1. Brevifoliol ester induces apoptosis in prostate cancer cells by activation of caspase pathway.
- Author
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Bhukya B, Fatima K, Nagar A, Lakshmi V, Dubey P, Kumar S, Kumar Y, Luqman S, Chanda D, Tandon S, Shanker K, Khan F, and Negi AS
- Subjects
- Acetic Acid chemistry, Animals, Antineoplastic Agents pharmacology, Apoptosis drug effects, Benzoic Acid chemistry, Drug Screening Assays, Antitumor, Esterification, Humans, Male, Mice, Molecular Docking Simulation, Neoplasms, Experimental drug therapy, PC-3 Cells, Plant Extracts pharmacology, Taxoids pharmacology, Taxus chemistry, Antineoplastic Agents chemistry, Esters chemistry, Plant Extracts chemistry, Prostatic Neoplasms drug therapy, Taxoids chemistry
- Abstract
Prostate cancer is fourth most abundant cancer type around the globe. Brevifoliol, a rearranged taxoid from Taxus walllichiana needles has been derivatized as C5 esters using Steglich esterification reaction. Seventeen diverse analogues were evaluated against a panel of human cancer cell lines by MTT assay. Among these, two of the semi-synthetic analogues, that is, 13 and 16 exhibited potent cytotoxicity, selectively against PC-3, prostate cancer cell lines. In cell cycle analysis, analogue 13 induced S and G2/M phase arrest and induced apoptosis by activating caspase-3. Compound 13 showed moderate efficacy in in-vivo Ehrlich ascites carcinoma in Swiss albino mice. Further, compound 13 was found to be safe in Swiss albino mice up to 1,000 mg/kg dose in acute oral toxicity. Brevifoliol ester 13 may further be optimized for better efficacy., (© 2019 John Wiley & Sons A/S.)
- Published
- 2020
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