ORCID Profile
0000-0001-6592-4210
Current Organisation
West China Hospital, Sichuan University
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Publisher: Bentham Science Publishers Ltd.
Date: 2022
DOI: 10.2174/0929867328666210623150552
Abstract: 6-Fluoro-3-(4H-1,2,4-triazol-3-yl)quinolin-4(1H)-ones are promising antitumor agents with enormous data on their profound cytotoxic effects on the human cancer cell lines. We sought to perform a Quantitative structure cytotoxicity relationship (QSCR) analysis of a series of previously reported fluoroquinolone analogues using computerassisted multiple regression analysis and investigate the cytotoxicity-inducing structural parameters among these congeners. The dataset was segregated into training and test sets of 6-Fluoro-3-(4H-1,2,4- triazol-3-yl)quinolin-4(1H)-ones by using a random selection method embedded in Vlife MDS 4.6 software and subjected to QSCR analysis. Next, cross-validation of the generated QSCR models was performed along with the external test set prediction. Finally, the data was analyzed and contour plots were developed to deduce the cytotoxicity-inducing structural parameters among these congeners using Minitab® software. The validated QSCR model exhibited a statistically significant predictive value of 92.27 percent. Our QSCR model revealed a direct proportionality between hydrogen counts and cytotoxicity, and exclusion of sulphur and nitrogen with lesser crowding of cyclopropyl rings in future potential 6-Fluoro-3-(4H-1,2,4-triazol-3-yl)quinolin-4(1H)-one analogues. Based on the QSCR model predictions and contour plot analysis, the de novo REPUBLIC1986 molecule provided the best hit with predicted IC50 (μM) of 0.45 against CHO cell line and is amenable to salt formation crucial for anti-ovarian cancer activity. These findings suggest the relevancy of the developed QSCR model in designing novel, potent, and safer anti-cancer drugs with 6-Fluoro-3-(4H-1,2,4-triazol-3-yl)quinolin- 4(1H)-ones as seed compounds.
Publisher: MDPI AG
Date: 06-02-2023
Abstract: As the world’s most prevalent cancer, breast cancer imposes a significant societal health burden and is among the leading causes of cancer death in women worldwide. Despite the notable improvements in survival in countries with early detection programs, combined with different modes of treatment to eradicate invasive disease, the current chemotherapy regimen faces significant challenges associated with chemotherapy-induced side effects and the development of drug resistance. Therefore, serious concerns regarding current chemotherapeutics are pressuring researchers to develop alternative therapeutics with better efficacy and safety. Due to their extremely biocompatible nature and efficient destruction of cancer cells via numerous mechanisms, phytochemicals have emerged as one of the attractive alternative therapies for chemotherapeutics to treat breast cancer. Additionally, phytofabricated nanocarriers, whether used alone or in conjunction with other loaded phytotherapeutics or chemotherapeutics, showed promising results in treating breast cancer. In the current review, we emphasize the anticancer activity of phytochemical-instigated nanocarriers and phytochemical-loaded nanocarriers against breast cancer both in vitro and in vivo. Since erse mechanisms are implicated in the anticancer activity of phytochemicals, a strong emphasis is placed on the anticancer pathways underlying their action. Furthermore, we discuss the selective targeted delivery of phytofabricated nanocarriers to cancer cells and consider research gaps, recent developments, and the druggability of phytoceuticals. Combining phytochemical and chemotherapeutic agents with nanotechnology might have far-reaching impacts in the future.
Publisher: Bentham Science Publishers Ltd.
Date: 31-01-2019
DOI: 10.2174/1568026619666181224111319
Abstract: Inflammation and oxidative stress are very closely related to pathophysiological processes and linked to multiple chronic diseases. Traditionally, the coconut fruits were used in Guatemala for treatment of dermatitis and inflammation. Isolation of the anti-inflammatory agent from the hard shell of the coconut fruit was targeted in the current study. Fractionation of ethanolic extract of the coconut hard shell was done by using column chromatography, solvent treatments and TLC that led to the isolation of a molecule. Spectral characterization of the molecule by LC-MS/MS QTOF, FTIR, 1HNMR, 13C-NMR, HMQC and HMBC indicated that it is a novel keto fatty acid, which is named as nuciferoic acid. Hyaluronidase inhibitory potential of the nuciferoic acid was found to be moderate. It was further docked in all the ten cavities of hyaluronidase and was compared with the substrate hyaluronic acid. Cavity 1 and cavity 4 could be the probable sites of action on hyaluronidase for nuciferoic acid. ADME and toxicological characterization suggested that the key sites of metabolism on nuciferoic acid are C1, C2, C14 and C17. Toxicity prediction against 55 toxicological endpoints revealed that nuciferoic acid does not have any indication of existing toxicological features. A novel keto fatty acid, nuciferoic acid, from C. nucifera hard shell has been isolated and characterized. It was found to inhibit hyaluronidase activity, which indicated its potential application as an anti-inflammatory drug or as an adjuvant.
Publisher: Instituto de Investigaciones Sociales
Date: 23-08-2023
DOI: 10.21670/REF.2312123
Abstract: Se analizan contenidos alusivos a migración, respeto hacia la ersidad cultural, nacionalismo y chilenidad en currículos de las asignaturas historia, geografía y ciencias sociales y lenguaje y comunicación/lengua y literatura, implementados en escuelas urbanas y rurales de la región trifronteriza de Arica y Parinacota (norte de Chile) con mayor concentración de estudiantes de origen andino o afro e hijos nacidos en Chile de padres inmigrantes. A través del análisis de contenido temático, con el programa QSR-Nvivo 12, se examina el corpus de programas de estudio y textos escolares utilizados en siete niveles educativos, desde sexto año de enseñanza básica hasta cuarto año de enseñanza media, entre 2018 y 2020. Los resultados revelan la escasez de contenidos sobre migración y ersidad cultural los contenidos sobre chilenidad y nacionalismo remiten a tensiones y disputas políticas ─presentes y pasadas─ entre Chile y los países vecinos, donde predomina una posición nacionalista de soberanía. Se concluye que los currículos no presentan pertinencia cultural para la región trifronteriza.
Publisher: Bentham Science Publishers Ltd.
Date: 28-11-2017
DOI: 10.2174/1381612823666170823103830
Abstract: Andropause or male menopause is defined as androgen decline and onset of hypogonadism in the aging male. Testosterone deficiency in adult male is associated with diabetes mellitus, coronary artery disease, and heart failure. Type 2 diabetic male patients aged above 30 years showed low testosterone levels which is common in diabetic men and had symptoms of hypogonadism. Male sexual dysfunction among diabetic patients can include disorders of libido, ejaculatory problems, and erectile dysfunctions are common among people with diabetes, particularly in older men who had diabetes for years. Older diabetics tend to have both impaired insulin release as well as insulin resistance. There is growing evidence indicating the pathophysiological connections among the mechanisms of oxidative damage by disruption of the oxidative balance, increased levels of enzymatic glycation products in testicular region and glucose transporters, obesity and proinflammatory cytokines in male infertile patients with diabetes. Epidemiological studies suggest that many clinical findings in diabetics are linked to low testosterone levels. This article reviews pathophysiological mechanisms, observational studies, and clinical implications of testosterone therapy in type 2 diabetes mellitus.
Location: Chile
Location: India
Location: India
No related grants have been discovered for Rodolfo Bastián Valle-Kendall.