Posted by admin on Jan 31, 2022 in |
Independent studies have shown that chalcones and 123 triazole exhibited cytotoxic effects on human cancer cell lines. In the present study, we prepared a series of novel 1,2,3-triazole-chalcone hybrid compounds and evaluated the cytotoxic effect and probable mode of action in HT29 colon cancer cell line. Among the 10 evaluated compounds, compounds 4 (3-nitro) and 8 (3-chloro) were the only compounds that elicited a dose-dependent decrease in cell viability (IC50 values 9.7 and 33 M, respectively) of HT 29 cells. The same compounds exhibited a significant inhibitory effect on the cell proliferation and colony-forming capability of HT29 cells. Co-administration of compounds 4 and 8 with electron transport chain inhibitors and mitochondrial K+-ATP channel blockers in H9C2 enhanced the anti-proliferative capacity of the compound. Furthermore, Insilco molecular docking studies revealed that the anti-proliferative effect of these compounds could be attributed to interactions with the colchicine-binding site of tubulin. In conclusion, our results demonstrated that novel 1,2,3-triazole-chalcone hybrid can be a potent therapeutic agent against HT-29 cells, and its anti proliferating...
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Posted by admin on Jan 31, 2022 in |
Objective: The present research was focused on designing, formulate and evaluate the trilayer matrix tablets incorporated with quinapril for extending drug release. Methods: Quinapril trilayer matrix tablets were formulated using response surface methodology wherein initially 27 formulations (QF1-QF27) were designed for active layer from which one best formulation was chosen based on drug content, swelling index, and in-vitro release studies. The chosen formulation was formulated into extended-release trilayed matrix tablet by varying proportions of polymers by direct compression technique and was evaluated for various physicochemical parameters, drug release and the drug release data were fitted into the various kinetic model to know the mechanism of drug release. The best-optimized formulation was further characterized by FTIR and stability studies. Results: 27 active layer formulations were evaluated for various physicochemical properties and drug release, out of which the highest drug release was exhibited by QF16 (98.85%). Thus, QF16 was used for formulation into trilayer matrix tablets (AQF16-HQF16). All the formulations were evaluated for drug content, swelling index, and percentage drug release...
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Posted by admin on Jan 31, 2022 in |
Lupeol (I) is a naturally occurring triterpene that has been isolated from the stem bark of Crataeva nurvala in appreciable amount. Due to the presence of a single hydroxyl group and a large, apolar skeleton, lupeol acts as an amphiphile. The two possible sites for chemical modification present in lupeol are ring-A and isopropenyl side chain. We modified it in three naturally occurring analogous derivatives, i.e., 3a, 5a, 5b, 8, 8, 11a-Hexamethyl-1-(2-methyl-oxiranyl)-icosahydro-cyclopenta[a] chrysen-9-ol (II), lupeol acetate (III), and lupenone (IV) by oxidation and acylation process. The structures of the newly synthesized compounds were confirmed by elemental analysis, 1H, 13C NMR, IR, and MS spectroscopy. In-vitro antioxidant activity for all the compounds evaluated where ascorbic acid (vitamin C) treated as standard. All the analysis was made with the use of UV-Visible spectrophotometer. Result of the study suggested that all the compounds showed effective efficacy for antioxidant properties in a concentration-dependant manner, although lupeol acetate was found most significant in comparison to...
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Posted by admin on Dec 31, 2021 in |
An accurate, simple, precise, rapid stability-indicating assay method was developed and subsequently validated for the estimation of Telmisartan in API and Tablets. The best separation of the drug was achieved on Kromasil C18 (4.6 × 150 mm, 5 µm) with the mobile phase consisted of mixture of 0.01 M Phosphate buffer (pH: 3) and Acetonitrile in ratio of (40:60%) at flow rate of 2 ml/min, with detection at 226 nm using PDA detector. The retention time was found to be 2.728 min. The method was found to be linear in the range of 10-60 µg/ml with a correlation coefficient (r2) of 0.999. The LOD and LOQ of the method were calculated to be 0.256 and 0.776 µg/ml, respectively. The Precision was estimated by employing repeatability; intra-day and inter-day studies and the results were calculated as %RSD values and were found to be within the acceptable limits. Recovery of the drug was found to be in the range of 97-102%, which establishes the accuracy of the method. Forced degradation studies...
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Posted by admin on Dec 31, 2021 in |
Leishmaniasis is a neglected tropical infectious disease affecting poor people, especially in the developing countries of the world. It is a systemic disease caused by a protozoan parasite leishmania donovani and is fatal if left untreated. The aim of the present study is to develop and evaluate the in-vitro antileishmanial activity of the combination of amphotericin B and mitefosinenano vesicles for targeted delivery to macrophages in the treatment of visceral leishmaniasis to increase the efficacy, decrease emergency of resistance and increase overall patient compliance. Drug-loaded nanovesicles were prepared by ethanol injection method. Physicochemical characterization and cytotoxicity, and antileishmanial activity evaluations were assessed. Nanovesicles of optimal AmB-MTF formulation was prepared from phosphatidylcholine-cholesterol-stearic acid (20:4:1 w/w) lipids, ethanol-water (1:4 v/v) dispersion medium, and AmB-MTF (1:1 w/w) drugs at drug loading of 1:8 and stirring rate of 1000 rpm. AmB-MTF 1:1 nanovesicles exhibited a mean particle size of 145.6 nm, polydispersity index (PDI) 0.19, zeta potential -27.3 mV and drug entrapment efficiency 87%. The AmB-MTF combination nanovesicles demonstrated low CC50 against J774...
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