ORCID Profile
0000-0002-4569-2317
Current Organisation
Monash University
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Publisher: MDPI AG
Date: 06-05-2020
DOI: 10.3390/MOLECULES25092171
Abstract: Natural product studies explore potential and interesting new compounds to discover innovative drugs. Nigella sativa (N. sativa) (Ranunculaceae) is traditionally used to treat diabetes. Flavonoids and triterpenoid mostly show anti-diabetic activity. The current study aim to identify new compounds by a systematic study of the anti-oxidant and anti-diabetic activity of aerial parts of N. sativa concerning. Phytochemicals were isolated from the methanolic extract of aerial parts of the plant by column chromatography and identified by nuclear magnetic resonance spectroscopy and mass spectroscopy. A new triterpenoid saponin glycoside was isolated along with flavonoids. The anti-diabetic study was carried out by DPPH, ABTS, α -glucosidase, and protein tyrosine phosphatase 1B assays at doses of 12.5 to 250 µM. The isolated phytochemicals were identified as 3-O-(β-d-xylopyranosyl-(1-3)-α-l-rhamnopyrnaosyl-(1-2)-α-l-arabinopyranosyl]-28-O-(α-l-rhamno-pyranosyl-(1-4)-β-d-glucopyranosyl-(1-6)-β-d-glucopyranosyl] hederagenin (1), flaccidoside III (2), catechol (3), quercetin-3-gentiobiosides (4), magnoflorine (5), nigelflavonoside B (6), nigelloside (7), quercetin sphorotrioside (8), kaempferol-3, 7-diglucoside (9), kaempferol 3-O-rutinoside (10), rutin (11), 3-O-[α-l-rhamnopyranosyl-(1→2)-α-l-arabinopyranpsylhederagenin (12), 3β,23,28-trihydroxyolean-12-ene-3-O-α-l-arabinopyranoside(1→4)-a-rhamnopyranosyl,(1→4)-β-d-gluco-pyranoside (13), 3-O-α-l-rhamnopyranosyl-(1→2)-α-l-arabinopyranpsyl]-28-O-β-d-gluco-pyranosyl hederagenin (14), and α-hederin (15). These were isolated and are reported for the first time in this study. Compared 13 was identified as a new compound. Compound 2 was isolated for first time from the genus Nigella. Compound 6 was found to be the most active in the DPPH, and ABTS assays and compound 10 was found to be the most active in the α-glucosidase assay, with IC50 32.7 ± 0.1, 95.18 ± 0.9, 214.5 ± 0.0 µΜ, respectively. Compound 12, at a dose of 125 µΜ, showed anti-diabetic activity in a PTP1B assay with IC50 91.30 ± 2.5 µΜ. In conclusion, the anti-diabetic activity of N. sativa is due to its flavonoids and TTSGs. Therefore, our studies suggest that the aerial parts of N. sativa are also a valuable and alternate source of valuable phytochemicals that could be used to develop anti-oxidant and anti-diabetic medicines.
Publisher: Informa UK Limited
Date: 08-2019
DOI: 10.1080/07391102.2019.1647287
Abstract: Tyrosinase plays an important role in melanin biosynthesis and protects skin against ultraviolet radiations. Functional deficiency of tyrosinase results in serious dermatological diseases. Tyrosinase also participates in neuromelanin formation in the human brain, which leads to neurodegeneration resulting in Parkinson's disease. In fruits and vegetables, tyrosinase plays a critical role in senescence, causing undesired browning that results in faster deterioration and shorter shelf lines. The only commercially available tyrosinase is mushroom tyrosinase and it shows the highest homology to the mammalian tyrosinase. Although kojic acid is currently used as a tyrosinase inhibitor, they have serious side effects such as dermatitis, carcinogenesis and hepatotoxicity. Therefore, in order to develop a more active and safer tyrosinase inhibitor, 3D QSAR pharmacophore models were generated based on experimentally known inhibitors. The pharmacophore model, Hypo1, was developed with a large cost difference, high correlation coefficient and low RMS deviation. Hypo1 showed a good spatial arrangement consisting of five-point features including two hydrogen bond acceptor, one hydrogen bond donor and two hydrophobic features. Hypo1 was further validated by cost analysis, test set and Fisher's randomisation method. Hypo1 was used as a 3D query for screening the in-house drug-like databases, and the hits were further selected by applying ADMET, Lipinski's rule of five and fit value criteria. To identify binding conformations, the obtained hits were subjected to molecular docking. Finally, molecular dynamics simulations revealed the appropriate binding modes of hit compounds. To conclude, we propose the final three hit compounds with new structural scaffolds as a virtual candidate as tyrosinase inhibitors.Communicated by Ramaswamy H. Sarma.
Publisher: Wiley
Date: 19-08-2019
DOI: 10.1002/JBM.A.36770
Abstract: For cancer therapy, the usefulness of mesoporous silica nanoparticles (MPSNPs) has been widely discussed, likely due to its inorganic nature and excellent structural features. The MPSNPs-based chemotherapeutics have been promisingly delivered to their target sites that help to minimize side effects and improve therapeutic effectiveness. A wide array of studies have been conducted to functionalize drug-loaded MPSNPs using targeting ligands and stimuli-sensitive substances. In addition, anticancer drugs have been precisely delivered to their target sites using MPSNPs, which respond to multi-stimuli. Furthermore, MPSNPs have been extensively tested for their safety and compatibility. The toxicity level of MPSNPs is substantially lower as compared to that of colloidal silica however, in oxidative stress, they exhibit cytotoxic features. The biocompatibility of MPSNPs can be improved by modifying their surfaces. This article describes the production procedures, functionalization, and applications of biocompatible MPSNPs in drug delivery.
Publisher: Springer Science and Business Media LLC
Date: 08-06-2020
Publisher: Springer International Publishing
Date: 05-08-2021
Publisher: Springer Science and Business Media LLC
Date: 07-06-2019
Publisher: Springer International Publishing
Date: 05-08-2020
Publisher: Springer Science and Business Media LLC
Date: 30-03-2020
Publisher: World Scientific Pub Co Pte Ltd
Date: 2020
DOI: 10.1142/S0192415X20500147
Abstract: Many cultivated and wild plants are used for the management of various diseases, specifically renal and hepatic diseases and those of the immune and cardiovascular systems. In China, medicinal plants from ancient to modern history have been used in patients with angina pectoris, congestive heart failure (CHF), systolic hypertension, arrhythmia, and venous insufficiency for centuries. The latest increase in the fame of natural products and alternative medicine has revived interest in conventional remedies that have been consumed in the management of CVD. The cardio-protective properties of the various herbs are possibly due to their anti-oxidative, antihypercholesterolemic, anti-ischemic activities, and inhibition of platelet aggregation that reduce the risk of CVD. Ethno-pharmacological and biological properties of these plants are explored, based upon published scientific literature. Although a majority of medicinal plants having a biological mechanism that linked with CVD management, to date, published literature pertaining to their promising scientific properties are still poorly understood. Compared with synthetic medicines, alternative medicines do not need scientific studies before their formal approval from the government sector and due to this purpose their safety, as well as efficacy, still remain elusive. Taken together, we addressed all accessible evidence on alternative medicines commonly consumed in CVD management. Our comprehensive analysis of the scientific literature indicated that many TCMs are available and valuable herbal medication would be the best alternative for the management of CVD as a complementary therapy. Furthermore, practitioners should always discuss possible benefits–risks of alternative medicines with patients so that they are aware of the consumption of alternative medications.
Publisher: Wiley
Date: 12-11-2020
DOI: 10.1002/PAT.4763
Publisher: Elsevier BV
Date: 03-2021
Publisher: Springer Science and Business Media LLC
Date: 09-03-2020
Publisher: Informa UK Limited
Date: 19-05-2021
DOI: 10.1080/02652048.2021.1915398
Abstract: Current study aimed to improve the solubility and release profile of the celecoxib for cancer application. However, the low water solubility of celecoxib limited its application for cancer chemotherapy. Hence, new drug delivery-based approaches are compulsory for the efficient delivery of hydrophobic celecoxib for chemotherapy. The celecoxib-loaded nanocrystals were prepared by anti-solvent precipitation-ultrasonication technique, and the formulation was optimised through various process parameters. The optimised formulation had an average particle diameter of 171.09 ± 6.23 nm, with a PDI of 0.123 ± 0.009 and high ZP -27.3 ± 0.2 mV. The optimised formulation was stable, had higher entrapment efficiency 97.26 ± 1.12%. The conformational changes in the denatured protein solution were detected through fluorescence spectroscopy. The transmission electron microscopy investigation showed rod-shaped nanocrystals morphology, and no chemical interactions were observed in optimised formulation through FTIR. The DSC and PXRD analysis exhibited an amorphous state of the freeze-dried formulation drug. Also, optimised nanocrystals enhance drug solubility around 26.01-fold, 15.51-fold and 19.08-fold in purified water, pH 6.8 and pH 7.4, and accomplish sustained drug delivery, respectively. It can be concluded that biopolymer-coated celecoxib nanocrystals might be potential drug delivery of hydrophobic molecules for cancer therapy.
Publisher: Royal Society of Chemistry (RSC)
Date: 2020
DOI: 10.1039/D0TB00987C
Abstract: Graphical representation of local and systemic drug delivery systems.
Publisher: Wiley
Date: 29-05-2020
DOI: 10.1002/PAT.4947
Publisher: Elsevier BV
Date: 12-2020
Publisher: MDPI AG
Date: 28-09-2021
DOI: 10.3390/NANO11102535
Abstract: The exploration of multiplexed bacterial virulence factors is a major problem in the early stages of Escherichia coli infection therapy. Traditional methods for detecting Escherichia coli (E. coli), such as serological experiments, immunoassays, polymerase chain reaction, and isothermal microcalorimetry have some drawbacks. As a result, detecting E. coli in a timely, cost-effective, and sensitive manner is critical for various areas of human safety and health. Intelligent devices based on nanotechnology are paving the way for fast and early detection of E. coli at the point of care. Due to their specific optical, magnetic, and electrical capabilities, nanostructures can play an important role in bacterial sensors. Another one of the applications involved use of nanomaterials in fighting microbial infections, including E. coli mediated infections. Various types of nanomaterials, either used directly as an antibacterial agent such as metallic nanoparticles (NPs) (silver, gold, zinc, etc.), or as a nanocarrier to deliver and target the antibiotic to the E. coli and its infected area. Among different types, polymeric NPs, lipidic nanocarriers, metallic nanocarriers, nanomicelles, nanoemulsion/ nanosuspension, dendrimers, graphene, etc. proved to be effective vehicles to deliver the drug in a controlled fashion at the targeted site with lower off-site drug leakage and side effects.
Publisher: Elsevier BV
Date: 2022
Publisher: Elsevier BV
Date: 12-2019
Publisher: Springer Science and Business Media LLC
Date: 08-01-2021
Publisher: Wiley
Date: 06-06-2019
DOI: 10.1002/PAT.4676
Publisher: Elsevier BV
Date: 04-2020
Publisher: Elsevier BV
Date: 10-2020
Publisher: Elsevier BV
Date: 06-2019
DOI: 10.1016/J.IJPHARM.2019.04.055
Abstract: Carbon dots are a carbonaceous nanomaterial that were discovered accidentally and are now drawing significant attention as a new quantum-sized fluorescent nanoparticle. Carbon dots are biocompatible, non-toxic, photostable, and easily functionalized with good photoluminescence and water solubility. Due to these unique properties, they are used broadly in live cell imaging, catalysis, electronics, biosensing, power, targeted drug delivery, and other biomedical applications. Here, we review the recent development of carbon dots in nanomedicine from their use in drug carriers to imaging agents to multifunctional theranostic systems. Finally, we discuss the challenges and views on next-generation carbon dot-based theranostics for clinical applications.
Publisher: MDPI AG
Date: 22-07-2020
DOI: 10.3390/MOLECULES25153324
Abstract: Traditional synthetic techniques for silver nanoparticles synthesis involve toxic chemicals that are harmful to humans as well as the environment. The green chemistry method for nanoparticle synthesis is rapid, eco-friendly, and less toxic as compared to the traditional methods. In the present research, we synthesized silver nanoparticles employing a green chemistry approach from Parthenium hysterophorus leaf extract. The optimized parthenium silver nanoparticles (PrSNPs) had a mean particle size of 187.87 ± 4.89 nm with a narrow size distribution of 0.226 ± 0.009 and surface charge −34 ± 3.12 mV, respectively. The physicochemical characterization of optimized SNPs was done by Fourier transform infrared spectroscopy (FTIR), thermogravimetric analysis (TGA) and differential scanning calorimetry (DSC). Moreover, the transmission electron microscopy (TEM) analysis indicates the spherical shape of NPs with an average diameter of 20–25 nm. PrSNPs were investigated for in vitro antibacterial, antifungal, anti-inflammatory, and antioxidant properties, and showed excellent profiles. The cytotoxic activity was analyzed against two cancer cell lines, i.e., B16F10 and HepG2 for 24 h and 48 h. PrSNPs proved to be an excellent anticancer agent. These PrSNPs were also employed for the treatment of wastewater by monitoring the E. coli count, and it turned out to be reduced by 58% hence these NPs could be used for disinfecting water. Hence, we can propose that PrSNPs could be a suitable candidate as an antimicrobial, antioxidant, anti-inflammatory, and antitumor agent for the treatment of several ailments.
Publisher: FapUNIFESP (SciELO)
Date: 2022
Publisher: Elsevier BV
Date: 04-2020
Publisher: Wiley
Date: 19-04-2021
DOI: 10.1002/JBM.A.37198
Abstract: Mesoporous silica nanoparticles coated with Chitosan are exploited here as a potential carrier for oral vaccine delivery. Bovine serum albumin (BSA) was used as a protein antigen model to reveal the carrier property. Chitosan‐coated BSA‐loaded silica NPs had particle size 345 ± 60 nm with a cationic surface charge of 18.28 ± 0.71 mV. The encapsulation efficiency, drug loading was 25.34 ± 0.76 and 20.21 ± 0.48%, respectively. Transmission electron microscopy investigation showed the spherical shape of NPs, also confirmed surface coating around modified nanoparticles (NPs), and nitrogen absorption/desorption isotherm confirmed mesostructured inside the NPs. Fourier transform infrared spectroscopy did not show any physiochemical interactions between excipients and formulations. The structural stability of antigen after release from NPs was confirmed by sodium dodecyl sulfate‐polyacrylamide gel electrophoresis analysis, and chitosan‐coated silica NPs exhibited a slow‐release pattern. The results of in vivo experiments presented that chitosan‐mesoporous silica NPs could induce a robust immune response in mice, indicating that chitosan‐mesoporous silica NPs might be used as a promising carrier for oral vaccine delivery.
Publisher: MDPI AG
Date: 13-02-2019
DOI: 10.3390/PHARMACEUTICS11020077
Abstract: Mesoporous silica nanomaterials (MSNs) have made remarkable achievements and are being thought of by researchers as materials that can be used to effect great change in cancer therapies, gene delivery, and drug delivery because of their optically transparent properties, flexible size, functional surface, low toxicity profile, and very good drug loading competence. Mesoporous silica nanoparticles (MSNPs) show a very high loading capacity for therapeutic agents. It is well known that cancer is one of the most severe known medical conditions, characterized by cells that grow and spread rapidly. Thus, curtailing cancer is one of the greatest current challenges for scientists. Nanotechnology is an evolving field of study, encompassing medicine, engineering, and science, and it has evolved over the years with respect to cancer therapy. This review outlines the applications of mesoporous nanomaterials in the field of cancer theranostics, as well as drug and gene delivery. MSNs employed as therapeutic agents, as well as their importance and future prospects in the ensuing generation of cancer theranostics and drug and therapeutic gene delivery, are discussed herein. Thus, the use of mesoporous silica nanomaterials can be seen as using one stone to kill three birds.
Publisher: Elsevier BV
Date: 10-2020
Publisher: Informa UK Limited
Date: 19-03-2020
Publisher: American Chemical Society (ACS)
Date: 16-09-2020
Publisher: Elsevier BV
Date: 06-2020
Publisher: Informa UK Limited
Date: 08-05-2019
DOI: 10.1080/21691401.2019.1604535
Abstract: Cisplatin cis-(diammine)dichloridoplatinum(II) (CDDP) is the first platinum-based complex approved by the food and drug administration (FDA) of the United States (US). Cisplatin is the first line chemotherapeutic agent used alone or combined with radiations or other anti-cancer agents for a broad range of cancers such as lung, head and neck. Aroplatin™, Lipoplatin™ and SPI-077 are PEGylated liposome-based nano-formulations that are still under clinical trials. They have many limitations, for ex le, poor aqueous solubility, drug resistance and toxicities, which can be overcome by encapsulating the cisplatin in Nemours nanocarriers. The extensive literature from different electronic databases covers the different nano-delivery systems that are developed for cisplatin. This review critically emphasizes on the recent advancement, development, innovations and updated literature reported for different carrier systems for CDDP.
Publisher: Springer International Publishing
Date: 05-08-2020
Publisher: American Chemical Society (ACS)
Date: 10-08-2020
Publisher: Springer Science and Business Media LLC
Date: 12-06-2019
Publisher: Springer Science and Business Media LLC
Date: 22-11-2019
Publisher: MDPI AG
Date: 23-05-2022
DOI: 10.3390/PHARMACEUTICS14051113
Abstract: Research into the application of nanocarriers in the delivery of cancer-fighting drugs has been a promising research area for decades. On the other hand, their cytotoxic effects on cells, low uptake efficiency, and therapeutic resistance have limited their therapeutic use. However, the urgency of pressing healthcare needs has resulted in the functionalization of nanoparticles’ (NPs) physicochemical properties to improve clinical outcomes of new, old, and repurposed drugs. This article reviews recent research on methods for targeting functionalized nanoparticles to the tumor microenvironment (TME). Additionally, the use of relevant engineering techniques for surface functionalization of nanocarriers (liposomes, dendrimers, and mesoporous silica) and their critical roles in overcoming the current limitations in cancer therapy—targeting ligands used for targeted delivery, stimuli strategies, and multifunctional nanoparticles—were all reviewed. The limitations and future perspectives of functionalized nanoparticles were also finally discussed. Using relevant keywords, published scientific literature from all credible sources was retrieved. A quick search of the literature yielded almost 400 publications. The subject matter of this review was addressed adequately using an inclusion/exclusion criterion. The content of this review provides a reasonable basis for further studies to fully exploit the potential of these nanoparticles in cancer therapy.
Publisher: Royal Society of Chemistry (RSC)
Date: 2020
DOI: 10.1039/C9RA09468G
Abstract: Disulfiram (DSF), an FDA-approved anti-alcoholic drug, has recently shown that it possesses anti-cancer effects.
No related grants have been discovered for Muhammad Asim Farooq.