pig ileum with 8-50 times more potency than in rabbit jejunum and ileum and rat stomach fundus and ileum. Spasmogenicity in all the gut preparations except in guinea-pig ileum was atropine-sensitive. Zo.Cr exhibited a stimulant effect in vivo in mice and enhanced the intestinal transit of charcoal meal. A spasmolytic effect, mediated via Ca2 + antagonist activity, was also exhibited by Zo.Cr, reflected in terms of inhibition of spontaneous contractions, K+ (80 mM)-induced contractions and displacement of Ca2 + dose-response curves. The ginger pure compounds (6-shogaol, 6-gingerol, 8-gingerol and 10-gingerol) also exhibited a spasmolytic activity, which reduced with the increasing size of the side chain in their chemical structures. The study showed that the aqueous extract of ginger exhibits species-specific spasmogenicity in gut tissues of rabbit and rat (muscarinic-type) while through an uncharacterized pathway in guinea-pig ileum, along with a dormant relaxant effect, mediated via the blockade of voltage-dependent Ca2 + channels.
Publisher: Elsevier BV
Date: 08-2021
Publisher: Elsevier BV
Date: 07-2004
DOI: 10.1016/J.PHYMED.2003.05.002
Abstract: Caffeic acid and quercetin, the well-known phenolic compounds widely present in the plant kingdom, were investigated for their possible protective effects against paracetamol and CCl4-induced hepatic damage. Paracetamol at the oral dose of 1 g/kg produced 100% mortality in mice while pretreatment of separate groups of animals with caffeic acid (6 mg/kg) and quercetin (10 mg/kg) reduced the death rate to 20% and 30%, respectively. Oral administration of sub-lethal dose of paracetamol (640 mg/kg) produced liver damage in rats as manifested by the significant (P<0.01) rise in serum levels of aminotransferases (aspartate transaminase (AST) and alanine transaminase (ALT)) compared to respective control values. The serum enzyme values were significantly (P<0.01) lowered on pretreatment of rats with either caffeic acid (6 mg/kg) or quercetin (10 mg/kg). Similarly, the hepatotoxic dose of CCl4 (1.5 ml/kg orally) also raised significantly (P<0.05) the serum AST and ALT levels as compared to control values. The same dose of the caffeic acid and quercetin was able to prevent CCl4-induced rise in serum enzymes. Caffeic acid and quercetin also prevented the CCl4-induced prolongation in pentobarbital sleeping time confirming their hepatoprotectivity. These results indicate that caffeic acid and quercetin exhibited hepatoprotective activity possibly through multiple mechanisms.
Publisher: Springer Science and Business Media LLC
Date: 25-02-2016
Publisher: Springer Science and Business Media LLC
Date: 12-2016
Publisher: Wiley
Date: 03-1994
Publisher: Wiley
Date: 09-07-2019
DOI: 10.1002/PTR.6423
Abstract: The genus Mentha comprises several aromatic species, which are cultivated world-over due to their distinct aroma and commercial value. In addition to traditional food flavoring uses, Mentha are well recognized for their folk medicinal uses, especially to treat cold, fever, and digestive and cardiovascular disorders. A number of biological activities such as antioxidant, antimicrobial, biopesticidal, antitumor, anticancer, antiviral, antiallergic, antiinflammatory, antihypertensive, and urease inhibitory activity have been ascribed to Mentha. The traditional pharmacological attributes of Mentha herbs can be linked to the occurrence of bioactive phytochemicals such as terpenoids, alcohols, rosmarinic acid, and antioxidant phenolics among others. A rich source of bioactives, different species of Mentha, can be explored as a promising candidate for the development of nutra-pharmaceuticals. This review covers the nutritional, phytochemical, and traditional medicinal aspects and multiple biological activities of some commonly available species of Mentha so as to explore their potential applications for nutra-pharmaceutical and cosmo-nutraceutical industry. Detailed chemical profile and pharmaceutical attributes of various Mentha essential oils are also covered. Moreover, based on computational analysis, quantitative chemical component-antioxidant activity relationship model is reviewed to predict and correlate structure-activity relationship of potential bioactives in selected Mentha essential oils leading to discovery and developmenmt of novel natural drugs.
Publisher: Walter de Gruyter GmbH
Date: 11-01-2012
Publisher: Portland Press Ltd.
Date: 11-1993
DOI: 10.1042/BST021461S
Publisher: Springer Science and Business Media LLC
Date: 06-1994
DOI: 10.1007/BF02974250
Publisher: Elsevier BV
Date: 04-2005
DOI: 10.1016/J.JEP.2005.01.017
Abstract: This study describes the antihypertensive, antispasmodic, bronchodilator and hepatoprotective activities of the aqueous-methanolic extract of Carum copticum Benth. seeds (CSE) to rationalize some of its traditional uses. CSE (3-100 mg/kg) caused a dose-dependent fall in arterial blood pressure in anaesthetized rats. In isolated rabbit aorta and jejunum preparations, CSE (0.1-3.0 mg/ml) caused an inhibitory effect on the K+-induced contractions. The calcium channel blocking (CCB) effect was confirmed when CSE shifted the Ca2+ dose-response curves (DRCs) to right similar to verapamil. In isolated guinea-pig tracheal preparations, it caused inhibition of carbachol and K+-induced bronchoconstriction at 0.1-1.0 mg/ml as well as shifted the dose-response curves (DRCs) of carbachol and histamine to the right with suppression of maximum response suggestive of non-specific bronchodilator effect mediated possibly through CCB. Pretreatment of rats with CSE (500 mg/kg orally for 2 days at 12 h intervals) prevented paracetamol (640 mg/kg) and CCl4 (150 ml/kg)-induced rise in serum alkaline phosphatase (ALP) and aminotransferases (AST and ALT). The same dose of CSE was able to prevent the CCl4-induced prolongation in pentobarbital-induced sleeping time in mice confirming its hepatoprotectivity. These results indicate the presence of calcium antagonist(s) in Carum copticum seeds and thus provides sound mechanistic basis for some of their folkloric uses.
Publisher: Informa UK Limited
Date: 12-08-2016
Publisher: AME Publishing Company
Date: 02-2022
DOI: 10.21037/CDT-21-518
Publisher: American Chemical Society (ACS)
Date: 26-10-2002
DOI: 10.1021/NP020127X
Abstract: A new triterpenoid acid named eucalyptanoic acid (1) has been isolated from the fresh uncrushed leaves of Eucalyptus camaldulensis var. obtusa along with two known constituents, beta-sitosterol (2) and betulinic acid (3). The structure of 1 has been established as 3beta-hydroxyolean-9(11),12-dien-28-oic acid through spectral studies including 1D and 2D NMR. 1 and its acetyl (1a) and acetylmethyl (1b) derivatives were tested for spasmolytic activity. 1b was found to be the most active spasmolytic, mediated through blockade of calcium influx at 1 mg/mL. In the present study 1b was also prepared starting from oleanolic acid (4). Acetylation of 4 gave 4a, which on methylation afforded 4b. Reaction of 4b with N-bromosuccinimide (NBS) furnished 1b. Hence 4 may be regarded as the biogenetic precursor of 1. Compounds 4 and 4a were found inactive at 1 mg/mL, while 4b was moderately active in showing spasmolytic activity.
Publisher: Portland Press Ltd.
Date: 10-1989
DOI: 10.1042/BST0170902
Publisher: Elsevier BV
Date: 11-2020
Publisher: Bentham Science Publishers Ltd.
Date: 26-10-2020
DOI: 10.2174/1381612826666200806095649
Abstract: Nuts hold prime significance throughout the world as they offer multiple health benefits owing to their highly nutritious profile. A number of scientific studies have demonstrated their actions against inflammation, oxidative damage, the aging process, as well as dementia or memory loss. However, only walnuts, followed by almonds, hazelnuts and pistachios, have shown promising results in empirical studies for memory improvements. So, the current review focuses on presenting hypotheses regarding anti-dementia property of nine different nuts: almond, walnut, pistachio, Brazil nut, peanut, pecans, cashew, hazelnut, and chestnut. The nutritious profile of nuts contains essential fats (mostly mono- and poly-unsaturated fatty acids), proteins (source for arginine, lysine and tryptophan), vitamins (riboflavin, folate, and various tocopherols), fibers, minerals (calcium, sodium, magnesium, phosphorus and potassium) and trace elements (copper, zinc, and selenium). Interestingly, the constituents of natural products, nuts being an excellent ex le, work synergistically and/or in a side-effect neutralizing manner. These latter properties can make nuts an alternate therapy for humankind to fight against memory loss.
Publisher: Elsevier BV
Date: 12-2004
DOI: 10.1016/J.JEP.2004.06.038
Abstract: The crude extract of Raphanus sativus leaves (Rl.Cr) showed a dose-dependent (0.03-5.0 mg/ml) spasmogenicity in guinea-pig ileum and colon. The effect was insensitive to atropine pre-treatment but was completely abolished by pyrilamine indicating involvement of histaminergic (H(1)) receptors. The contractile effect at high doses (3.0-5.0mg/ml) was followed by relaxation. Rl.Cr also enhanced the transit of charcoal meal in mice at 30-100 mg/kg. The petroleum spirit, chloroform and aqueous fractions all showed histaminergic activity in ileum aqueous fraction being more potent. The study shows the presence of a histaminergic component(s) along with a weak spasmolytic factor thus providing sound mechanistic basis for the traditional use of the plant in constipation.
Publisher: Elsevier
Date: 2016
Publisher: Oxford University Press (OUP)
Date: 11-2005
Abstract: This study describes the gastrointestinal (GI) prokinetic effects of the aqueous extract of radish seeds (Rs.Cr). Rs.Cr, which tested positive for terpenes, flavonoids, phenols, alkaloids and saponins, showed a spasmogenic effect in isolated rabbit jejunum and ileum, rat stomach fundus and ileum, and guinea-pig ileum and jejunum. Rs.Cr was around 10 times more potent in the guinea-pig tissues and this effect was resistant to atropine, pyrilamine or SB203186 while the spasmogenic effect in the rat and rabbit tissues was atropine sensitive. The extract exhibited atropine-sensitive GI prokinetic and laxative effects in vivo in mice. In the atropinized rabbit jejunum, Rs.Cr produced a spasmolytic effect independent of Ca++ or K+ channels, adrenergic or opioid receptor involvement. Activity-directed fractionation of Rs.Cr yielded four fractions, all showing effects similar to that of the parent extract. Rs.Cr and its fractions were found to be non-lethal up to 10 g kg−1 in mice for 24 h, except for the petroleum fraction, which showed 50% mortality at high doses. Some known radish compounds (spermine, spermidine, putrescine and sinigrin) were also tested and found to be devoid of any activity. The study shows species-specific spasmogenic effects of radish in rabbit, rat and mouse via muscarinic receptors but through an uncharacterized pathway in guinea-pig tissues. Additionally, a dormant relaxant effect was also seen, while the three polyamines and one glucosinolate from radish were found to be inactive, indicating that the compound(s) responsible for the activities reported remains to be isolated.
Publisher: Elsevier BV
Date: 11-2014
Publisher: Wiley
Date: 18-11-2005
DOI: 10.1111/J.1472-8206.2005.00378.X
Abstract: The crude extract of aerial parts of St John's wort (Hypericum perforatum) (Hp.Cr) and its fractions were studied in vitro for its possible spasmolytic and bronchodilator activities to rationalize some of its medicinal uses. In rabbit jejunum preparations, Hp.Cr caused a concentration-dependent relaxation of both spontaneous and K+ (80 mm)-induced contractions at a similar concentration range (0.1-1.0 mg/mL), similar to that produced by papaverine, whereas verapamil was relatively potent against K+-induced contractions. Hp.Cr shifted the Ca2+ concentration-response curves (CRCs) to the right, similar to that caused by papaverine or verapamil and also caused leftward shift of isoprenaline-induced inhibitory CRCs, similar to papaverine. In guinea-pig tracheal preparations, Hp.Cr caused relaxation of carbachol and K+-induced contractions at similar concentrations (0.01-0.3 mg/mL) and also shifted the isoprenaline-induced inhibitory CRCs to the left, similar to that caused by papaverine. In rabbit aorta preparations at rest, Hp.Cr produced a moderate vasoconstriction, while exhibited vasodilator effect against phenylephrine and K+-induced contractions. Papaverine and verapamil also produced similar non-specific vasodilation, but were devoid of any vasoconstrictor effect. Hp.Cr caused suppression of atrial force of contractions at concentrations about 20 times higher than those that produced inhibitory effect in smooth muscle preparations, similar to papaverine. These results suggest that the spasmolytic effects of Hp.Cr are mediated through dual inhibition of calcium influx and phosphodiesterase (PDE)-like mechanisms, which might explain the medicinal use of St John's wort in the disorders of gastrointestinal and respiratory tracts. Furthermore, the presence of Ca2+ antagonist and PDE inhibitory-like constituents might also be contributing to some extent in the well established use of plant in depression.
Publisher: Wiley
Date: 03-1994
Publisher: MDPI AG
Date: 10-07-2023
DOI: 10.3390/JCM12144595
Abstract: The universal definition of acute myocardial infarction (MI) requires both evidence of myocardial injury and myocardial ischaemia. In MINOCA (MI with non-obstructive coronary arteries), patients must fulfil this MI criteria, but is their chest pain similar to those who have MI with obstructive CAD (MICAD)? This study compares prospectively collected chest pain features between patients with MINOCA and MICAD. Utilising the Coronary Angiogram Database of South Australia (CADOSA), consecutive MI patients were categorized as MINOCA or MICAD based on angiographic findings. Chest pain data were collected via direct patient interviews by trained staff members. Of 6811 consecutive patients fulfilling a clinical MI diagnosis, 411 (6.0%) were MINOCA, and 5948 MICAD. The MINOCA patients were younger, more often female and had less cardiovascular risk factors than those with MICAD. There were no significant differences in chest pain characteristics between the MINOCA and MICAD cohorts in relation to pain location, quality, associated symptoms, or duration. In conclusion, MINOCA patients have chest pain characteristics that are indistinguishable from MICAD patients, suggesting that their pain is ischaemic in nature. Thus, in the presence of positive myocardial injury markers, ischaemic chest pain fulfils the universal criteria for MI, despite the absence of obstructive coronary artery disease.
Publisher: Wiley
Date: 12-1999
DOI: 10.1002/(SICI)1099-1573(199912)13:8<665::AID-PTR563>3.0.CO;2-T
Abstract: A methanol extract of Acacia nilotica pods (AN) caused a dose-dependent (3-30 mg/kg) fall in arterial blood pressure. Treatment of animals with atropine abolished the vasodilator response of acetylcholine (ACh), whereas the antihypertensive effect of the plant extract remained unaltered. Phentolamine (an alpha-adrenergic blocker) abolished the vasoconstrictor effect of norepinephrine (NE), whereas pretreatment of the animal with AN, did not modify the NE response. These results indicate that the antihypertensive effect of plant extract is independent of muscarinic receptor stimulation or adrenoceptor blockade. In the in vitro studies, AN produced a dose-dependent (0.3-3.0 mg/mL) inhibitory effect on force and rate of spontaneous contractions in guinea-pig paired atria. Similarly, it inhibited the spontaneous contraction of rabbit jejunum in a concentration-dependent (0.1-3.0 mg/mL) manner. AN also inhibited K(+)-induced contractions in rabbit jejunum at a similar concentration range, which suggests that the antispasmodic action of AN is mediated through calcium channel blockade, and this may also be responsible for the blood pressure lowering effect of AN, observed in the in vivo studies.
Publisher: Elsevier BV
Date: 12-2009
DOI: 10.1016/J.JEP.2009.09.010
Abstract: The present study describes antispasmodic, antidiarrheal, bronchodilatory and tracheo-relaxant activities of Artemisia vulgaris to rationalize some of its traditional uses. Crude extract of Artemisia vulgaris (Av.Cr) was studied in the isolated tissue preparations of rabbit jejunum and guinea-pig trachea, as well as in the in vivo castor oil-induced diarrhea and bronchodilatory techniques. Av.Cr which tested positive for alkaloids, coumarins, flavonoids, saponins, sterols, tannins and terpenes caused concentration-dependent (0.03-10mg/mL) relaxation of jejunum spontaneous contractions. Av.Cr inhibited the carbachol (CCh, 1 microM) and K(+) (80 mM)-induced contractions in a pattern, similar to that of dicyclomine. Av.Cr shifted the Ca(2+) concentration-response curves to right, like that caused by verapamil and dicyclomine. Av.Cr produced rightward parallel shift in CCh-curves, followed by non-parallel shift at higher concentration with the suppression of the maximum response, similar to that caused by dicyclomine. It exhibited protective effect against castor oil-induced diarrhea and CCh-mediated bronchoconstriction in rodents. In trachea, Av.Cr relaxed the CCh (1 microM) and K(+) (80 mM)-induced contractions and shifted the CCh-curves to right. These results indicate that Artemisia vulgaris exhibits combination of anticholinergic and Ca(2+) antagonist mechanisms, which provides pharmacological basis for its folkloric use in the hyperactive gut and airways disorders, such as abdominal colic, diarrhea and asthma.
Publisher: American Chemical Society (ACS)
Date: 09-1994
DOI: 10.1021/NP50111A011
Abstract: Bioassay-guided analysis of an EtOH extract of Moringa oleifera leaves showing hypotensive activity led to the isolation of two nitrile glycosides, niazirin [1] and niazirinin [2], and three mustard oil glycosides, 4-[(4'-O-acetyl-alpha-L-rhamnosyloxy)benzyl]isothiocyanate [4], niaziminin A, and niaziminin B. Glycoside 2 is a new compound. Niaziminins A and B have previously been obtained from the left extract as a mixture, while compound 4 is new from this source. Structural determination was accomplished by means of spectroscopic methods including appropriate 2D nmr experiments and chemical reactions. This is the first report of the isolation of nitriles, an isothiocyanate, and thiocarbamates from the same plant species. Isothiocyanate 4 and the thiocarbamate glycosides niaziminin A and B showed hypotensive activity while nitrile glycosides 1 and 2 were found to be inactive in this regard.
Publisher: Springer Science and Business Media LLC
Date: 21-11-2022
DOI: 10.1186/S12905-022-02035-Y
Abstract: Pregnancy complications affect over one quarter of Australian pregnancies, and this group of mothers is vulnerable and more likely to experience adverse cardiometabolic health outcomes in the postpartum period. Metabolic syndrome is common in this population and may be associated with postpartum mental health issues. However, this relationship remains poorly understood. To compare the differences in psychosocial parameters and mental health outcomes between women with metabolic syndrome and women without metabolic syndrome 6 months after a complicated pregnancy. This study is prospective registry analysis of women attending a postpartum healthy lifestyle clinic 6 months following a complicated pregnancy. Mental health measures included 9-item Patient Health Questionnaire (PHQ-9), 7-item Generalised Anxiety Disorder questionnaire (GAD-7), self-reported diagnosed history of depression, anxiety and/or other psychiatric condition, and current psychotropic medication use. Women with metabolic syndrome reported significantly more subjective mental health concerns, were more likely to have a history of depression and other psychiatric diagnoses and were more likely prescribed psychotropic medications. However, there were no significant differences in PHQ-9 and GAD-7 scores. Amongst new mothers who experienced complications of pregnancy, those with metabolic syndrome represent a particularly vulnerable group with regards to psychosocial disadvantage and mental health outcomes. These vulnerabilities may not be apparent when using common standardised cross-sectional mental health screening tools such as PHQ-9 and GAD-7.
Publisher: Informa UK Limited
Date: 12-06-2009
Publisher: Springer Science and Business Media LLC
Date: 17-11-2010
DOI: 10.1007/S10620-010-1466-0
Abstract: The objective of this study was to determine the pharmacological basis of the medicinal use of psyllium husk (Ispaghula) in gastrointestinal motility disorders. In-vivo studies were conducted on mice, and isolated rabbit jejunum and guinea-pig ileum were used in in-vitro experiments. The crude extract of Ispaghula (Po.Cr) had a laxative effect in mice at 100 and 300 mg/kg, which was partially sensitive to atropine or SB203186 (5-HT(4) antagonist). At higher doses (500 and 1,000 mg/kg), Po.Cr had antisecretory and antidiarrheal activity. In guinea-pig ileum, Po.Cr (1-10 mg/ml) had a stimulatory effect, which was partially sensitive to atropine or SB203186. In rabbit jejunum, Po.Cr had a partially atropine-sensitive stimulatory effect followed by relaxation at 10 mg/ml. The relaxation was inhibited by the presence of L-NAME, a nitric oxide (NO) synthase inhibitor, or methylene blue, a guanylyl cyclase inhibitor. Similarly, the relaxant effect of Po.Cr on K(+) (80 mM)-induced contractions, was attenuated in the presence of L-NAME or methylene blue. Activity-directed fractionation of Po.Cr revealed that the gut stimulatory and inhibitory constituents were widely distributed in the aqueous and organic fractions. This study demonstrates that Ispaghula has a gut-stimulatory effect, mediated partially by muscarinic and 5-HT(4) receptor activation, which may complement the laxative effect of its fiber content, and a gut-inhibitory activity possibly mediated by blockade of Ca(2+) channels and activation of NO-cyclic guanosine monophosphate pathways. This may explain its medicinal use in diarrhea. It is, perhaps, also intended by nature to offset an excessive stimulant effect.
Publisher: Elsevier BV
Date: 05-1995
DOI: 10.1016/0306-3623(94)00200-7
Abstract: 1. The hepatoprotective activity of aqueous-methanolic extract of Cyperus scariosus (Cyperaceae) was investigated against acetaminophen and CCl4-induced hepatic damage. 2. Acetaminophen produced 100% mortality at a dose of 1 g/kg in mice while pretreatment of animals with plant extract (500 mg/kg) reduced the death rate to 30%. 3. Acetaminophen at a dose of 640 mg/kg produced liver damage in rats as manifested by the rise in serum levels of alkaline phosphatase (ALP), glutamate oxaloacetate transaminase (GOT) and glutamate pyruvate transaminase (GPT) to 430 +/- 68, 867 +/- 305 and 732 +/- 212 IU/l (n = 10) respectively, compared to respective control values of 202 +/- 36, 59 +/- 14 and 38 +/- 7. 4. Pretreatment of rats with plant extract (500 mg/kg) significantly lowered (P < 0.05) the respective serum ALP GOT and GPT levels to 192 +/- 31, 63 +/- 9 and 35 +/- 8. 5. The hepatotoxic dose of CCl4 (1.5 ml/kg orally) raised serum ALP, GOT and GPT levels to 328 +/- 30, 493 +/- 102 and 357 +/- 109 IU/l (n = 10) respectively, compared to respective control values of 177 +/- 21, 106 +/- 15 and 47 +/- 12. 6. The same dose of plant extract (500 mg/kg) was able to significantly prevent (P < 0.05) CCl4-induced rise in serum enzymes and the estimated values of ALP, GOT and GPT were 220 +/- 30, 207 +/- 95 and 75 +/- 38, respectively. 7. The plant extract also prevented CCl4-induced prolongation in pentobarbital sleeping time confirming hepatoprotectivity.(ABSTRACT TRUNCATED AT 250 WORDS)
Publisher: Wiley
Date: 15-12-2011
DOI: 10.1002/PTR.3687
Publisher: Royal Society of Chemistry (RSC)
Date: 1992
DOI: 10.1039/P19920003237
Publisher: Wiley
Date: 2003
DOI: 10.1002/PTR.1146
Abstract: The effect of an aqueous extract of Nigella sativa seeds was studied on candidiasis in mice. An intravenous inoculum of Candida albicans produced colonies of the organism in the liver, spleen and kidneys. Treatment of mice with the plant extract (6.6 mL/kg equivalent to 5 mg of estimated protein, once daily for 3 days) 24 h after the inoculation caused a considerable inhibitory effect on the growth of the organism in all organs studied. A 5-fold decrease in Candida in kidneys, 8-fold in liver and 11-fold in spleen was observed in the groups of animals post-treated with the plant extract. Histopathological examination of the respective organs confirmed these findings. These results indicate that the aqueous extract of Nigella sativa seeds exhibits inhibitory effect against candidiasis and this study validates the traditional use of the plant in fungal infections.
Publisher: Wiley
Date: 19-12-2013
DOI: 10.1002/PTR.4897
Abstract: Coriander (Coriandrum sativum L.), a herbal plant, belonging to the family Apiceae, is valued for its culinary and medicinal uses. All parts of this herb are in use as flavoring agent and/or as traditional remedies for the treatment of different disorders in the folk medicine systems of different civilizations. The plant is a potential source of lipids (rich in petroselinic acid) and an essential oil (high in linalool) isolated from the seeds and the aerial parts. Due to the presence of a multitude of bioactives, a wide array of pharmacological activities have been ascribed to different parts of this herb, which include anti-microbial, anti-oxidant, anti-diabetic, anxiolytic, anti-epileptic, anti-depressant, anti-mutagenic, anti-inflammatory, anti-dyslipidemic, anti-hypertensive, neuro-protective and diuretic. Interestingly, coriander also possessed lead-detoxifying potential. This review focuses on the medicinal uses, detailed phytochemistry, and the biological activities of this valuable herb to explore its potential uses as a functional food for the nutraceutical industry.
Publisher: Springer Science and Business Media LLC
Date: 18-03-2015
Publisher: Wiley
Date: 2006
DOI: 10.1002/PTR.2000
Abstract: Acorus calamus Linn. (Araceae) is a native of Central Asia and Eastern Europe and has widespread use in the traditional system of medicine for gastrointestinal disorders such as colic pain and diarrhoea. This study was aimed at providing a possible pharmacological basis to the use of this plant as an antispasmodic and antidiarrhoeal. In the isolated rabbit jejunum preparation the crude extract (Ac.Cr), which tested positive for the presence of alkaloid, saponins and tannins, caused inhibition of spontaneous and high K(+) (80 mm)-induced contractions, with respective EC(50) values of 0.42 +/- 0.06 and 0.13 +/- 0.04 mg/mL (mean +/- SEM n = 6-8), thus showing spasmolytic activity, mediated possibly through calcium channel blockade (CCB). The CCB activity was confirmed when pre-treatment of the tissue with Ac.Cr (0.3-1.0 mg/mL) caused a rightward shift in the Ca(++) dose-response curves similar to that caused by verapamil, a standard calcium channel blocker. Activity-directed fractionation revealed that the CCB activity was concentrated in the n-hexane fraction while the ethylacetate fraction was less potent. These results suggest that the spasmolytic effect of the plant extract is mediated through the presence of CCB-like constituent(s) which is concentrated in the n-hexane fraction and this study provides a strong mechanistic base for its traditional use in gastrointestinal disorders such as colic pain and diarrhoea.
Publisher: Springer Science and Business Media LLC
Date: 09-08-2011
DOI: 10.1007/S11418-011-0561-7
Abstract: This investigation was aimed to probe the pharmacological base of medicinal use of Acorus calamus in ischemic heart diseases. Effect on heart parameters was studied in isolated rabbit heart while coronary vasodilator effect was studied in isolated bovine coronary arterial rings, suspended in tissue baths filled with Krebs solution, maintained at 37°C, aerated with carbogen and responses were measured on PowerLab data acquisition system. In Langendorrf's perfused rabbit heart, the crude extract of Acorus calamus (Ac.Cr) at 0.01-10 mg/mL partially suppressed force of ventricular contractions (FVC), heart rate (HR) and coronary flow (CF). The ethylacetate fraction completely suppressed FVC, partially suppressed HR and CF, while the nHexane fraction exhibited similar effect on FVC and HR but increased CF, similar to methacholine and arachidonic acid. In bovine coronary arterial preparations, Ac.Cr caused inhibition of U46619 (20 nM)-precontractions, which was blocked in presence of increasing concentration of K(+) (4.8-20 mM), tetraethylammonium (1 μM) and SKF525A (10 μM), similar to arachidonic acid and methacholine, indicating K(+) channels activation and possible involvement of endothelial-derived hyperpolarizing factor (EDHF). Activity-directed fractionation revealed that EDHF-mediated activity is concentrated in the nHexane fraction. When tested against high K(+), the ethylacetate fraction was found more potent than parent crude extract and nHexane fraction. These data indicate that Ac.Cr mediates coronary vasodilator effect primarily through EDHF, responsible for the increase in CF, while the cardiac depressant effects may be due to the presence of additional cardiac depressant constituent(s), thus provides possible mechanistic basis to its medicinal use in ischemic heart diseases.
Publisher: Wiley
Date: 14-05-2020
DOI: 10.1111/MICC.12622
Publisher: Ovid Technologies (Wolters Kluwer Health)
Date: 19-02-1999
Abstract: Abstract —The clinical efficacy of anthracycline antineoplastic agents is limited by a high incidence of severe and usually irreversible cardiac toxicity, the cause of which remains controversial. In primary cultures of neonatal and adult rat ventricular myocytes, we found that daunorubicin, at concentrations ≤1 μmol/L, induced myocyte programmed cell death within 24 hours, as defined by several complementary techniques. In contrast, daunorubicin concentrations ≥10 μmol/L induced necrotic cell death within 24 hours, with no changes characteristic of apoptosis. To determine whether reactive oxygen species play a role in daunorubicin-mediated apoptosis, we monitored the generation of hydrogen peroxide with dichlorofluorescein (DCF). However, daunorubicin (1 μmol/L) did not increase DCF fluorescence, nor were the antioxidants N -acetylcysteine or the combination of α-tocopherol and ascorbic acid able to prevent apoptosis. In contrast, dexrazoxane (10 μmol/L), known clinically to limit anthracycline cardiac toxicity, prevented daunorubicin-induced myocyte apoptosis, but not necrosis induced by higher anthracycline concentrations (≥10 μmol/L). The antiapoptotic action of dexrazoxane was mimicked by the superoxide-dismutase mimetic porphyrin manganese(II/III)tetrakis(1-methyl-4-peridyl)porphyrin (50 μmol/L). The recognition that anthracycline-induced cardiac myocyte apoptosis, perhaps mediated by superoxide anion generation, occurs at concentrations well below those that result in myocyte necrosis, may aid in the design of new therapeutic strategies to limit the toxicity of these drugs.
Publisher: Public Library of Science (PLoS)
Date: 03-11-2016
Publisher: Informa UK Limited
Date: 02-2011
DOI: 10.1080/14786419.2010.529445
Abstract: Caesalpinia bonducella F. (Leguminosae) has been used as a folk medicine for a variety of ailments. The crude extract of C. bonducella and its fractions were studied for antibacterial, antifungal, antispasmodic and Ca++ antagonistic properties. The strongest antibacterial effect was displayed by the n-butanol (72%) and ethyl acetate (80%) fractions, followed by the crude extract (46% and 42%), against Escherichia coli and Bacillus subtilis, respectively. The plant extract and its fractions showed mild to excellent activity in antifungal bioassays, with maximum antifungal activity against Candida glaberata (80%) and Aspergillus flavus (70%) by the n-butanol and chloroform fractions, followed by the crude extract (70% and 65%). Caesalpinia bonducella extract caused concentration-dependent inhibition of spontaneous and high K+ (80 mM)-induced contractions of isolated rabbit jejunum preparations, similar to that caused by Verapamil. These results indicate that C. bonducella exhibits antibacterial, antifungal, spasmolytic and Ca++ channel blocking actions.
Publisher: Elsevier BV
Date: 05-2023
Publisher: Elsevier BV
Date: 11-2005
DOI: 10.1016/J.JEP.2005.07.023
Abstract: The aqueous-ethanolic extract of the aerial parts of Hibiscus rosasinensis Linn. (Malvaceae) was studied for the possible presence of spasmogenic and spasmolytic constituents to rationalize its traditional use in gastrointestinal disorders. The crude extract (Hr.Cr) caused a concentration-dependent (1-10mg/mL) spasmogenic effect in isolated guinea-pig ileum, which was blocked in the presence of atropine (0.1 microM). In spontaneously contracting rabbit jejunum, the plant extract exhibited a weak stimulatory effect at lower doses (0.03-0.30 mg/mL) followed by an inhibitory effect at higher doses (1.0-3.0mg/mL). Pretreatment of the tissues with atropine blocked the stimulatory effect resulting in the potentiation of the spasmolytic effect. Hr.Cr (0.03-1.0mg/mL) also showed an inhibitory effect on K(+) (80 mM)-induced contractions. The calcium channel blocking activity was confirmed when Hr.Cr shifted the Ca(2+) concentration-response curves to the right, similar to verapamil. Activity-directed fractionation revealed that the spasmolytic component(s) was separated in the ethyl acetate, while the spasmogenic in the petroleum ether fraction. The aqueous fraction exhibited a combination of weak spasmogenic and spasmolytic effects. These data indicate that the crude extract contains spasmogenic and spasmolytic constituents mediating their effect through cholinergic receptors activation and blockade of Ca(2+) influx, respectively, which may explain its traditional use in constipation and diarrhoea.
Publisher: Wiley
Date: 05-1994
Publisher: Wiley
Date: 05-1994
Publisher: Wiley
Date: 27-05-2016
DOI: 10.1002/PTR.5641
Abstract: Morus nigra Linn. (black mulberry) is used in gastrointestinal ailments. This study demonstrates gut modulatory properties of M. nigra. The prokinetic, laxative, and antidiarrheal activities of M. nigra were assessed in mice, while isolated rabbit jejunum and guinea-pig ileum were used to explore insight into mechanism(s). At 30 and 70 mg/kg, the crude extract of M. nigra (Mn.Cr) exhibited atropine-sensitive prokinetic and laxative effects, similar to carbachol (CCh). While at higher doses (100, 300, and 500 mg/kg), Mn.Cr offered protection against castor oil-induced diarrhea. In rabbit jejunum, Mn.Cr and its chloroform fraction inhibited CCh-induced contractions more potently compared with high K(+) (80 mm). Conversely, petroleum fraction was more potent against high-K(+) -induced contractions. At 0.01 mg/mL, Mn.Cr caused a parallel shift in acetylcholine concentration-response curves (CRCs) followed by a non-parallel shift at 0.03 mg/mL, similar to dicyclomine. At further tested concentrations, Mn.Cr (0.1 and 0.3 mg/mL) and petroleum fraction suppressed Ca(2+) CRCs, similar to verapamil. In guinea-pig ileum, Mn.Cr, its aqueous and ethyl acetate fractions exhibited atropine-sensitive gut stimulant activity along with additional uncharacterized excitatory response in the aqueous fraction only. These results suggest that black mulberry possesses prokinetic, laxative, and antidiarrheal effects, putatively mediated through cholinomimetic, antimuscarinic, and Ca(2+) antagonist mechanisms, respectively. Copyright © 2016 John Wiley & Sons, Ltd.
Publisher: Elsevier BV
Date: 02-2010
DOI: 10.1016/J.JEP.2009.10.003
Abstract: The current study was designed to establish the pharmacological rationale for the traditional use of the rhizomes of Polygonatum verticillatum in the treatment of painful conditions and as a plant diuretic. The crude methanolic extract of the rhizomes of Polygonatumverticillatum (PR) was tested in various established pain models in rodents at 50, 100 and 200mg/kg i.p. while the diuretic activity was assessed at 300 and 600 mg/kg p.o. in rats. PR demonstrated significant reduction (14-72%) in the number of writhes induced by acetic acid in a dose-dependent manner. When nociceptive threshold was measured in the formalin test, PR strongly attenuated the formalin-induced flinching behaviour in both phases (6-30% in first phase while 12-72% in second phase). Central involvement in the analgesic profile of PR was confirmed by the hot plate test, in which PR elicited a significant (P<0.01) analgesic activity by increasing latency time. However, an opioid receptor antagonist, naloxone (2mg/kg s.c.) strongly antagonized the antinociceptive activity of PR. As a plant diuretic, PR showed mild but statistically insignificant diuretic activity at 300 mg/kg. The crude extract and solvent fractions of the plant contained reasonable quantity of total saponin and alkaloid contents. The mechanisms underlying the analgesic action of PR shows that the opioid dependant central mediation has synergistic effect by enforcing the peripheral analgesic effects. Interestingly, our findings not only substantiated the folk use of the plant as an analgesic but also reported for the first time in the whole genus.
Publisher: Science Alert
Date: 15-03-2013
Publisher: Science Alert
Date: 11-2014
Publisher: Elsevier BV
Date: 2017
Publisher: Springer Science and Business Media LLC
Date: 08-2006
Publisher: Ovid Technologies (Wolters Kluwer Health)
Date: 09-2016
DOI: 10.1161/CIRCOUTCOMES.115.002488
Abstract: High-sensitivity troponin T (hs-TnT) assays promise greater discrimination of evolving myocardial infarction, but the impact of unguided implementation on the effectiveness of care is uncertain. We evaluated the impact of hs-TnT reporting on care and outcome among chest pain patients presenting to 5 emergency departments within a multicenter randomized trial. Patients were allocated to hs-TnT reporting (hs-report) or standard reporting (std-report Roche Elecys). The primary end point was death and new or recurrent acute coronary syndrome by 12 months. A total of 1937 patients without ST-segment elevation were enrolled between July 2011 and March 2013. The median age was 61 (interquartile range, 48–74) years, and 46.3% were women. During the index hospitalization, 1466 patients (75.7%) had maximal troponin ng/L within 24 hours. Randomization to hs-report format did not alter the admission rate (hs-report: 57.7% versus std-report: 58.0% P =0.069). There was no difference in angiography (hs-report: 11.9% versus std-report: 10.9% P =0.479). The hs-reporting did not reduce 12-month death or new/recurrent acute coronary syndrome in the overall population (hs-report: 9.7% versus std-report: 7.2% [hazard ratio, 0.83 (0.57–1.22) P =0.362]). However, among those with troponin levels ng/L, a modest reduction in the primary end point was observed (hs-report: 2.6% versus std-report: 4.4%, [hazard ratio, 0.58 95% confidence interval, 0.34–0.1.00 P =0.050). High-sensitivity troponin reporting alone is associated with only modest changes in practice. Clinical effectiveness in the adoption of high-sensitivity troponin may require close coupling with protocols that guide interpretation and care. URL: www.ANZCTR.org.au . Unique identifier: ACTRN12611000879965.
Publisher: Wiley
Date: 2007
DOI: 10.1002/PTR.2139
Abstract: A methanol extract of Zizyphus oxyphylla Edgew leaves has been investigated for its analgesic and antipyretic activities in Adult Wistar and Swiss albino mice of either sex at 50, 100 and 200 mg/kg orally. The extract demonstrated marked antipyretic activity against Brewer's yeast-induced pyrexia in rats. The extract demonstrated significant peripheral analgesic effect in the acetic acid-induced writhing test in mice. The phytochemical tests revealed that the extract contained alkaloids, anthraquinones, flavonoids, glycosides, phenols, resins, saponins and tannins using standard procedures. In conclusion, the present study suggests that the methanol extract of Zizyphus oxyphylla Edgew leaves possesses potent antipyretic and antinociceptive activities and thus validates its use in the treatment of pain and fever.
Publisher: Springer Science and Business Media LLC
Date: 24-03-2015
Publisher: Ovid Technologies (Wolters Kluwer Health)
Date: 29-10-1999
Abstract: Abstract —Increased production of nitric oxide (NO) after induction of the cytokine-inducible isoform of nitric oxide synthase (iNOS or NOS2) in cardiac myocytes and other parenchymal cells within the heart may in addition to contributing to myocyte contractile dysfunction also contribute to the induction of programmed cell death (apoptosis). To investigate the mechanism(s) by which increased NO production leads to apoptosis, we examined the role of NO in primary cultures of neonatal rat ventricular myocytes (NRVMs) after induction by the cytokines interleukin-1β (IL-1β) and interferon γ (IFNγ) or exposure to the exogenous NO donor S -nitroso- N -acetylcysteine (SNAC) or peroxynitrite (ONOO − ). Both SNAC (1 mmol/L) and ONOO − (100 μmol/L), but not their respective controls (ie, N -acetylcysteine and pH-inactivated ONOO − ), induced apoptosis in confluent, serum-starved NRVMs at 48 hours. Similarly, incubation of NRVMs with IL-1β and IFNγ for 48 hours resulted in an increase in iNOS expression, nitrite production, and programmed cell death. Both the cytokine-induced nitrite accumulation and myocyte apoptosis could be completely prevented by the nonselective NOS inhibitor l -nitroarginine (3 mmol/L) or the specific iNOS inhibitor 2-amino-5,6-dihydro-6-methyl-4 H -1,3-thiazine (AMT, 100 μmol/L). NO-mediated myocyte apoptosis was not attenuated by the inhibition of soluble guanylyl cyclase with ODQ, nor could apoptosis be induced by the incubation of NRVMs with 1 mmol/L 8-bromo-cGMP, a cell-permeant cGMP analogue. However, NO-mediated apoptosis was significantly attenuated by the superoxide dismutase mimetic and ONOO − scavenger Mn(III)tetrakis (4-benzoic acid) porphyrin (MnTBAP, 100 μmol/L). NO/ONOO − -mediated apoptosis was associated with increased expression of Bax with no change in Bcl-2 mRNA abundance. Furthermore, apoptotic cell death was also confirmed in adult rat ventricular myocytes (ARVMs) when grown in heteroculture with IL-1β– and IFNγ-treated rat cardiac microvascular endothelial cells. Therefore, cytokine-induced apoptosis in NRVMs and ARVMs is mediated by iNOS induction, ONOO − , and associated with an increase in Bax levels.
Publisher: Elsevier BV
Date: 12-2012
DOI: 10.1016/J.EXPPARA.2012.09.007
Abstract: Acanthamoeba is an opportunist protist pathogen that is known to infect the cornea to produce eye keratitis and the central nervous system to produce fatal granulomatous encephalitis. Early diagnosis, followed by aggressive treatment using a combination of drugs is a prerequisite in successful treatment but even then, prognosis remains poor due to lack of effective drugs. The overall aim of the present study was to determine the anti-Acanthamoebic potential of natural compounds, resveratrol and curcuminoids. Adhesion and cytotoxicity assays were performed using primary human brain microvascular endothelial cells, which constitute the blood-brain barrier. Pre-exposure of organisms to 100 μg resveratrol and demethoxy curcumin prevented amoeba binding by 57% and 73%, respectively, while cytotoxicity of host cells was inhibited by 86%. In an assay for viability of amoebae in the absence of host cells, resveratrol and de-methoxy curcumin exhibited significant amoebicidal effects (23% and 25%, respectively) at 100 μg concentrations (P<0.01). Neither resveratrol nor demethoxycurcumin had any effect on the proteolytic activities of Acanthamoeba castellanii. Of both compounds, resveratrol is of most interest for further investigation, because of the selective toxicity of resveratrol on A. castellanii but not the human brain microvascular endothelial cells.
Publisher: Wiley
Date: 2007
DOI: 10.1002/PTR.2023
Abstract: Moringa oleifera Lam (Moringaceae) is a highly valued plant, distributed in many countries of the tropics and subtropics. It has an impressive range of medicinal uses with high nutritional value. Different parts of this plant contain a profile of important minerals, and are a good source of protein, vitamins, beta-carotene, amino acids and various phenolics. The Moringa plant provides a rich and rare combination of zeatin, quercetin, beta-sitosterol, caffeoylquinic acid and kaempferol. In addition to its compelling water purifying powers and high nutritional value, M. oleifera is very important for its medicinal value. Various parts of this plant such as the leaves, roots, seed, bark, fruit, flowers and immature pods act as cardiac and circulatory stimulants, possess antitumor, antipyretic, antiepileptic, antiinflammatory, antiulcer, antispasmodic, diuretic, antihypertensive, cholesterol lowering, antioxidant, antidiabetic, hepatoprotective, antibacterial and antifungal activities, and are being employed for the treatment of different ailments in the indigenous system of medicine, particularly in South Asia. This review focuses on the detailed phytochemical composition, medicinal uses, along with pharmacological properties of different parts of this multipurpose tree.
Publisher: Elsevier BV
Date: 03-2008
DOI: 10.1016/J.JEP.2007.12.021
Abstract: Taxus wallichiana Zucc. (Himalayan Yew) is often used in northern areas of Pakistan for the treatment of pyrexia, acute pains and epilepsy. We have investigated certain pharmacological activities of the methanol leaf extract against convulsion, nociception and pyrexia induced in rodents. The aim was to justify and explore its folk uses in these pathological conditions, on scientific basis. The studies were carried out using acetic acid-induced nociception and pentylenetetrazole-induced convulsions in mice, while formalin test and yeast-induced pyrexia in rats. Significant analgesic (67.77 and 74.29%) effect was found in acetic acid-induced model at doses of 100 and 200mg/kg, i.p. respectively. Crude extract exhibited significant (P<0.05) inhibition of the formalin noxious stimulation on both early and late phases of pain by the extracts (100 and 200mg/kg doses). In case of yeast-induced pyrexia model, 200mg/kg dose showed very significant (P<0.01) inhibition while 50 and 100mg/kg dose caused a significant (P<0.05) inhibition. Plant extract has controlled the pentylenetetrazole-induced convulsions in mice. 100 and 200mg/kg i.p doses of the extract significantly (P<0.05) inhibited the mioclonus and clonus while inhibition of tonus and hind limb tonic extension (HLTE) was highly significant (P<0.01). The anticonvulsant activity of this plant has been reported for the first time throughout the whole genus. The observed pharmacological activities provide the scientific basis for the folkloric use of the plant in treating epilepsy, pyrexia and acute pain.
Publisher: Proceedings of the National Academy of Sciences
Date: 28-05-1996
Abstract: Cardiac myocytes express both constitutive and cytokine-inducible nitric oxide syntheses (NOS). NO and its congeners have been implicated in the regulation of cardiac contractile function. To determine whether NO could affect myocardial energetics, 31P NMR spectroscopy was used to evaluate high-energy phosphate metabolism in isolated rat hearts perfused with the NO donor S-nitrosoacetylcysteine (SNAC). All hearts were exposed to an initial high Ca2+ (3.5 mM) challenge followed by a recovery period, and then, either in the presence or absence of SNAC, to a second high Ca2+ challenge. This protocol allowed us to monitor simultaneously the effect of SNAC infusion on both contractile reserve (i.e., baseline versus high workload contractile function) and high-energy phosphate metabolism. The initial high Ca2+ challenge caused the rate-pressure product to increase by 74 +/- 5% in all hearts. As expected, ATP was maintained as phosphocreatine (PCr) content briefly dropped and then returned to baseline during the subsequent recovery period. Control hearts responded similarLy to the second high Ca2+ challenge, but SNAC-treated hearts did not demonstrate the expected increase in rate-pressure product. In these hearts, ATP declined significantly during the second high Ca2+ challenge, whereas phosphocreatine did not differ from controls, suggesting that phosphoryl transfer by creatine kinase (CK) was inhibited. CK activity, measured biochemically, was decreased by 61 +/- 13% in SNAC-treated hearts compared to controls. Purified CK in solution was also inhibited by SNAC, and reversal could be accomplished with DTT, a sulfhydryl reducing agent. Thus, NO can regulate contractile reserve, possibly by reversible nitrosothiol modification of CK.
Publisher: Elsevier BV
Date: 12-2015
Publisher: Informa UK Limited
Date: 1995
Publisher: SAGE Publications
Date: 24-09-2021
Abstract: The differential impact of young age and female gender on transradial access (TRA) outcomes remains to be confirmed. The primary objective was to assess the impact of young age and female gender on in-hospital net adverse cardiovascular events (NACE). Among 12 346 patients from the Coronary Angiogram Database of South Australia (CADOSA) Registry, the impact of gender men (transfemoral access [TFA] 1995, TRA 6168) and women (TFA 1249, TRA 2934), and a median split of age, ≤63 years (TFA 1617, TRA 4727) and years (TFA 1627, TRA 4375) were analyzed on in-hospital outcomes by creating 5 separate propensity-matched cohorts (entire cohort, men, women, ≤63 and 63 years). Net adverse cardiovascular event reduction with TRA was limited to the years old cohort (odds ratio [OR] = 0.56, 95% CI: 0.34-0.93, P = .02) and women (OR = 0.37, 95% CI: 0.18-0.76, P = .007). In both the age groups and genders, TRA was associated with a lower risk of bleeding and all-cause mortality. On multivariate logistic regression, TRA was associated with a significant reduction in NACE, major bleeding, and mortality in the overall cohort. In conclusion, a reduction in bleeding and mortality was noted with TRA in all the subgroups in this observational study.
Publisher: Mary Ann Liebert Inc
Date: 06-2009
Abstract: The seed extracts from Nigella sativa is used by Unani physicians of traditional medicine (Hakims or Tabibs) and Ayurvedic practitioners (Vaids) in the treatment of several medical disorders including dyslipidemia, obesity, and hypertension. It is, therefore, important to prove or disprove the effectiveness, safety, and tolerability of powdered N. sativa (Kalonji) seed in capsules on serum lipid levels, blood sugar, blood pressure, and body weight in adults. The study design was a randomized, double-blind trial. Conducted at Aga Khan University Hospital, Karachi, from February 2006 to January 2007. Half of the respondents received powdered N. sativa (Kalonji) seed in capsule and the rest received a placebo. Baseline and after-intervention variables recorded were the following: body-mass index, waist-hip ratio, blood pressure, fasting blood sugar, serum lipids, serum alanine aminotransferase, and serum creatinine. One hundred and twenty-three (123) patients were recruited. Sixty-four (64) and 59 patients were randomized to the intervention and the control arms, respectively. Thirty-nine (39) patients in the intervention group and 34 in the control group completed the study. Favorable impact of powdered N. sativa (Kalonji) seed in capsule was noted on almost all variables, but results were not statistically significant because of small s le size. Favorable impact of powdered N. sativa (Kalonji) seed in capsule was noted on almost all variables, but results were not statistically significant. A larger study with adequate s le size is recommended.
Publisher: Wiley
Date: 06-2010
DOI: 10.1002/PTR.3089
Abstract: The effects of aqueous-methanol extract of Saussurea lappa Clarke root (Sl.Cr) was investigated against D-galactosamine (D-GalN) and lipopolysaccharide (LPS)-induced hepatitis in mice. Co-administration of D-GalN (700 mg/kg) and LPS (1 microg/kg) significantly raised the plasma transaminase levels (ALT/AST) as compared to the control group (p < 0.05). Pretreatment of mice with different doses of Sl.Cr (150, 300 and 600 mg/kg) significantly prevented the D-GalN and LPS-induced rise in plasma levels of ALT and AST in a dose-dependent manner (p < 0.05). Post-treatment with Sl.Cr (600 mg/kg) significantly restricted the progression of hepatic damage induced by D-GalN and LPS (p < 0.05). The improvement in plasma enzyme levels was further verified by histopathology of the liver, which showed improved architecture, absence of parenchyma congestion, decreased cellular swelling and apoptotic cells in treatment groups as compared to the toxin group of animals. These data indicate that the Sl.Cr exhibits hepatoprotective effect in mice and this study rationalize the traditional use of this plant in liver disorders.
Publisher: Wiley
Date: 04-2019
DOI: 10.1002/EJHF.1459
Abstract: Physicians' adherence to guideline-recommended therapy is associated with short-term clinical outcomes in heart failure (HF) with reduced ejection fraction (HFrEF). However, its impact on longer-term outcomes is poorly documented. Here, we present results from the 18-month follow-up of the QUALIFY registry. Data at 18 months were available for 6118 ambulatory HFrEF patients from this international prospective observational survey. Adherence was measured as a continuous variable, ranging from 0 to 1, and was assessed for five classes of recommended HF medications and dosages. Most deaths were cardiovascular (CV) (228/394) and HF-related (191/394) and the same was true for unplanned hospitalizations (1175 CV and 861 HF-related hospitalizations, out of a total of 1541). According to univariable analysis, CV and HF deaths were significantly associated with physician adherence to guidelines. In multivariable analysis, HF death was associated with adherence level [subdistribution hazard ratio (SHR) 0.93, 95% confidence interval (CI) 0.87-0.99 per 0.1 unit adherence level increase P = 0.034] as was composite of HF hospitalization or CV death (SHR 0.97, 95% CI 0.94-0.99 per 0.1 unit adherence level increase P = 0.043), whereas unplanned all-cause, CV or HF hospitalizations were not (all-cause: SHR 0.99, 95% CI 0.9-1.02 CV: SHR 0.98, 95% CI 0.96-1.01 and HF: SHR 0.99, 95% CI 0.96-1.02 per 0.1 unit change in adherence score P = 0.52, P = 0.2, and P = 0.4, respectively). These results suggest that physicians' adherence to guideline-recommended HF therapies is associated with improved outcomes in HFrEF. Practical strategies should be established to improve physicians' adherence to guidelines.
Publisher: Public Library of Science (PLoS)
Date: 17-03-2020
Publisher: Science Alert
Date: 15-03-2016
Publisher: Informa UK Limited
Date: 06-10-2011
DOI: 10.3109/10641963.2010.549273
Abstract: This investigation was aimed to provide pharmacological evidences for the medicinal use of Capparis aphylla in hypertension. In normotensive anesthetized rats, intravenous administration of the crude extract of Capparis aphylla (Ca.Cr 3-100 mg/kg) caused a fall in mean arterial pressure (MAP), which was partially blocked in the presence of atropine (2 mg/kg). In isolated rabbit aortic rings, Ca.Cr inhibited phenylephrine (1 μM) and high K(+) (80 mM) precontractions with respective EC(50) values of 0.10 (0.07-0.15) and 1.22 mg/mL (1.00-1.50), suggesting calcium channel blocking (CCB) activity with a predominant inhibitory effect on receptor operated Ca(2+) channels. Pretreatment of the arotic rings with Ca.Cr (0.1-1 mg/mL) caused a rightward shift in the Ca(2+) concentration response curves, similar to verapamil. In isolated rat aorta preparations, Ca.Cr caused a partial endothelium-dependent L-NAME/atropine-sensitive vasodilator effect. In guinea-pig atria, Ca.Cr suppressed both rate and force of spontaneous atrial contractions with respective EC(50) values of 1.35 (1.01-1.79) and 1.60 mg/mL (1.18-2.17), which remained unchanged in the presence of atropine (1 μM). These data indicate that the blood pressure (BP) lowering effect of the crude extract of Capparis aphylla is mediated through a vasodilator and cardiac depressant effect. The vasodilator effect is partly mediated by an endothelium-dependent, atropine-sensitive NO pathway, while the CCB effect is partly responsible for endothelium-independent vasodilatation and also for the cardiac depressant effect thus, this study provides pharmacologic evidence with respect to the medicinal use of the plant in hypertension.
Publisher: Wiley
Date: 06-2015
DOI: 10.1002/PTR.5384
Abstract: The aqueous methanolic extract of the aerial parts of Salvia officinalis (So.Cr) was studied to provide possible underlying mechanism(s) for its medicinal use in asthma using the in vivo bronchodilatory assay and isolated tracheal preparations. S. officinalis (1-10 mg/kg) dose-dependently inhibited carbachol (CCh)-induced bronchospasm in anesthetized rats with three-fold greater potency than the positive control, aminophylline. In tracheal preparations, So.Cr inhibited the low K
Publisher: Wiley
Date: 10-06-2015
DOI: 10.1002/PTR.5380
Abstract: This review summarizes literature related to medicinal plants reputed in traditional medical systems for treatment of asthma and coughs. The plants that are pharmacologically investigated for their effectiveness in such conditions, along with respective experimental protocol details, are also discussed. Some of plant origin compounds, which are considered useful as antitussive and antiasthmatic agents, are described as well. Chrysoeriol, a constituent of Aspalathus linearis (Fabaceae) was observed to be selective for relaxant effect in airways (through K
Publisher: Elsevier BV
Date: 04-2011
DOI: 10.1016/J.JEP.2011.01.047
Abstract: To provide ethnopharmacological basis for the medicinal use of Lepidium sativum seeds in indigestion and constipation. The in vivo studies were conducted in mice, while isolated tissues of mouse, guinea-pig and rabbit were suspended in tissue bath to measure isotonic contractions. The aqueous-methanolic extract of Lepidium sativum seeds (Ls.Cr) at 30 and 100mg/kg showed atropine-sensitive prokinetic and laxative activities in mice, which were partially sensitive to atropine. In isolated gut preparations of mouse and guinea-pig, Ls.Cr (0.1-1mg/mL) caused a concentration-dependent stimulatory effects both in jejunum and ileum, which was blocked in the presence of atropine. In rabbit jejunum, the stimulant effect of Ls.Cr remained unchanged in the presence of atropine, pyrilamine or SB203186, while in rabbit ileum, the stimulatory effect was partially blocked by atropine. The Ls.Cr was more efficacious in gut preparations of rabbit than in guinea-pig or mouse. The phytochemical analysis of the plant extract detected alkaloids, saponins and anthraquinones as plant constituents. This study showed the prokinetic and laxative effects of Lepidium sativum in mice, which were partially mediated through a cholinergic pathway. The in vitro spasmodic effect of the plant extract mediated through a similar mechanism with species and tissue-selectivity, provides a rationale for the medicinal use of the seeds of Lepidium sativum in indigestion and constipation, and suggests studying the plant extracts on more than one species to get the wider picture.
Publisher: Elsevier BV
Date: 06-2022
Publisher: Elsevier BV
Date: 06-2012
DOI: 10.1016/J.JEP.2012.03.039
Abstract: Carum roxburghianum is traditionally used in hyperactive gastrointestinal and respiratory disorders. The present study was carried out to investigate the possible gut and airways relaxant potential of Carum roxburghianum to rationalize its folk uses. Crude extract of Carum roxburghianum (Cr.Cr) was studied in in vivo and in vitro techniques. Cr.Cr exhibited protective effect against castor oil-induced diarrhea in mice at 100-1000 mg/kg. In rabbit jejunum preparations, Cr.Cr (0.03-3.0 mg/mL) caused relaxation of spontaneous and K(+) (80 mM)-induced contractions at similar concentrations, like papaverine. Pretreatment of tissues with Cr.Cr (0.1-1.0 mg/mL) shifted Ca(++) concentration-response curves (CRCs) to right, like verapamil. Cr.Cr (0.03 and 0.1 mg/mL) caused leftward shift of isoprenaline-induced inhibitory CRCs, similar to papaverine. In isolated guinea-pig ileum, Cr.Cr (0.01 and 0.03 mg/mL) produced rightward parallel shift of acetylcholine-curves, like atropine. Cr.Cr (1.0-30 mg/kg) caused suppression of carbachol (CCh, 100 μg/kg)-induced increase in inspiratory pressure of anaesthetized rats. In guinea-pig trachea, Cr.Cr (0.03-1.0 mg/mL) relaxed CCh and high K(+)-induced contractions, shifted isoprenaline-induced inhibitory CRCs to left at 0.1 and 0.3 mg/mL and CCh-curves parallel to right (0.01 and 0.03 mg/mL). Cr.Cr did not cause any mortality of mice up to 10 g/kg dose. These results indicate that Carum roxburghianum possess combination of antidiarrheal, antispasmodic and bronchodilatory effects, which provides pharmacological basis to its traditional use in the disorders of gut and airways hyperactivity, like diarrhea, colic and asthma.
Publisher: Informa UK Limited
Date: 06-2012
DOI: 10.1080/14786419.2010.551754
Abstract: This study describes the antidiarrhoeal and bronchodilatory activities of Valeriana wallichii D.C. (Valerianaceae). The crude extract of V. wallichii (Vw.Cr) caused inhibition of castor oil-induced diarrhoea in mice at 300-600 mg kg⁻¹. In guinea-pig trachea, Vw.Cr concentration dependently (0.03-3.0 mg mL⁻¹) relaxed the low K+ (25 mM)-induced contractions, with a mild effect on the contractions induced by high K+ (80 mM). In the presence of glibenclamide, the relaxation of low K+-induced contractions was prevented. Similarly, cromakalim caused glibenclamide-sensitive inhibition of low K+, without any effect on high K+. These results indicate that V. wallichii exhibits antidiarrhoeal and bronchodilatory activities, possibly through K+ channel activation, and thus reveal its medicinal usefulness in hyperactive gut and airway disorders such as diarrhoea and asthma.
Publisher: Springer Science and Business Media LLC
Date: 08-1998
DOI: 10.1007/BF02974628
Publisher: Bangladesh Journals Online (JOL)
Date: 14-10-2011
Publisher: Elsevier BV
Date: 07-1995
Publisher: Springer Science and Business Media LLC
Date: 03-12-2011
DOI: 10.1007/S11418-011-0605-Z
Abstract: Crude extract of Juniperus excelsa (JeExt), which tested positive for the presence of anthraquinone, flavonoids, saponins, sterols, terpenes and tannin, exhibited a protective effect against castor oil-induced diarrhoea in mice at 100-1000 mg/kg. In rabbit jejunum preparations, JeExt (0.01-1.0 mg/mL) caused relaxation of spontaneous and K(+) (80 mM)-induced contractions at similar concentrations to papaverine, whereas verapamil was relatively more potent against K(+). JeExt (0.03-0.3 mg/mL) shifted Ca(2+) concentration-response curves to the right, like papaverine or verapamil. JeExt (0.003-0.01 mg/mL) caused a leftward shift of isoprenaline-induced inhibitory concentration-response curves, similar to papaverine. JeExt (1.0-30 mg/kg) caused suppression of carbachol (CCh, 100 μg/kg)-induced increase in inspiratory pressure of anaesthetized rats. In guinea-pig trachea, JeExt (0.001-3.0 mg/mL) relaxed CCh (1 μM)- and high K(+)-induced contractions and shifted isoprenaline-induced inhibitory curves to the left. This study suggests that Juniperus excelsa possibly exhibits a combination of Ca(2+) antagonist and phosphodiesterase inhibitory effects, which provides a pharmacological basis for its traditional use in disorders of gut and airways hyperactivity, such as diarrhoea, colic and asthma.
Publisher: Elsevier BV
Date: 09-2008
DOI: 10.1016/J.JEP.2008.05.040
Abstract: The ripe dried fruit of Ficus carica Linn. (Moraceae) commonly known as "Fig" has medicinal value in traditional system of medicine for its use in gastrointestinal and inflammatory disorders. To rationalize the medicinal use of Fig (Ficus carica) in gastrointestinal and inflammatory disorders. The aqueous-ethanolic extract of Ficus carica (Fc.Cr) was studied for antispasmodic effect on the isolated rabbit jejunum preparations and for antiplatelet effect using ex vivo model of human platelets. Fc.Cr tested positive for alkaloids, flavonoids, coumarins, saponins, sterols and terpenes. When tested in isolated rabbit jejunum, Fc.Cr (0.1-3.0mg/mL) produced relaxation of spontaneous and low K(+) (25 mM)-induced contractions with negligible effect on high K(+) (80 mM) similar to that caused by cromakalim. Pretreatment of the tissue with glibenclamide caused rightward shift in the curves of low K(+)-induced contractions. Similarly, cromakalim inhibited the contractions induced by low K(+), but not of high K(+), while verapamil equally inhibited the contractions of K(+) at both concentrations. Fc.Cr (0.6 and 0.12 mg/mL) inhibited the adenosine 5'-diphosphate and adrenaline-induced human platelet aggregation. This study showed the presence of spasmolytic activity in the ripe dried fruit of Ficus carica possibly mediated through the activation of K(+)(ATP) channels along with antiplatelet activity which provides sound pharmacological basis for its medicinal use in the gut motility and inflammatory disorders.
Publisher: Springer International Publishing
Date: 28-11-2015
Publisher: Elsevier BV
Date: 07-1997
Abstract: The effects of protopine on human platelet aggregation and arachidonic acid (AA) metabolism via cyclooxygenase (COX) and lipoxygenase (LOP) enzymes were examined. Platelet aggregation induced by various platelet agonists (AA, ADP, collagen and PAF) was strongly inhibited by protopine in a concentration-related manner. The IC50 values (microM) of protopine (mean +/- SEM) against: AA 12 +/- 2: ADP 9 +/- 2: collagen 16 +/- 2 and PAF 11 +/- 1, were much less than those observed for aspirin. In addition, protopine selectively inhibited the synthesis of thromboxane A2 (TXA2) via COX pathway and had no effect on the LOP pathway in platelets. In vivo, pretreatment with protopine (50-100 mg kg-1) protected rabbits from the lethal effects of AA (2 mg kg-1) or PAF (11 micrograms kg-1) in dose-dependent fashion. Protopine (50-100 mg kg-1) also inhibited carrageenan-induced rat paw oedema with a potency of three-fold as compared to aspirin. These results are suggestive that protopine acts as a potent inhibitor of thromboxane synthesis and PAF with anti-inflammatory properties.
Publisher: Mary Ann Liebert Inc
Date: 10-2010
Abstract: Dried fruits of Piper nigrum (black pepper) are commonly used in gastrointestinal disorders. The aim of this study was to rationalize the medicinal use of pepper and its principal alkaloid, piperine, in constipation and diarrhea using in vitro and in vivo assays. When tested in isolated guinea pig ileum, the crude extract of pepper (Pn.Cr) (1–10 mg/mL) and piperine (3–300 μM) caused a concentration-dependent and atropine-sensitive stimulant effect. In rabbit jejunum, Pn.Cr (0.01–3.0 mg/mL) and piperine (30–1,000 μM) relaxed spontaneous contractions, similar to loperamide and nifedipine. The relaxant effect of Pn.Cr and piperine was partially inhibited in the presence of naloxone (1 μM) similar to that of loperamide, suggesting the naloxone-sensitive effect in addition to the Ca(2+) channel blocking (CCB)-like activity, which was evident by its relaxant effect on K+ (80 mM)-induced contractions. The CCB activity was confirmed when pretreatment of the tissue with Pn.Cr (0.03–0.3 mg/mL) or piperine (10–100 μM) caused a rightward shift in the concentration–response curves of Ca(2+), similar to loperamide and nifedipine. In mice, Pn.Cr and piperine exhibited a partially atropine-sensitive laxative effect at lower doses, whereas at higher doses it caused antisecretory and antidiarrheal activities that were partially inhibited in mice pretreated with naloxone (1.5 mg/kg), similar to loperamide. This study illustrates the presence of spasmodic (cholinergic) and antispasmodic (opioid agonist and Ca(2+) antagonist) effects, thus providing the possible explanation for the medicinal use of pepper and piperine in gastrointestinal motility disorders.
Publisher: Springer Science and Business Media LLC
Date: 13-01-2010
Publisher: Elsevier
Date: 2017
Publisher: Informa UK Limited
Date: 07-09-2010
DOI: 10.3109/13880201003727960
Abstract: Holarrhena antidysenterica Wall. (Apocynaceae) is widely used in traditional medical system for treatment of constipation, colic, and diarrhea. This study was carried out to provide pharmacological basis for medicinal use of Holarrhena antidysenterica in gastrointestinal disorders. Hydro-ethanolic crude extract of Holarrhena antidysenterica (HaCE) and its fractions were studied in various gastrointestinal isolated tissue preparations. In guinea pig ileum tissues, HaCE at 0.3-10 mg/mL caused pyrilamine-sensitive spasmogenic effect. When tested in spontaneously contracting rabbit jejunum preparations, HaCE (0.01-3.0 mg/mL) caused moderate stimulation, followed by a relaxant effect at next higher concentrations. In presence of pyrilamine, the contractile effect was blocked and the relaxation was observed at lower concentrations (0.01-0.3 mg/mL). HaCE inhibited the high K(+) (80 mM)-induced contractions at concentration range of 0.01-1.0 mg/mL and shifted Ca(++) concentration response curves to the right, like that caused by verapamil. Activity-directed fractionation revealed that the spasmogenic component was concentrated in the aqueous fraction, while the spasmolytic component was concentrated in the organic fraction. These results indicate that the gut stimulant and relaxant activities of Holarrhena antidysenterica are mediated possibly through activation of histamine receptors and Ca(++) channel blockade, respectively and this study provides sound mechanistic background for its usefulness in gut motility disorders such as constipation, colic, and possibly diarrhea.
Publisher: Elsevier BV
Date: 08-2014
DOI: 10.1016/J.JEP.2014.06.011
Abstract: Citrullus colocynthis (L.) Schrad is a valuable cucurbit plant, widely distributed in the desert areas of the world. Citrullus colocynthis fruits are usually recognized for its wide range of medicinal uses as well as pharmaceutical and nutraceutical potential. This review aims to appraise the published information on the ethnobotanical knowledge, phytochemistry, ethnopharmacology, nutraceutical potential and safety studies of Citrullus colocynthis (bitter apple) fruit, with critical analysis on the gaps and potential for future studies. A literature survey was performed by searching the scientific databases including PubMed, Scopus, SciFinder, Google Scholar, Web of Science, ACS as well as published books. The plant has been reported to possess a wide range of traditional medicinal uses including in diabetes, leprosy, common cold, cough, asthma, bronchitis, jaundice, joint pain, cancer, toothache, wound, mastitis, and in gastrointestinal disorders such as indigestion, constipation, dysentery, gastroenteritis, colic pain and different microbial infections. Several bioactive chemical constituents from fruits were recorded, such as, glycosides, flavonoids, alkaloids, fatty acids and essential oils. The isolation and identification of curcurbitacins A, B, C, D, E, I, J, K, and L and Colocynthosides A, and B were also reported. The fruit of Citrullus colocynthis has been studied extensively for its wide range of biological activities, which include antioxidant, cytotoxic, antidiabetic, antilipidemic, insecticide, antimicrobial and anti-inflammatory. The plant was also shown to be rich in nutritional value with high protein contents and important minerals as well as edible quality of seed oil. It is evident from the literature that Citrullus colocynthis possesses a wide range of medicinal uses and has been well studied for its antidiabetic, anticancer, antioxidant, antimicrobial and anti-inflammatory activities, while its therapeutic potential for gut, airways and cardiovascular disorders remains to be explored. Critical analysis revealed that the plant has the huge potential for pharmaceutical and nutraceutical application, with some indications for the presence of synergistic and /or side effects neutralizing combinations of activities.
Publisher: Bangladesh Journals Online (JOL)
Date: 13-03-2015
Publisher: Wiley
Date: 19-07-2014
DOI: 10.1002/PTR.5030
Abstract: Alzheimer's disease (AD) is the most common form of dementia. There is limited choice in modern therapeutics, and drugs available have limited success with multiple side effects in addition to high cost. Hence, newer and alternate treatment options are being explored for effective and safer therapeutic targets to address AD. Turmeric possesses multiple medicinal uses including treatment for AD. Curcuminoids, a mixture of curcumin, demethoxycurcumin, and bisdemethoxycurcumin, are vital constituents of turmeric. It is generally believed that curcumin is the most important constituent of the curcuminoid mixture that contributes to the pharmacological profile of parent curcuminoid mixture or turmeric. A careful literature study reveals that the other two constituents of the curcuminoid mixture also contribute significantly to the effectiveness of curcuminoids in AD. Therefore, it is emphasized in this review that each component of the curcuminoid mixture plays a distinct role in making curcuminoid mixture useful in AD, and hence, the curcuminoid mixture represents turmeric in its medicinal value better than curcumin alone. The progress in understanding the disease etiology demands a multiple-site-targeted therapy, and the curcuminoid mixture of all components, each with different merits, makes this mixture more promising in combating the challenging disease.
Publisher: Wiley
Date: 02-08-2013
DOI: 10.1111/AJCO.12092
Publisher: African Journals Online (AJOL)
Date: 13-07-2018
DOI: 10.4314/TJPR.V17I6.6
Publisher: Ovid Technologies (Wolters Kluwer Health)
Date: 08-2014
Publisher: Elsevier BV
Date: 06-2006
Publisher: Science Alert
Date: 15-12-2017
Publisher: Informa UK Limited
Date: 21-11-2014
DOI: 10.3109/13880209.2013.854811
Abstract: Hypericum perforatum Linn. (Hypericaceae) (St. John's wort) attenuates opium withdrawal signs. To explore the therapeutic potential of Hypericum perforatum in the management of opium-induced withdrawal syndrome. The effect of the Hypericum perforatum hydro-ethanol extract was investigated for potential to reverse naloxone (0.25 mg/kg)-induced opium withdrawal physical signs. Rats received opium extract (80-650 mg/kg) twice daily for 8 days along with Hypericum perforatum (20 mg/kg, orally) twice daily in chronic treatment and the same single dose 1 h before induction of withdrawal syndrome in the acute treated group. Hypericum perforatum reduced stereotype jumps and wet dog shake number in the chronic treatment compared to the saline control group (F(2, 24) = 3.968, p < 0. 05) and (F(2, 24) = 3.689, p < 0.05), respectively. The plant extract in the acutely treated group reduced diarrhea (F(2, 24) = 4.850, p < 0. 05 vs. saline). It decreased rectal temperature by chronic treatment at 30 min (F(2, 24) = 4.88, p < 0.05), 60 min (F(2, 240 = 5.364, p < 0.01) and 120 min (F(2, 24) = 4.907, p < 0.05). This study reveals that the extract of Hypericum perforatum attenuates some physical signs of opium withdrawal syndrome possibly through direct or indirect interaction with opioid receptors. Further study is needed to clarify its mechanism.
Publisher: Elsevier BV
Date: 02-2009
DOI: 10.1016/J.JEP.2008.12.016
Abstract: Coriander (Coriandrum sativum) is traditionally used for various gastrointestinal and cardiovascular disorders and this study was designed to rationalize its use in dyspepsia, abdominal colic, diarrhea, hypertension and as diuretic. Coriander crude extract (Cs.Cr) was evaluated through in vitro and in vivo techniques. Cs.Cr caused atropine sensitive stimulatory effect in isolated guinea-pig ileum (0.1-10 mg/ml). In rabbit jejunum preparations, Cs.Cr evoked a similar contractile response but in the presence of atropine, it exhibited relaxation against both spontaneous and high K(+) (80 mM)-induced contractions as well as shifted the Ca(2+) concentration-response curves to right, similar to that caused by verapamil. Cs.Cr (1-30 mg/ml) caused fall in arterial blood pressure of anesthetized animals, partially blocked by atropine. Cs.Cr produced vasodilatation against phenylephrine and K(+) (80 mM)-induced contractions in rabbit aorta and cardio-depressant effect in guinea-pig atria. Cs.Cr produced diuresis in rats at 1-10mg/kg. Bio-assay-directed fractionation revealed the separation of spasmogenic and spasmolytic components in the aqueous and organic fractions respectively. These results indicate that coriander fruit exhibits gut stimulatory, inhibitory and hypotensive effects mediating possibly through cholinergic, Ca(2+) antagonist and the combination of these mechanisms respectively. Diuretic activity adds value to its use in hypertension.
Publisher: Bangladesh Journals Online (JOL)
Date: 10-07-2013
Publisher: Informa UK Limited
Date: 02-04-2012
DOI: 10.3109/10641963.2011.631651
Abstract: Juniperus excelsa Bieb. is used in folk medicine for lowering blood pressure (BP). Its BP-lowering effect, endothelium-dependent and endothelium-independent vasodilator effects, and cardio-modulatory effect are reported here. The crude extract of J. excelsa (Je.Cr) which tested positive for the presence of anthraquinone, flavonoids, saponins, sterols, terpenes, and tannins induced a dose-dependent (10-300 mg/kg) fall in the arterial BP of anesthetized rats. In isolated rabbit aorta, Je.Cr (0.01-5.0 mg/mL) inhibited high K(+) (80 mM)- and phenylephrine (1 μM)-induced contractions, like that caused by verapamil and papaverine. In endothelium-intact rat aortic preparations, N(ω)-nitro-l-arginine methyl ester hydrochloride-sensitive vasodilator activity was noted from Je.Cr, which also relaxed the endothelium-denuded aorta tissues. In guinea pig atria, Je.Cr initially caused mild cardiac stimulation, followed by inhibition, like that exhibited by papaverine. Je.Cr prolonged the R-R interval in electrocardiogram of rats under anesthesia. These results reveal that cardiovascular effects of J. excelsa are mediated possibly through a combination of Ca(++) antagonism, nitric oxide-modulating mechanism, and phosphodiesterase inhibitory mechanism, which explain its medicinal use in hypertension.
Publisher: Elsevier BV
Date: 08-2019
Publisher: Oxford University Press (OUP)
Date: 29-04-2015
Publisher: Elsevier BV
Date: 04-2015
Publisher: Elsevier BV
Date: 03-1995
DOI: 10.1016/0306-3623(94)00194-R
Abstract: 1. Effect of aqueous-methanolic extract of Artemisia absinthium (Compositae) was investigated against acetaminophen- and CCl4-induced hepatic damage. 2. Acetaminophen produced 100% mortality at the dose of 1 g/kg in mice while pretreatment of animals with plant extract (500 mg/kg) reduced the death rate to 20%. 3. Pretreatment of rats with plant extract (500 mg/kg, orally twice daily for two days) prevented (P < 0.01) the acetaminophen (640 mg/kg) as well as CCl4 (1.5 ml/kg)-induced rise in serum transaminases (GOT and GPT). 4. Post-treatment with three successive doses of extract (500 mg/kg, 6 hr) restricted the hepatic damage induced by acetaminophen (P 0.05). 5. Plant extract (500 mg/kg) caused significant prolongation (P < 0.05) in pentobarbital (75 mg/kg)-induced sleep as well as increased strychnine-induced lethality in mice suggestive of inhibitory effect on microsomal drug metabolizing enzymes (MDME). 6. These results indicate that the crude extract of Artemisia absinthium exhibits hepatoprotective action partly through MDME inhibitory action and validates the traditional use of plant in hepatic damage.
Publisher: Walter de Gruyter GmbH
Date: 02-2005
Abstract: The hexane extract of Syzygium samarangense (Ss.Hex) dose-dependently (10D1000 μg/ ml) relaxed the spontaneously contracting isolated rabbit jejunum. Four rare C-methylated flavonoids with a chalcone and a flavanone skeleton were isolated from Ss.Hex and were subsequently tested for spasmolytic activity. All flavonoids, identified as 2′-hydroxy-4′,6′- dimethoxy-3′-methylchalcone (1), 2′,4′-dihydroxy-6′-methoxy-3′,5′-dimethylchalcone (2), 2′,4′-dihydroxy-6′-methoxy-3′-methylchalcone (3), and 7-hydroxy-5-methoxy-6,8-dimethylflavanone (4), showed dose-dependent spasmolytic activity in the rabbit jejunum with IC 50 values of 148.3 ± 69.4, 77.2 ± 43.5, 142.4 ± 58.6 and 178.5 ± 37.5 μg/ml (mean ± SEM), respectively. The dihydrochalcone derivative of compound 1, 2′-hydroxy-4′,6′-dimethoxy-3′- methyldihydrochalcone (5), when tested for spasmolytic activity, did not significantly relax the smooth muscle relative to the other compounds. Verapamil, a standard spasmolytic, has an IC 50 value of 0.16 ± 0.04 μg/ml. This is the first report of the relaxant activity of chalcones, specifically of compounds 1-3.
Publisher: Elsevier BV
Date: 02-2015
DOI: 10.1016/J.JEP.2014.11.030
Abstract: Linum usitatissimum, commonly known as Flaxseed has traditionally been used for the management of diarrhea and gastrointestinal infections. This study was planned to assess pharmacological basis for the medicinal use of Flaxseed in infectious and non-infectious diarrhea. The crude aqueous-methanolic extract of Flaxseed was studied using the in vivo castor oil-induced diarrhea, gut motility and enteropooling assays. Mechanistic basis was further elucidated by testing the inhibitory effect on spontaneously contracting isolated rabbit jejunum preparations, suspended in a 10ml tissue bath containing Tyrode׳ solution, maintained at 37°C and aerated with carbogen. Antibacterial efficacy of the Flaxseed extract was tested against different enteric and non-enteric pathogenic bacteria using in vitro antibacterial assays. Flaxseed extract reduced the diarrheal score in mice, by 39%, 63.90% and 68.34% at the respective doses of 100, 300 and 500mg/kg. Intestinal secretions were reduced by 24.12%, 28.09% and 38.80%, whereas the intestinal motility was reduced by 31.66%, 46.98% and 56.20% at respective doses of 100, 300 and 500mg/kg. When tested on isolated rabbit jejunum preparations, Flaxseed extract produced a dose-dependent inhibition of both spontaneous and high K(+) (80mM)-induced contractions, and shifted the concentration-response curves of Ca(++) to the right with suppression of the maximum response, similar to that caused by verapamil. Flaxseed extract was found to possess bactericidal activity at the tested concentrations of 12.5mg/ml, against vancomycin-resistant Enterococcus faecalis (100%), Escherichia coli K1 (88.88%), methicillin-resistant Staphylococcus aureus (98.76%), Bacillus cereus (92.64%), Pseudomonas aeruginosa (76.83%) and Salmonella typhi (26.91±3.35%). The concentration of 10mg/ml showed bactericidal effects against all the aforementioned pathogens except Escherichia coli K1, whereas for Pseudomonas aeruginosa and Salmonella typhi, it was bacteriostatic at this concentration. Our results indicate that Linum usitatissimum (Flaxseed) extract exhibits antidiarrheal and antispasmodic activities by virtue of its antimotility and antisecretory effects which are mediated possibly through inhibition of Ca(++) channels, though additional mechanism(s) cannot be ruled out. Flaxseed extract proved effective against both enteric and non-enteric pathogens causing diarrhea, thus ensuring wide coverage and rationalizing its medicinal use in both the infectious and non-infectious diarrhea.
Publisher: Wiley
Date: 2006
DOI: 10.1002/PTR.1801
Abstract: Syzygium samarangense (Family Myrtaceae) or 'makopa', as it is commonly known, is native to Malaysia, some islands of Indonesia and to Far East in general. This study was undertaken to rationalize the use of this plant in hypermotility states of the gut. The hexane extract of S. samarangense (Ss.Hex) was found to dose-dependently (10-3000 microg/mL) relax the spontaneously contracting isolated rabbit jejunum. When tested for a possible calcium channel blocking (CCB) activity, the extract (10-1000 microg/mL) relaxed the high K+-induced contractions and also decreased the Ca++ dose-response curves in a dose-dependent manner (30-100 microg/mL), confirming the CCB activity. Four flavonoids isolated from the hexane extract were tested for a possible spasmolytic activity. All flavonoids, identified as: 2'-hydroxy-4',6'-dimethoxy-3'-methylchalcone (SS1), 2',4'-dihydroxy-6'-methoxy-3',5'-dimethylchalcone (SS2), 2',4'-dihydroxy-6'-methoxy-3'-methylchalcone (SS3) and 7-hydroxy-5-methoxy-6,8-dimethylflavanone (SS4), showed dose-dependent (10-1000 microg/mL) spasmolytic activity with SS2 being the most potent. These results indicate that the presence of compounds with spasmolytic and calcium antagonist activity may be responsible for the medicinal use of the plant in diarrhoea.
Publisher: Wiley
Date: 2006
DOI: 10.1002/PTR.1800
Abstract: The in vitro and in vivo anthelmintic activity of Nicotiana tabacum L. leaves was studied to rationalize its traditional use. Live Haemonchus contortus were used to assess the in vitro anthelmintic effect of a crude aqueous extract (CAE) and a methanol extract (CME) of N. tabacum. The in vitro inhibitory effect of both the extracts was evident from the paralysis and/or mortality of worms noted at 6 h post-exposure. For the in vivo studies, CAE and CME were administered in increasing doses (1.0-3.0 g/kg) to sheep naturally infected with mixed species of gastrointestinal nematodes. A maximum reduction of 73.6% in eggs per gram (EPG) of faeces was recorded on day 5 post-treatment with CME (3.0 g/kg) while the same dose of CAE showed a 49.4% reduction. Levamisole (7.5 mg/kg), a standard anthelmintic agent, showed a 99.6% reduction in EPG. These data show that the aqueous and methanol extracts of Nicotiana tabacum exhibit dose-dependent anthelmintic activity both in vitro and in vivo, thus justifying its use in the traditional medicine system of Pakistan.
Publisher: Springer Science and Business Media LLC
Date: 10-03-2012
Abstract: Fumaria parviflora Linn. ( Fumariaceae ), is a small branched annual herb found in many parts of the world including Saudi Arabia and Pakistan. This study was designed to provide pharmacological basis for the medicinal use of Fumaria parviflora in gut motility disorders. The in-vivo prokinetic and laxative assays were conducted in mice. Isolated intestinal preparations (ileum and jejunum) from different animal species (mouse, guinea-pig and rabbit) were separately suspended in tissue baths containing Tyrode's solution bubbled with carbogen and maintained at 37°C. The spasmogenic responses were recorded using isotonic transducers coupled with PowerLab data acquisition system. The aqueous-methanol extract of Fumaria parviflora (Fp.Cr), which tested positive for the presence of alkaloids, saponins, tannins and anthraquinones showed partially atropine-sensitive prokinetic and laxative activities in the in-vivo in mice at 30 and 100 mg/kg. In the in-vitro studies, Fp.Cr (0.01-1 mg/ml) caused a concentration-dependent atropine-sensitive stimulatory effect both in mouse tissues (jejunum and ileum), and rabbit jejunum but had no effect in rabbit ileum. In guinea-pig tissues (ileum and jejunum), the crude extract showed a concentration-dependent stimulatory effect with higher efficacy in ileum and the effect was partially blocked by atropine, indicating the involvement of more than one types of gut-stimulant components (atropine-sensitive and insensitive). This could be a plausible reason for the greater efficacy of Fp.Cr in gut preparations of guinea-pig than in rabbit or mouse. This study shows the prokinetic, laxative and spasmodic effects of the plant extract partially mediated through cholinergic pathways with species and tissue-selectivity, and provides a sound rationale for the medicinal use of Fumaria parviflora in gut motility disorders such as, indigestion and constipation. This study also suggests using different species to know better picture of pharmacological profile of the test material.
Publisher: Informa UK Limited
Date: 2006
DOI: 10.1080/14756360600889708
Abstract: During this study, one new coumarin 7-O-beta-D-glucopyranoside-2H-1-benzopyran-2-one (1) and three quinoline alkaloids 3-hydroxy, 2, 2, 6-trimethyl-3, 4, 5, 6-tetrahydro-2H-pyrano[3,2-c] quinoline 5-one (2), ribalinine (3) and methyl isoplatydesmine (4) were isolated from the aerial parts of Skimmia laureola and their structures established by spectroscopic studies. Compounds 2-4 were found to be linear mixed type inhibitors of acetylcholinesterase (K(i) = 110.0, 30.0 and 30.0 microM, respectively). Compounds 2 and 3 were also found to be linear mixed type inhibitors of butyrylcholinesterase, while compound 4 was a noncompetitive inhibitor of the enzyme (K(i) = 90.0, 70.0 and 19.0 microM, respectively). The inhibition of acetyl- and butyryl-cholinesterase enzymes persists as the most promising therapeutic strategy for activating the impaired cholinergic functions in Alzheimer's disease and related dementias. Compound 4 also showed dose-dependent spasmolytic activity in the isolated rabbit jejunum intestinal preparation by relaxing the spontaneous (EC50 = 0.1 mg/mL) and K(+)-induced contractions (EC50 = 0.4 mg/mL), suggesting that the spasmolytic effect of compound 4 is mediated through the blockade of voltage-dependent Ca2+ channels.
Publisher: Elsevier BV
Date: 02-2009
DOI: 10.1016/J.JEP.2008.12.004
Abstract: Bergenia ligulata is widely used plant in South Asia, mainly India and Pakistan, as a traditional medicine for treatment of urolithiasis. To rationalize the Bergenia ligulata use in kidney stones and to explain the underlying mechanisms. The crude aqueous-methanolic extract of Bergenia ligulata rhizome (BLR) was studied using in vitro and in vivo methods. BLR inhibited calcium oxalate (CaC(2)O(4)) crystal aggregation as well as crystal formation in the metastable solutions and exhibited antioxidant effect against 1,1-diphenyl-2-picrylhydrazyl free radical and lipid peroxidation in the in vitro. BLR caused diuresis in rats accompanied by a saluretic effect. In an animal model of urolithiasis, developed in male Wistar rats by adding 0.75% ethylene glycol (EG) in drinking water, BLR (5-10 mg/kg) prevented CaC(2)O(4) crystal deposition in the renal tubules. The lithogenic treatment caused polyuria, weight loss, impairment of renal function and oxidative stress, manifested as increased malondialdehyde and protein carbonyl contents, depleted reduced glutathione and decreased antioxidant enzyme activities of the kidneys, which were prevented by BLR. Unlike the untreated animals, EG intake did not cause excessive hyperoxaluria and hypocalciuria in BLR treated groups and there was a significant increase in the urinary Mg(2+), instead of a slight decrease. These data indicate the antiurolithic activity in Bergenia ligulata mediated possibly through CaC(2)O(4) crystal inhibition, diuretic, hypermagneseuric and antioxidant effects and this study rationalizes its medicinal use in urolithiasis.
Publisher: Portland Press Ltd.
Date: 11-1992
DOI: 10.1042/BST020357S
Publisher: Wiley
Date: 30-01-2008
DOI: 10.1111/J.1472-8206.2007.00561.X
Abstract: This study describes the spasmolytic, antidiarrhoeal, antisecretory, bronchodilatory and urinary bladder relaxant properties of Hyoscyamus niger to rationalize some of its medicinal uses. The crude extract of H. niger seeds (Hn.Cr) caused a complete concentration-dependent relaxation of spontaneous contractions of rabbit jejunum, similar to that caused by verapamil, whereas atropine produced partial inhibition. Hn.Cr inhibited contractions induced by carbachol (1 microM) and K(+) (80 mM) in a pattern similar to that of dicyclomine, but different from verapamil and atropine. Hn.Cr shifted the Ca(2+) concentration-response curves to the right, similar to that caused by verapamil and dicyclomine, suggesting a Ca(2+) channel-blocking mechanism in addition to an anticholinergic effect. In the guinea-pig ileum, Hn.Cr produced a rightward parallel shift of the acetylcholine curves, followed by a non-parallel shift with suppression of the maximum response at a higher concentration, similar to that caused by dicyclomine, but different from that of verapamil and atropine. Hn.Cr exhibited antidiarrhoeal and antisecretory effects against castor oil-induced diarrhoea and intestinal fluid accumulation in mice. In guinea-pig trachea and rabbit urinary bladder tissues, Hn.Cr caused relaxation of carbachol (1 microM) and K(+) (80 mM) induced contractions at around 10 and 25 times lower concentrations than in gut, respectively, and shifted carbachol curves to the right. Only the organic fractions of the extract had a Ca(2+) antagonist effect, whereas both organic and aqueous fractions had anticholinergic effect. A constituent, beta-sitosterol exhibited Ca(2+) channel-blocking action. These results suggest that the antispasmodic effect of H. niger is mediated through a combination of anticholinergic and Ca(2+) antagonist mechanisms. The relaxant effects of Hn.Cr occur at much lower concentrations in the trachea and bladder. This study offers explanations for the medicinal use of H. niger in treating gastrointestinal and respiratory disorders and bladder hyperactivity.
Publisher: Elsevier BV
Date: 09-2010
DOI: 10.1016/J.JEP.2010.07.024
Abstract: This study was undertaken to provide a pharmacological basis for traditional use of Acorus calamus in airways disorders. Isolated guinea-pig trachea and atria were suspended in organ baths bubbled with carbogen and mechanisms were found using different parameters. In isolated guinea-pig tracheal segments, crude extract of Acorus calamus was more effective than carbachol in causing relaxation of high K(+) (80 mM) precontractions, similar to verapamil, suggesting blockade of calcium channels. The n-hexane fraction was equipotent against both precontractions, similar to papaverine, while ethylacetate fraction was more potent against carbachol precontractions but had a negligible dilator effect against K(+), similar to atropine and or rolipram. Pretreatment of tracheal preparations with n-hexane or ethylacetate fractions potentiated isoprenaline-induced inhibitory concentration-response curves, similar to papaverine or rolipram. Pretreatment of tracheal preparations with ethylacetate fraction caused a rightward parallel shift in carbachol response curve at lower concentration (0.003 mg/mL) similar to atropine and a non-parallel shift at higher concentrations (0.01 mg/mL), with reduction of maximum response, similar to rolipram. In isolated guinea-pig atrial preparations, crude extracts, its fractions and papaverine inhibited force and rate of contractions at higher concentrations than the smooth muscle while verapamil was equipotent. These data indicate the presence of unique combination of airways relaxant constituents in crude extract of Acorus calamus, a papaverine-like dual inhibitor of calcium channels and phosphodiesterase in n-hexane fraction and a novel combination of anticholinergic, rolipram-like phosphodiesterase4 inhibitor in ethylacetate fraction and associated cardiac depressant effect, provide a pharmacological basis for traditional use of Acorus calamus in disorders of airways.
Publisher: Informa UK Limited
Date: 18-04-2011
DOI: 10.3109/13880209.2010.550056
Abstract: The present study describes the spasmogenic and spasmolytic activities of Daphne oleoides Schreb. (Thymelaeaceae), exploring the possible underlying pharmacological mechanisms. Pharmacological investigation of Daphne oleoides to provide evidence for its therapeutic application in gastrointestinal motility disorders. Methanol crude extract of Daphne oleoides (Do.Cr) was studied in gastrointestinal isolated tissues. In spontaneously contracting rabbit jejunum preparations, Do.Cr at 0.3-3.0 mg/mL caused moderate stimulation, followed by relaxant effect at the next higher concentrations (5.0-10 mg/mL). In presence of atropine, spasmogenic effect was blocked and the relaxation was emerged, suggesting that the spasmogenic effect of Daphne oleoides is mediated through activation of muscarinic receptors. When tested against the high K+ (80 mM)-induced contractions, Do.Cr (0.3-5.0 mg/mL), like verapamil, inhibited the induced contractions, suggesting Ca++ channel blockade (CCB) effect. The CCB effect was further confirmed when pre-treatment of the tissue with Do.Cr shifted the Ca++ concentration-response curves to the right, similar to that caused by verapamil. These results indicate that Daphne oleoides exhibits gut excitatory and inhibitory effects, occurred via cholinergic and Ca++ antagonistic pathways, respectively.
Publisher: Elsevier BV
Date: 03-1993
DOI: 10.1016/0031-9422(93)85244-L
Abstract: A new triterpenoidal saponin of hederagenin named symphytoxide A has been isolated from the ethanolic extract of the roots of Symphytum officinale and characterized on the basis of chemical investigations and spectroscopic studies as 3-O-[beta-D-glucopyranosyl-(1-->2)-beta-D-glucopyranosyl-(1-->4)- alpha-L-arabinopyranosyl] hederagenin. The structure of this new saponin was established on the basis of 1D and 2D NMR experiments including heteroCOSY, COSY-45 degrees as well as HMBC measurements and other spectroscopic techniques. The saponin exhibited hypotensive activity in anesthetized rats.
Publisher: Ovid Technologies (Wolters Kluwer Health)
Date: 05-02-2019
Abstract: Using data from the GARFIELD ‐ AF (Global Anticoagulant Registry in the FIELD –Atrial Fibrillation), we evaluated the impact of chronic kidney disease ( CKD ) stage on clinical outcomes in patients with newly diagnosed atrial fibrillation ( AF ). GARFIELD ‐ AF is a prospective registry of patients from 35 countries, including patients from Asia (China, India, Japan, Singapore, South Korea, and Thailand). Consecutive patients enrolled (2013–2016) were classified with no, mild, or moderate‐to‐severe CKD , based on the National Kidney Foundation's Kidney Disease Outcomes Quality Initiative guidelines. Data on CKD status and outcomes were available for 33 024 of 34 854 patients (including 9491 patients from Asia) 10.9% (n=3613) had moderate‐to‐severe CKD , 16.9% (n=5595) mild CKD , and 72.1% (n=23 816) no CKD . The use of oral anticoagulants was influenced by stroke risk (ie, post hoc assessment of CHA 2 DS 2 ‐ VAS c score), but not by CKD stage. The quality of anticoagulant control with vitamin K antagonists did not differ with CKD stage. After adjusting for baseline characteristics and antithrombotic use, both mild and moderate‐to‐severe CKD were independent risk factors for all‐cause mortality. Moderate‐to‐severe CKD was independently associated with a higher risk of stroke/systemic embolism, major bleeding, new‐onset acute coronary syndrome, and new or worsening heart failure. The impact of moderate‐to‐severe CKD on mortality was significantly greater in patients from Asia than the rest of the world ( P =0.001). In GARFIELD ‐ AF , moderate‐to‐severe CKD was independently associated with stroke/systemic embolism, major bleeding, and mortality. The effect of moderate‐to‐severe CKD on mortality was even greater in patients from Asia than the rest of the world. URL : www.clinicaltrials.gov . Unique identifier: NCT 01090362.
Publisher: Informa UK Limited
Date: 26-01-2015
DOI: 10.3109/13880209.2014.919327
Abstract: Vitex negundo Linn. (Verbenaceae) is traditionally used in hyperactive respiratory disorders. This study explored the mechanisms underlying the effectiveness of Vitex negundo in hyperactive respiratory disorders. Crude extract of V. negundo leaves was obtained. For in vivo bronchodilatory activity in anesthetized rats, different doses (1, 3, 10, 30, and 50 mg/kg) of the crude extract of V. negundo (Vn.Cr) were tested. The underlying mechanisms were studied in isolated guinea pig tracheal strips, suspended in organ baths at 37 °C. Intravenous doses of the crude extract of Vn.Cr showed dose-dependent bronchodilatory effect (9-50%) against carbachol (CCh 100 µg/kg)-induced bronchoconstriction, similar to aminophylline. In isolated guinea-pig tracheal strips, Vn.Crrelaxed CCh (1 µM) and high K(+) pre-contractions with respective EC50 values of 0.72 (0.48-1.10 n = 5) and 3.38 mg/mL (1.84-6.21 n = 4), similar to papaverine. Diltiazem also relaxed both contractions with more potency against high K(+) pre-contraction (p < 0.05). Pre-incubation of the tracheal strips with Vn.Cr potentiated the isoprenaline inhibitory concentration response curves (CRCs), similar to papaverine. The inhibitory effect against CCh and high K(+) suggests involvement of phosphodiesterase (PDE) inhibitory pathway(s), in addition to an inhibitory effect on Ca(++) entry. This finding was further strengthened when pre-treatment of the tracheal strips potentiated the isoprenaline CRCs. RESULTS suggest Vn.Cr possesses a combination of papaverine-like PDE inhibitor and diltiazem-like Ca(++) entry blocking constituents, which partly explain its bronchodilatory effect, thus validating its medicinal importance in asthma.
Publisher: Portland Press Ltd.
Date: 11-1992
DOI: 10.1042/BST020358S
Publisher: Wiley
Date: 24-09-2015
DOI: 10.1002/PTR.5222
Abstract: Alhagi, a plant genus from family Fabaceae, is widely distributed in many countries of Asia, Australia and Europe. Commonly known as camel thorn, Alhagi has many species famous for feed and folk medicinal uses. Different species of Alhagi such as Alhagi pseudalhagi, A. graecorum, A. sparsifolia, A. kirgisorum, A. maurorum, A. camelorum and A. persarum have been explored for their antioxidant potential and nutritive value along with various medicinal properties. A wide array of pharmacologically active secondary metabolites such as flavonoids, alkaloids (alhacidin and alhacin), steroids, pseudalhagin A, phospholipids and polysaccharides have been reported from different parts of Alhagi species. A broad range of biological activities such as antioxidant, cardiovascular, anti-ulcer, hepatoprotective, antispasmodic, antidiarrheal, antinociceptive, antipyretic, anti-inflammatory, anti-rheumatic, antibacterial and antifungal have been ascribed to different parts of Alhagi. In addition, Alhagi plants are also valued as a rich source of digestible protein and important minerals. This review focuses on the medicinal applications and detailed profile of high-value bioactive phytochemicals along with pharmacological attributes and therapeutic potential of these multi-purpose plants.
Publisher: Bangladesh Journals Online (JOL)
Date: 26-10-2012
Publisher: Elsevier BV
Date: 07-2017
Publisher: Elsevier BV
Date: 1998
Abstract: Esculetin, a phenolic compound found in Cichorium intybus and Bougainvllra spectabillis was investigated for its possible protective effect against paracetamol and CCl4-induced hepatic damage. Paracetamol produced 100% mortality at the dose of 1 g kg-1 in mice while pre-treatment of animals with esculetin (6 mg kg-1) reduced the death rate to 40%. Oral administration of paracetamol (640 mg kg-1) produced liver damage in rats as manifested by the rise in serum enzyme levels of alkaline phosphatase (ALP) and aminotransferases (AST and ALT). Pre-treatment of rats with esculetin (6 mg kg-1) prevented the paracetamol-induced rise in serum enzymes. The hepatotoxic dose of CCl4 (1.5 ml kg-1 orally) also raised serum ALP, AST and ALT levels. The same dose of esculetin (6 mg kg-1) was able to prevent the CCl4-induced rise in serum enzymes. Esculetin also prevented CCl4-induced prolongation in pentobarbital sleeping time confirming hepatoprotectivity. These results indicate that esculetin possesses anti-hepatotoxic activity and the presence of this compound in Cichorium intybus and Bougainvllra spectabillis may explain the folkloric use of these plants in liver damage.
Publisher: Elsevier BV
Date: 08-1997
DOI: 10.1016/S0306-3623(96)00413-2
Abstract: 1. The extract of Acacia nilotica (A. nilotica) blocked platelet aggregation mediated by platelet agonists, arachidonic acid (0.75 mM), ADP (4.3 microM), platelet activating factor (800 nM) and collagen (638 nM) in a dose-dependent manner. 2. The extract (0.21-1.4 mg/ml) blocked the platelet aggregation induced by Ca2+ ionophore, A-23187 (6 microM), in a dose-dependent manner, indicating that the Ca2+ influx is involved in aggregation. 3. The plant extract also inhibited aggregation in platelets pretreated with phorbol, 12-myristate, 13-acetate (196 nM) alone or in combination with ADP (4.3 microM), indicating an effect on protein kinase C. 4. These results indicate that the antiplatelet aggregatory activity of the extract of A. nilotica is mainly due to blockade of Ca2+ channels, although evidence also suggests the involvement of protein kinase C.
Publisher: Portland Press Ltd.
Date: 10-1988
DOI: 10.1042/BST0160815
Publisher: Elsevier BV
Date: 06-1999
DOI: 10.1016/S0278-6915(99)00039-3
Abstract: The potential of vanillin to potentiate the paracetamol and carbon tetrachloride (CCl4)-induced hepatotoxicity was investigated in rats. Vanillin when given alone (15 mg/kg, orally), did not modify liver function in rats as the values of serum enzymes of alkaline phosphatase (ALP) and aminotransaminases (AST and ALT) were found similar to those in the normal animals. However, when given repeatedly before the administration of the subtoxic dose of paracetamol (500 mg/kg) or CCl4 (1 ml/kg), vanillin caused liver damage, as manifested by the significant increase in the serum levels of hepatic enzymes. When tested for its possible interaction with pentobarbital (75 mg/kg, i.p.) and strychnine (0.9 mg/kg, i.p.), it caused reduction in pentobarbital-induced sleep in mice as well as preventing the animals against the lethal effect of strychnine, suggestive of an induction of microsomal drug metabolizing enzymes. These results indicate that vanillin potentiates the hepatotoxic potential of paracetamol and CCl4 in rats probably through an enzyme induction process.
Publisher: Informa UK Limited
Date: 26-08-2011
DOI: 10.3109/13880209.2010.494307
Abstract: This study describes the antispasmodic, bronchodilator, and cardiovascular-modulatory activities of Hypericum perforatum Linn. (Hypericaceae) fractions and constituents. Pharmacological investigation of H. perforatum fractions and active principles. H. perforatum extract fractions [petroleum spirit (HpPet), chloroform (HpCHCl(3)), ethyl acetate (HpEtAc), and aqueous (HpAq)] and its compounds (hyperforin, hypericin, and hyperoside) were studied in various isolated tissue preparations. In rabbit jejunum, HpCHCl(3), HpEtAc and HpAq, like papaverine, inhibited both spontaneous and K(+) (80 mM)-induced contractions at similar concentrations, whereas HpPet was relatively potent against K(+), as verapamil. All fractions caused rightward of Ca(2+) concentration-response curves (CRCs), similar to verapamil. HpCHCl(3), HpEtAc, and HpAq shifted isoprenaline-inhibitory CRCs to left, like papaverine, while HpPet was devoid of any such effect, as verapamil. In guinea-pig trachea, HpCHCl(3), HpEtAc, and HpAq equipotently relaxed carbachol and K(+)-induced contractions and shifted the isoprenaline-curves to the left, whereas HpPet was more effective against K(+), without potentiating isoprenaline effect. When tested in rabbit aorta, all fractions exhibited vasoconstrictor and vasodilator effects, except HpEtAc, which did not produce vasoconstriction. In guinea-pig atria HpCHCl(3), HpEtAc, and HpAq initially caused cardiac stimulation, followed by inhibition, similar to papaverine, whereas HpPet, like verapamil, caused only cardiac suppression. Hyperforin, hypericin, and hyperoside showed a similar pattern of spasmolytic effect to verapamil. Thus, all tested fractions of H. perforatum exhibit a combination of Ca(2+) antagonist and phosphodiesterase-inhibition, except petroleum spirit which was devoid of later mechanism. The compounds tested showed only Ca(2+) channel blocking effect.
Publisher: Springer Science and Business Media LLC
Date: 27-08-2020
Publisher: Ovid Technologies (Wolters Kluwer Health)
Date: 02-2015
Publisher: Bentham Science Publishers Ltd.
Date: 21-03-2017
Publisher: Springer Science and Business Media LLC
Date: 1986
DOI: 10.1007/BF00633191
Abstract: Cookies were produced from germinated pigeon pea, fermented sorghum, and cocoyam flour (CF) blends to determine their potentials in cookie manufacture. Ten flour formulations were produced and they were evaluated for their proximate and functional properties. Protein content ranged from 4.85% to 19.89% with 100% CF (100CF) having the least value, while 100% germinated pigeon pea flour (100GPF) had the highest value. Increase in levels of GPF to the flour blends resulted in increase in protein content of the blends. Cookies made with 100% fermented sorghum flour (100FSF) had the highest ash content of 2.73%, while cookies made with 100GPF had the least ash content. Energy values of the cookies ranged between 369.37 and 376.56 kcal/100 g, with cookie formulation 50%CF:50%FSF having the least value and cookies made with 16.7%CF:16.7%FSF:66.6GPF having the highest value. The control (cookies made with wheat) had the highest spread ratio of 24.13, while cookies made with 100FSF had the least spread ratio of 14.97. Cookies made with 100CF were the least fragile. Sensory ratings revealed that cookies containing up to 50% CF and above, compared favorably with those made with wheat flour.
Publisher: Portland Press Ltd.
Date: 11-1992
DOI: 10.1042/BST020347S
Publisher: Wiley
Date: 06-01-2014
DOI: 10.1002/PTR.5112
Abstract: This study evaluated the antispasmodic, bronchodilator and anti-platelet activities of Abies webbiana to rationalize some of its folk uses in gut and airways disorders and inflammation. The crude extract of A. webbiana (Aw.Cr) caused a complete relaxation of both spontaneous and K(+) (80 mM)-induced contractions in isolated rabbit jejunum in a concentration-dependent manner. Aw.Cr shifted the Ca(++) concentration-response curves (CRCs) to the right, in a fashion similar to verapamil, confirming its Ca(++) channel blocking (CCB) effect. In isolated rabbit tracheal preparations, it caused relaxation of carbachol (1 μM) and K(+) (80 mM)-induced contractions comparable to verapamil suggesting that the bronchodilatory effect may possibly be mediated through CCB activity. Aw.Cr was found to be the inhibitor of both ADP- and epinephrine-induced aggregation of human platelets thereby suggesting therapeutic potential in this plant against thrombo-embolic conditions. The exhibited anti-platelet effect was observed at low doses against epinephrine as compared to ADP. This study confirmed the presence of spasmolytic activity in Abies webbiana through possible blockade of Ca(++) channels providing evidence for its folkloric use in gut and respiratory disorders in addition to anti-platelet activity.
Publisher: Portland Press Ltd.
Date: 11-1992
DOI: 10.1042/BST020359S
Publisher: Elsevier BV
Date: 06-1995
DOI: 10.1016/0378-8741(95)01252-9
Abstract: The hepatoprotective activity of the aqueous-methanolic extract of Artemisia maritima was investigated against acetaminophen (paracetamol, 4-hydroxy acetanilide)- and carbon tetrachloride (CCl4)-induced hepatic damage. Acetaminophen produced 100% mortality at the dose of 1 g/kg in mice, while pretreatment of animals with the plant extract (500 mg/kg) reduced the death rate to 20%. Acetaminophen at the dose of 640 mg/kg produced liver damage in rats as manifested by the significant (P < 0.001) rise in serum levels of glutamate oxaloacetate transaminase (GOT) and glutamate pyruvate transaminase (GPT) to 1529 +/- 172 I.U./l and 904 +/- 116 I.U./l (n = 10), respectively, compared to respective control values of 87 +/- 12 I.U./l and 31 +/- 5 I.U./l. Pretreatment of rats with the plant extract (500 mg/kg) lowered significantly (P < 0.001) the respective serum GOT and GPT levels to 112 +/- 10 I.U./l and 47 +/- 11 I.U./l. Similarly, a hepatotoxic dose of CCl4 (1.5 ml/kg, orally) raised significantly (P < 0.01) the serum GOT and GPT levels to 463 +/- 122 I.U./l and 366 +/- 58 I.U./l (n = 10), respectively, compared to respective control values of 92 +/- 18 I.U./l and 35 +/- 9 I.U./l. The same dose of plant extract (500 mg/kg) was able to prevent significantly (P < 0.01) the CCl4-induced rise in serum transaminases and the estimated values of GOT and GPT were 105 +/- 29 I.U./l and 53 +/- 17 I.U./l, respectively. Moreover, it prevented CCl4-induced prolongation in pentobarbital sleeping time confirming hepatoprotectivity and validates the traditional use of this plant against liver damage.
Publisher: Springer Science and Business Media LLC
Date: 27-10-2021
Publisher: Elsevier BV
Date: 05-2023
Publisher: Elsevier BV
Date: 10-2005
DOI: 10.1016/J.VPH.2005.07.003
Abstract: Ginger is a world known food plant which is equally reputed for its medicinal properties. We report here the hypotensive, endothelium-dependent and independent vasodilator and cardio-suppressant and stimulant effects of its aqueous extract (Zo.Cr). Zo.Cr, which tested positive for saponins, flavonoids, amines, alkaloids and terpenoids, induced a dose-dependent (3.0-10.0 mg/kg) fall in the arterial blood pressure (BP) of anaesthetized rats which was partially blocked by atropine (1 mg/kg). In isolated endothelium-intact rat aorta, Zo.Cr (0.01-5.0 mg/ml) relaxed the phenylephrine (1 microM)-induced contractions, effect partially blocked by atropine (1 microM). Zo.Cr inhibited the K+ (80 mM)-induced contractions and also shifted the Ca++ dose-response curves to the right, similar to verapamil, indicating Ca++ antagonist activity. An atropine-resistant and l-NAME-sensitive vasodilator activity was also noted from ginger phenolic constituents 6-, 8- and 10-gingerol, while 6-shogaol showed a mild vasodilator effect. In guinea-pig atria, Zo.Cr (0.1-5.0 mg/ml) inhibited the force and rate of atrial contractions. Pretreatment with atropine blocked the inhibitory effect and a stimulatory effect was unmasked which was resistant to propranolol and verapamil but sensitive to ryanodine, blocker of Ca++ release from intracellular stores. Later at doses >or=1.0 mg/ml, the extract completely suppressed the atrial tissue, effect resistant to glibenclamide, pyrilamine, aminophylline and L-NAME. These data indicate that the aqueous ginger extract lowers BP through a dual inhibitory effect mediated via stimulation of muscarinic receptors and blockade of Ca++ channels and this study provides sound mechanistic basis for the use of ginger in hypertension and palpitations.
Publisher: Frontiers Media SA
Date: 08-01-2020
Publisher: Elsevier BV
Date: 09-2010
DOI: 10.1016/J.NEUROSCIENCE.2010.05.078
Abstract: Alzheimer's disease (AD) is a neurodegenerative disease. There are a limited number of therapeutic options available for the treatment of AD. Curcuminoids (a mixture of bisdemethoxycurcumin, demethoxycurcumin and curcumin) is the main chemical constituent found in turmeric, a well known curry spice, having potential in the treatment of AD. The objective of this study was to investigate the effects of curcuminoid mixture and in idual constituents on spatial learning and memory in an amyloid-beta (Abeta) peptide-infused rat model of AD and on the expression of PSD-95, synaptophysin and camkIV. Curcuminoid mixture showed a memory-enhancing effect in rats displaying AD-like neuronal loss only at 30 mg/kg, whereas in idual components were effective at 3-30 mg/kg. A shorter duration treatment with test compounds showed that the curcuminoid mixture and bisdemethoxycurcumin increased PSD-95 expression in the hippoc us at 3-30 mg/kg, with maximum effect at a lower dose (3 mg/kg) with respective values of 470.5 and 587.9%. However, after a longer duration treatment, two other compounds (demethoxycurcumin and curcumin) also increased PSD-95 to 331.7 and 226.2% respectively at 30 mg/kg. When studied for their effect on synaptophysin in the hippoc us after the longer duration treatment, the curcuminoid mixture and all three in idual constituents increased synaptophysin expression. Of these, demethoxycurcumin was the most effective showing a 350.1% increase (P<0.01) at 30 mg/kg compared to the neurotoxin group. When studied for their effect on camkIV expression after longer treatment in the hippoc us, only demethoxycurcumin at 30 mg/kg increased levels to 421.2%. These compounds salvaged PSD-95, synaptophysin and camkIV expression levels in the hippoc us in the rat AD model, which suggests multiple target sites with the potential of curcuminoids in spatial memory enhancing and disease modifying in AD.
Publisher: Science Alert
Date: 15-09-2013
Publisher: Elsevier BV
Date: 12-2011
DOI: 10.1016/J.JEP.2011.09.019
Abstract: The barks of Acacia leucophloea (Fabaceae) are used in Pakistan traditional medicine as an astringent, a bitter, a thermogenic, a styptic, a preventive of infections, an anthelmintic, a vulnery, a demulcent, an expectorant, an antipyretic, an antidote for snake bites and in the treatment of bronchitis, cough, vomiting, wounds, ulcers, diarrhea, dysentery, internal and external hemorrhages, dental caries, stomatitis, and intermittent fevers and skin diseases. A study was carried out for the possible elucidation of mechanisms justifying the traditional medicinal uses of A. leucophloea (Fabaceae) in gastrointestinal and respiratory diseases. In vitro experiments were carried out over isolated rabbit jejunum and guinea-pig ileum in order to determine spasmolytic and bronchorelaxant activities, while in vivo studies were conducted in mice for antidiarrheal properties. A methanol crude extract of barks of the plant caused a concentration-dependent relaxation (0.1-3 mg/ml) of isolated rabbit jejunum preparations in a pattern similar to that of nifedipine and dicyclomine, suggesting a Ca(2+) channel-blocking mechanism in addition to an anticholinergic effect. In guinea-pig ileum the extract caused a parallel shift in the Ach-curves without suppression of maximum contractile response, followed by a non-parallel shift with the suppression of maximum contractile response at higher concentration similar to that caused by dicyclomine. Moreover, in rabbit trachea, it also caused the relaxation of carbachol (1 μM) and high K(+)-induced contractions at a dose ranging between 0.1578 and 0.734 mg/ml and 0.46-0.94 mg/ml, respectively. These findings indicate that the extract possesses spasmolytic and bronchodilator activities, mediated possibly through blockade of Ca(2+) channels, thus justifying its medicinal use in diarrhea and asthma. Acacia leucophloea methanol extract exhibited dose-dependent (100-500 mg/ml) protective effect against castor oil induced diarrhea. The data obtained contribute to the validation of the traditional use of Acacia leucophloea bark in treating gastrointestinal and respiratory disorders, providing an hypothesis on the possible mechanisms of action.
Publisher: Elsevier BV
Date: 10-1999
DOI: 10.1016/S0006-2952(99)00206-3
Abstract: Curcumin, a dietary spice from turmeric, is known to be anti-inflammatory, anticarcinogenic, and antithrombotic. Here, we studied the mechanism of the antiplatelet action of curcumin. We show that curcumin inhibited platelet aggregation mediated by the platelet agonists epinephrine (200 microM), ADP (4 microM), platelet-activating factor (PAF 800 nM), collagen (20 microg/mL), and arachidonic acid (AA: 0.75 mM). Curcumin preferentially inhibited PAF- and AA-induced aggregation (IC50 25-20 microM), whereas much higher concentrations of curcumin were required to inhibit aggregation induced by other platelet agonists. Pretreatment of platelets with curcumin resulted in inhibition of platelet aggregation induced by calcium ionophore A-23187 (IC50 100 microM), but curcumin up to 250 microM had no inhibitory effect on aggregation induced by the protein kinase C (PKC) activator phorbol myrsitate acetate (1 microM). Curcumin (100 microM) inhibited the A-23187-induced mobilization of intracellular Ca2+ as determined by using fura-2 acetoxymethyl ester. Curcumin also inhibited the formation of thromboxane A2 (TXA2) by platelets (IC50 70 microM). These results suggest that the curcumin-mediated preferential inhibition of PAF- and AA-induced platelet aggregation involves inhibitory effects on TXA2 synthesis and Ca2+ signaling, but without the involvement of PKC.
Publisher: Elsevier BV
Date: 02-2008
DOI: 10.1016/J.JEP.2007.10.015
Abstract: Cardamom (Elettaria cardamomum) is traditionally used in various gastrointestinal, cardiovascular and neuronal disorders. To rationalize cardamom use in constipation, colic, diarrhea, hypertension and as diuretic. Cardamom crude extract (Ec.Cr) was studied using in vitro and in vivo techniques. Ec.Cr caused atropine-sensitive stimulatory effect in isolated guinea-pig ileum at 3-10mg/ml. In rabbit jejunum preparations, Ec.Cr relaxed spontaneous and K+ (80 mM)-induced contractions as well as shifted Ca++ curves to right, like verapamil. Ec.Cr (3-100mg/kg) induced fall in the arterial blood pressure (BP) of anaesthetized rats, partially blocked in atropinized animals. In endothelium-intact rat aorta, Ec.Cr relaxed phenylephrine (1 microM)-induced contractions, partially antagonized by atropine and also inhibited K+ (80 mM) contractions. In guinea-pig atria, Ec.Cr exhibited a cardio-depressant effect. Ec.Cr (1-10mg/kg) produced diuresis in rats, accompanied by a saluretic effect. It enhanced pentobarbital-induced sleeping time in mice. Bio-assay directed fractionation revealed the separation of spasmogenic and spasmolytic components in the aqueous and organic fractions respectively. These results indicate that cardamom exhibits gut excitatory and inhibitory effects mediated through cholinergic and Ca++ antagonist mechanisms respectively and lowers BP via combination of both pathways. The diuretic and sedative effects may offer added value in its use in hypertension and epilepsy.
Publisher: Springer Science and Business Media LLC
Date: 11-2006
DOI: 10.1007/BF02969283
Publisher: Georg Thieme Verlag KG
Date: 02-2005
Abstract: The aim of this investigation was to see if the crude extract of Sarcococca saligna (Ss.Cr) contains chemicals with gut function inhibitory activity by using in vitro and in vivo assays. Ss.Cr caused a dose-dependent (0.03 - 3 mg/mL) inhibitory effect on K+-induced contractions in rat stomach fundus, guinea-pig ileum and rabbit jejunum preparations. The calcium channel blocking(CCB) activity was confirmed when Ss.Cr caused a rightward shift in the Ca++ dose-response curves. It also potentiated, at lower do-ses (0.001 - 0.03 mg/mL), the contractile effect of a fixed dose of acetylcholine (ACh), similar to physostigmine, and suppressed the effect of ACh at higher doses (0.3 - 1.0 mg/mL). Both Ss.Cr and physostigmine inhibited acetylcholinesterase (AChE), in the in vitro assay, confirming the AChE inhibitory activity. In the in vivo studies, Ss.Cr exhibited antidiarrheal and antisecretory activities against castor oil-induced diarrhea and intestinal fluid accumulation in mice. Characteristic steroidal compounds of the plant (saracocine, saracodine, saracorine and alkaloid-C), exhibited a similar combination of AChE inhibitory and CCB activities. Thus this study provides a sound mechanistic base for some of the traditional uses of the plant in hyperactive gut states, in addition to providing the first evidence for verapamil to possess additional AChE inhibitory activity. Furthermore, these characteristic compounds with dual activity may be good candidates for further studies on their usefulness in Alzheimer's disease.
Publisher: Elsevier BV
Date: 2009
DOI: 10.1016/J.JEP.2008.11.004
Abstract: The study was aimed to investigate the chemical composition and pharmacological basis for traditional use of essential oil of Nepeta cataria L. (Limiaceae) (Nc.Oil) in gastrointestinal and respiratory disorders. Chemical analysis was carried out through GC-EIMS, 13C NMR and Kovats Retention Indices while pharmacological study was carried out in isolated tissues preparations. Four major components 1,8-cineol (21.00%), alpha-humulene (14.44%), alpha-pinene (10.43%) and geranyl acetate (8.21%) were identified among the 27 compounds in Nc.Oil. In isolated rabbit jejunum, Nc.Oil, papaverine and verapamil inhibited spontaneous and high K+(80 mM) precontractions, as well as shifted the Ca++ concentration-response curves (CRCs) to right, indicating calcium channel blocking activity. In isolated guinea-pig trachea, Nc.Oil and papaverine inhibited carbachol (1 microM) and K+ precontractions with similar potency, while verapamil was more potent against K+. Nc.Oil also potentiated isoprenaline inhibitory CRCs, similar to papaverine, indicating papaverine-like PDE inhibitor activity. In isolated guinea-pig atria, Nc.Oil caused cardiodepression at around 25-80 times higher concentrations, similar to papaverine. These data indicate that Nepeta cataria possesses spasmolytic and myorelaxant activities mediated possibly through dual inhibition of calcium channels and PDE, which may explain its traditional use in colic, diarrhea, cough and asthma.
Publisher: Elsevier BV
Date: 11-1999
DOI: 10.1016/S0306-3623(99)00035-X
Abstract: Berberis aristata is an edible plant employed in South Asian traditional medicine in particular, its fruit is used as a tonic remedy for liver and heart. In isolated cardiac tissues, Berberis aristata fruit extract exhibits a positive inotropic action. Activity-directed fractionation using organic solvents revealed that the cardiotonic activity is concentrated in the n-butanolic fraction (BF). The cardiac action of BF was investigated in spontaneously beating right atria and in electrically driven right ventricular strips and left atria obtained from reserpinized guinea pigs. The results show that this fraction produces a dose-dependent positive inotropic action with little effect on heart rate. To study its possible mode of action, guinea pig atria were pretreated with propranolol, a beta-adrenoceptor blocking agent. This treatment abolished the cardiotonic effect of isoprenaline, whereas the cardiotonic effect of BF remained unaltered, suggesting that this effect does not involve stimulation of beta-adrenoceptors. On the other hand, application of carbachol reverses only part of the BF-induced increase in ventricular force of contraction, indicating that besides a cyclic AMP (cAMP)-dependent mechanism, a cAMP-independent mechanism underlies the inotropic action of BF. This is in line with the observation that the dynamics of isometric twitch contractions are not significantly altered by BF. Investigations in skinned myocardial preparations showed that BF modulates the calcium-dependent interaction of actin and myosin, apparently by reducing the cooperativity of the calcium-dependent binding of myosin to actin, i.e., there is enhanced calcium activation at low to physiological intracellular calcium, and reduced calcium activation at high intracellular calcium concentrations as present, for ex le, in ischemic calcium overload. These data indicate that the edible plant, Berberis aristata, contains active principle(s) that cause(s) a selective inotropic effect, involving-in the form of the modulatory effect on actin myosin cooperativity-a novel mechanism of action. Further phytochemical and pharmacological studies may lead to isolation and structural identification of an attractive, new cardiotonic agent from Berberis aristata fruit.
Publisher: Portland Press Ltd.
Date: 11-1997
DOI: 10.1042/BST025S619
Abstract: As for other vestibular schwannomas, intralabyrinthine schwannomas commonly cause a sensorineural hearing loss, contrary to more lateral ear pathology that can cause conductive or mixed hearing loss. This case report features a patient that presented with a mixed and thus partly pseudo-conductive hearing loss due to an intracochlear schwannoma, a finding that is very rare. As a result, the patient was initially misdiagnosed as having otosclerosis and a stapedotomy was performed, without hearing improvement. We discuss the clinical implications of this atypical presentation, which illustrates the importance of performing supplementary audiological testing (e.g., the Gellé test), and the importance of considering vestibular system testing when otosclerosis is suspected. In addition, the importance of imaging and considering differential diagnoses in cases of conductive hearing loss is stressed.
Publisher: Wiley
Date: 14-05-2015
DOI: 10.1002/PTR.5367
Abstract: This study describes the antidiarrheal and antispasmodic activities of the hydro-alcoholic extract of Buddleja polystachya (Bp.Cr) with possible mode of action explored along with activity-directed fractionation. Bp.Cr and its aqueous (Bp.Aq) and organic fractions, petroleum ether (Bp.Pet), dichloromethane (Bp.DCM), ethylacetate (Bp.EtAc) and butanol (Bp.But), were tested using the in-vivo and in-vitro assays. The crude extract (100-300 mg/kg) showed 20 and 60% protection of castor oil-induced diarrhea in mice. In isolated rabbit jejunum, Bp.Cr like papaverine inhibited spontaneous and high K(+) (80 mM)-induced contractions equi-potently. In guinea-pig ileum, Bp.Cr showed a moderate spasmogenic effect. The activity-directed fractionation revealed that the spasmolytic activity was concentrated in the organic fractions and spasmogenic component in the aqueous fraction. Amongst the organic fractions, BP.DCM and Bp.Pet inhibited spontaneous and high K(+) -induced contractions equi-potently, while Bp.But, like verapamil was more potent against high K(+) . The crude extract and its organic fractions caused rightward shift in the Ca(++) -concentration response curves (CRCs), similar to verapamil, and all except Bp.But potentiated the isoprenaline-inhibitory CRCs to the left, similar to papaverine. The results of this study indicate that the crude extract of B. polystachya possesses antidiarrheal and antispasmodic activities, mediated possibly through dual inhibition of Ca(++) influx and phospodiesterase enzyme.
Publisher: Wiley
Date: 03-12-2009
DOI: 10.1002/PTR.3067
Abstract: The crude extract of Hypericum oblongifolium (Ho.Cr), which tested positive for flavonoids, saponins and tannins caused concentration-dependent (0.1-1.0 mg/mL) relaxation of spontaneous and high K(+) (80 mM)-induced contractions in isolated rabbit jejunum preparations, suggesting a Ca(++) antagonistic effect, which was confirmed when pretreatment of the tissue with Ho.Cr produced a rightward shift in the Ca(++) concentration-response curves, like that caused by verapamil. Ho.Cr relaxed carbachol (1 microM) and high K(+)-induced contractions in guinea pig tracheal preparations. It caused a dose-dependent (3-100 mg/kg) fall in arterial blood pressure of rats under anesthesia. In isolated guinea pig atria, Ho.Cr caused inhibition of both atrial force and rate of spontaneous contractions. When tested in rabbit aortic rings, Ho.Cr exhibited a vasodilator effect against phenylephrine (1 microM) and high K(+)-induced contractions. These results indicate that Ho.Cr possesses gastrointestinal, respiratory and cardiovascular inhibitory effects, mediated via a Ca(++) antagonist mechanism.
Publisher: Elsevier BV
Date: 12-2004
DOI: 10.1016/J.JSBMB.2004.08.003
Abstract: A new steroidal alkaloid, isosarcodine (1) along with four known bases, sarcorine (2), sarcodine (3), sarcocine (4) and alkaloid-C (5) were isolated from the MeOH extract of Sarcococca saligna. The structures of these alkaloids were identified by spectral data interpretation. These compounds were subjected to acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition studies, and were found to be noncompetitive inhibitors of AChE (Ki = 21.8, 90.3, 32.2, 16.0 and 50.0 microM, respectively) and uncompetitive or noncompetitive inhibitors of BChE (Ki = 8.3, 7.5, 15.6, 5.0 and 12.0 microM, respectively). The compounds (2-5) also showed dose-dependent spasmolytic activity in the rabbit jejunum intestinal preparations and also relaxed the high K+ (80 mM)-induced contraction, indicative of a calcium channel-blocking mechanism. Structure-activity relationship suggested that the nitrogen substituents at C-3 and/or C-20 of steroidal skeleton and the hydrophobic properties of the pregnane skeleton are the key structural features contributed to the inhibitory potency of these steroidal alkaloids against AChE and BChE.
Publisher: Wiley
Date: 2007
DOI: 10.1002/PTR.2098
Abstract: This study was carried out to provide a scientific basis for the traditional use of Saussurea lappa, in constipation and spasms. Isolated tissue preparations were used to see if the aqueous-methanol crude extract of the S. lappa root (Sl.Cr) contains gut stimulatory and inhibitory constituents. In isolated guinea-pig ileum, a quiescent preparation, Sl.Cr caused a concentration-dependent (0.3-5.0 mg/mL) spasmogenic effect, with the maximum effect reaching 91% of the acetylcholine maximum. A further increase in concentration caused a declining effect, indicating the presence of spasmolytic constituent(s). The spasmolytic effect was more marked in the spontaneously contracting rabbit jejunum and in the atropinized preparations. The spasmolytic effect was mediated through calcium channel blocking (CCB) activity, as evident by its inhibitory effect against high K(+) (80 mm)-induced contraction and displacement of the Ca(++) concentration-response curves to the right. These data indicate that the crude extract of Sl.Cr contains gut stimulatory constituent(s) of cholinergic-type providing a scientific basis for its use in constipation. The presence of spasmolytic constituents of CCB-type more evident in the spontaneous contracting gut preparation may explain its use in spasms.
Publisher: Informa UK Limited
Date: 2008
Publisher: Portland Press Ltd.
Date: 11-1997
DOI: 10.1042/BST025S618
Abstract: Establish outcomes following cochlear implantation (CI) in patients following temporal bone trauma. Systematic review and narrative synthesis. Medline, Pubmed, Embase, Web of Science, Cochrane Collection, and ClinicalTrials.gov. No limits are placed on language or year of publication. The review conducted in accordance with the PRISMA statement. Searches identified 223 abstracts and 64 full texts. Of these, 23 studies met the inclusion criteria reporting outcomes in 77 patients with at least 96 implants. Hearing outcomes were generally good with most patients demonstrating improved audiological and functional outcomes. Complications were reported in 14 cases with 10 of these being major. The methodological quality of included studies was modest, predominantly consisting of case reports and non-controlled case series with small numbers of patients. All studies were OCEBM grade IV. Hearing outcomes following CI in temporal bone trauma are good with useful functional improvement demonstrated in the majority of patients. It appears to be an effective method of aural rehabilitation and should be considered in selected cases following hearing loss due to temporal bone fracture.
Publisher: SAGE Publications
Date: 05-10-2022
DOI: 10.1177/08903344211034779
Abstract: There is evidence that breastfeeding may provide protection against cardiovascular risk factors in mothers with a history of gestational diabetes mellitus and their children who were exposed in utero. To perform a systematic review and meta-analysis of observational studies to ascertain the effects of breastfeeding on cardiovascular risk factors in women with previous gestational diabetes mellitus and their children exposed in utero. Studies assessing conventional cardiovascular risk factors in women with previous gestational diabetes mellitus and children exposed in utero stratified by breastfeeding/no breastfeeding or breastfed/not breastfed were included. Gestational diabetes mellitus was defined based on the International Association of Diabetes in Pregnancy Study Group definition or previous accepted definitions. Breastfeeding was defined as reported in each study. The literature search yielded 260 titles, of which 17 studies were selected to be in the review. Women with previous gestational diabetes mellitus who did not breastfeed had higher blood glucose ( SMD: 0.32, 95% CI [0.12, 0.53]) and a greater risk of developing Type 2 diabetes mellitus ( RR: 2.08 95% CI [1.44, 3.00]) compared to women with no history. There were not enough studies to conduct a meta-analysis on the effects of breastfeeding on risk factors for cardiovascular disease among children exposed to gestational diabetes mellitus in utero. Breastfeeding appears to be protective against cardiovascular risk factors among women who experience gestational diabetes mellitus.
Publisher: Science Alert
Date: 15-12-2006
Publisher: Wiley
Date: 20-10-2020
DOI: 10.1002/EMP2.12276
Publisher: Springer Science and Business Media LLC
Date: 03-1992
DOI: 10.1007/BF02973992
Publisher: Springer Science and Business Media LLC
Date: 24-05-2012
Publisher: Hindawi Limited
Date: 2015
DOI: 10.1155/2015/313821
Publisher: Bangladesh Journals Online (JOL)
Date: 14-07-2015
Abstract: class="Abstract" em Polygonum bistorta /em is a popular medicinal herb used to treat diarrhea. This study provides pharmacological basis to its folk use in diarrhea using em in vivo /em and em in vitro /em assays. Administration of em P. bistorta /em rhizomes extract to mice offered protection against castor oil-induced diarrhea at 300-1,000 mg/kg and was found safe up to the dose of 5 g/kg. In isolated rabbit jejunum, the extract caused a dose-dependent relaxation of spontaneous and low K sup + /sup (25 mM)-induced contractions with weak effect against high K sup + /sup (80 mM). In tissues pretreated with glibenclamide or tetraethylammonium chloride (TEA), the relaxant effect of the extract was markedly inhibited by TEA only. While verapamil showed complete relaxation of spontaneous, low K sup + /sup , low K sup + /sup with TEA and high K sup + /sup -induced contractions. In guinea-pig ileum, mild atropine-sensitive effect was observed. This study indicates that em P. bistorta /em possesses anti-diarrheal and antispasmodic activities mediated predominantly through K sup + /sup -channels activation along with weak Ca sup ++ /sup antagonist effect.
Publisher: Hindawi Limited
Date: 2012
DOI: 10.1155/2012/305319
Abstract: Thymoquinone (TQ) is a bioactive component found in many medicinal herbs. In this study, we report the smooth and cardiac muscle relaxant activities of this compound. TQ concentration dependently suppressed spontaneously contracting rabbit jejunum while also relaxed high K + -(80 mM) induced contractions in jejunum and guinea-pig ileum, indicating activity at voltage-operated Ca ++ channels (VOCC). Further, TQ displaced Ca ++ concentration-response curves, obtained in a Ca ++ -free environment, to the right, showing blockade of VOCC. Similar activity was observed with verapamil, a standard VOCC blocker. TQ also exhibited nonadrenergic relaxation of agonist-induced contractions in guinea-pig trachea. When tested in fluo-4-loaded mouse lung slices, TQ inhibited ACh-induced airway narrowing and Ca ++ signalling in airway smooth muscle cells. In endothelium-intact and endothelium-denuded rat aorta, TQ inhibited high K + -induced contractions at significantly lower concentrations than phenylephrine-(PE-) (1 microM) induced contractions. Relaxation of PE-induced contractions was resistant to blockade by L-NAME and atropine. In guinea-pig atria, TQ showed noncholinergic relaxation of atrial force and rate of contractions. These data suggest smooth and cardiac muscle relaxant activity of TQ possibly mediated, in part, via blockade of VOCC. The results also justify the use of TQ containing plants in related health disorders like colic, diarrhoea, cough, and asthma.
Publisher: Wiley
Date: 10-03-2014
DOI: 10.1002/PTR.5136
Abstract: Crude extract of Lens culinaris (Lc.Cr), which tested positive for presence of anthraquinones, flavonoids, saponins, sterol, tannins, and terpenes exhibited protective effect against castor oil-induced diarrhea in mice at 100-1000 mg/kg. In rabbit jejunum preparations, Lc.Cr caused relaxation of spontaneous contractions at 0.03-5.0 mg/mL. Lc.Cr inhibited carbachol (CCh, 1 μM) and K(+) (80 mM)-induced contractions in a pattern similar to dicyclomine, but different from verapamil and atropine. Lc.Cr shifted the Ca(++) concentration-response curves to the right, like dicyclomine and verapamil. Pretreatment of tissues with Lc.Cr (0.03-0.1 mg/mL) caused leftward shift of isoprenaline-induced inhibitory CRCs, similar to papaverine. In guinea-pig ileum, Lc.Cr produced rightward parallel shift of CCh curves, followed by non-parallel shift at higher concentration with suppression of maximum response, similar to dicyclomine, but different from verapamil and atropine. Lc.Cr (3.0-30 mg/kg) caused suppression of carbachol (CCh, 100 µg/kg)-induced increase in inspiratory pressure of anesthetized rats. In guinea-pig trachea, Lc.Cr relaxed CCh and high K(+) -induced contractions, shifted CCh curves to right and potentiated isoprenaline response. These results suggest that L. culinaris possesses antidiarrheal, antispasmodic, and bronchodilator activities mediated possibly through a combination of Ca(++) antagonist, anticholinergic, and phosphodiesterase inhibitory effects, and this study provides sound mechanistic background to its medicinal use in disorders of gut and airways hyperactivity, like diarrhea and asthma.
Publisher: Springer Science and Business Media LLC
Date: 08-2011
DOI: 10.1007/S12272-011-0801-0
Abstract: This study describes the chemical composition of the essential oil of Artemisia maritima (Am.Oil) and the pharmacological basis for its medicinal use in gut and airways disorders. Twenty five compounds, composing 93.7% of the oil, were identified among these, chrysanthenyl propionate and elixene were identified for the first time from any Artemisia species. The Am.Oil (0.3-1.0 mg/mL) suppressed spontaneous and high K(+) (80 mM)-induced contractions in isolated rabbit jejunum, suggestive of an antispasmodic effect mediated possibly through calcium channel blockade. The calcium channel blockade activity was confirmed when pre-treatment of the tissue with Am.Oil (0.01-0.03 mg/mL) shifted the Ca(++) concentration-response curves to the right, similar to verapamil and papaverine. In isolated tracheal strips, Am.Oil inhibited carbachol (CCh 1 μM)-induced contractions more than that induced by K(+) and shifted the isoprenaline-induced inhibitory CRCs to the left, similar to papaverine, suggestive of potentiation, while, verapamil was more potent against K(+) than CCh-induced contractions and had no potentiating effect on isoprenaline-induced inhibitory CRCs. These data indicate that the Am.Oil exhibited spasmolytic and bronchodilator activities mediated possibly through dual blockade of calcium channels and phosphodiesterase, which provides the pharmacological basis to the medicinal use of Artemisia maritima in colic, diarrhea and possibly asthma.
Publisher: Bangladesh Journals Online (JOL)
Date: 12-2014
Publisher: Elsevier BV
Date: 11-2018
Publisher: Wiley
Date: 17-06-2010
DOI: 10.1002/PTR.3196
Abstract: Berberis vulgaris is a widely used plant for the treatment of urolithiasis. To evaluate its antiurolithic potential, the crude aqueous-methanol extract of Berberis vulgaris root bark (Bv.Cr) was tested in an animal model of urolithiasis, developed in male Wistar rats by adding 0.75% ethylene glycol in drinking water. Bv.Cr (50 mg/kg) inhibited CaOx crystal deposition in renal tubules and protected against associated changes including polyuria, weight loss, impaired renal function and the development of oxidative stress in kidneys. Activity-guided fractionation revealed the concentration of antiurolithic constituent(s) mainly in the aqueous fraction. These data, indicating the presence of antiurolithic activity in Berberis vulgaris root bark, rationalize its medicinal use for the treatment of urolithiasis.
Publisher: Elsevier BV
Date: 10-2015
Abstract: More than one-half of coronary artery disease (CAD) patients have low HDL cholesterol despite having well-managed LDL cholesterol. Almond supplementation has not been shown to elevate circulating HDL cholesterol concentrations in clinical trials, perhaps because the baseline HDL cholesterol of trial subjects was not low. This clinical trial was designed to test the effect of almond supplementation on low HDL cholesterol in CAD patients. A total of 150 CAD patients (50 per group), with serum LDL cholesterol ≤100 mg/dL and HDL cholesterol ≤40 mg/dL in men and ≤50 mg/dL in women, were recruited from the Aga Khan University Hospital. After recording vital signs and completing a dietary and physical activity questionnaire, patients were randomly assigned to 1 of the following 3 groups: the no-intervention group (NI), the Pakistani almonds group (PA), and the American almonds group (AA). The respective almond varieties (10 g/d) were given to patients with instructions to soak them overnight, remove the skin, and eat them before breakfast. Blood s les for lipid profiling, body weight, and blood pressure were collected, and assessment of dietary patterns was done at baseline, week 6, and week 12. Almonds significantly increased HDL cholesterol. At weeks 6 and 12, HDL cholesterol was 12-14% and 14-16% higher, respectively, in the PA and AA than their respective baselines. In line with previous reports, serum concentrations of total cholesterol, triglycerides, LDL cholesterol, and VLDL cholesterol total-to-HDL and LDL-to-HDL cholesterol ratios, and the atherogenic index were reduced in both the PA and AA at weeks 6 and 12 compared with baseline (P < 0.05). Effects on serum lipids did not differ between the 2 almond groups. Dietary patterns, body weight, and blood pressure did not change in any of the 3 groups during the trial. A low dose of almonds (10 g/d) consumed before breakfast can increase HDL cholesterol, in addition to improving other markers of abnormal lipid metabolism in CAD patients with low initial HDL cholesterol. This trial was registered at the Australian New Zealand Clinical Trial Registry as ACTRN12614000036617.
Publisher: Hindawi Limited
Date: 05-04-2022
DOI: 10.1155/2022/4849464
Abstract: Background and Objective. Trigonella foenum-graecum Linn., also called fenugreek, is a popular medicinal plant cultivated all over the globe. Fenugreek seeds are known for their many medicinal properties. We present our findings on the effect of a 70% aqueous methanolic fenugreek seed extract (Tfg.Cr) on isolated GI smooth muscles (rabbit jejunum and rat ileum) and the effect of extract and its constituent diosgenin on acetylcholinesterase (AChE) enzyme. Results. When tested on the baseline of isolated tissues, Tfg.Cr was devoid of any activity (stimulant or relaxant) till 10 mg/ml. This is an interesting finding, keeping in mind that the fenugreek seeds are used to alleviate constipation and diarrhoea. When Tfg.Cr was tried for any potential AChE inhibitory activity, it did show an inhibitory effect in increasing concentrations (47-380 μg/ml). This inhibitory effect was comparable to the effect produced by a standard AChE inhibitor physostigmine. One of the known fenugreek constituents, diosgenin, was also tested, and it also showed an AChE inhibitory effect in a concentration-dependent manner (11-190 μg/ml). Interaction between diosgenin and AChE was further investigated by molecular docking and molecular dynamics simulations for 100 ns, which showed that diosgenin interacted with the active-site gorge of AChE through hydrophobic, pi-pi stacking, and hydrogen bonds with various amino acids of the AChE enzyme. Conclusion. The results show that the fenugreek extract does not possess any GI stimulant or relaxant activity even though it is used traditionally in GI motility disorders. The extract and diosgenin could inhibit the AChE enzyme pointing towards their benefit to enhance the memory.
Publisher: Canadian Science Publishing
Date: 05-2008
DOI: 10.1139/Y08-030
Abstract: Asthma is a chronic disease characterized by inflammation and hypersensitivity of airway smooth muscle cells (ASMCs) to different spasmogens. The past decade has seen increased use of herbal treatments for many chronic illnesses. Ginger ( Zingiber officinale ) is a common food plant that has been used for centuries in treating respiratory illnesses. In this study, we report the effect of its 70% aqueous methanolic crude extract (Zo·Cr) on acetylcholine (ACh)-induced airway contraction and Ca 2+ signalling in ASMCs using mouse lung slices. Airway contraction and Ca 2+ signalling, recorded via confocal microscopy, were induced with ACh, either alone or after pretreatment of slices with Zo·Cr and (or) verapamil, a standard Ca 2+ channel blocker. ACh (10 μmol/L) stimulated airway contraction, seen as decreased airway diameter, and also stimulated Ca 2+ transients (sharp rise in [Ca 2+ ] i ) and oscillations in ASMCs, seen as increased fluo-4-induced fluorescence intensity. When Zo·Cr (0.3–1.0 mg/mL) was given 30 min before ACh administration, the ACh-induced airway contraction and Ca 2+ signalling were significantly reduced. Similarly, verapamil (1 μmol/L) also inhibited agonist-induced airway contraction and Ca 2+ signalling, indicating a similarity in the modes of action. When Zo·Cr (0.3 mg/mL) and verapamil (1 μmol/L) were given together before ACh, the degree of inhibition was the same as that observed when each of these blockers was given alone, indicating absence of any additional inhibitory mechanism in the extract. In Ca 2+ -free solution, both Zo·Cr and verapamil, when given separately, inhibited Ca 2+ (10 mmol/L)-induced increase in fluorescence and airway contraction. This shows that ginger inhibits airway contraction and associated Ca 2+ signalling, possibly via blockade of plasma membrane Ca 2+ channels, thus reiterating the effectiveness of this age-old herb in treating respiratory illnesses.
No related grants have been discovered for Anwar Gilani.