Brevifoliol ester induces apoptosis in prostate cancer cells by activation of caspase pathway.
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.
['Bhukya|Balakishan|B|', 'Fatima|Kaneez|K|', 'Nagar|Abhishek|A|', 'Lakshmi|Vijaya|V|', 'Dubey|Poornima|P|', 'Kumar|Shailesh|S|', 'Kumar|Yogesh|Y|', 'Luqman|Suaib|S|', 'Chanda|Debabrata|D|', 'Tandon|Sudeep|S|', 'Shanker|Karuna|K|', 'Khan|Feroz|F|0000-0002-2704-5925', 'Negi|Arvind S|AS|0000-0002-1236-2493']
D019342:Acetic Acid D000818:Animals D000970:Antineoplastic Agents D017209:Apoptosis D019817:Benzoic Acid D004354:Drug Screening Assays, Antitumor D004951:Esterification D004952:Esters D006801:Humans D008297:Male D051379:Mice D062105:Molecular Docking Simulation D009374:Neoplasms, Experimental D000078722:PC-3 Cells D010936:Plant Extracts D011471:Prostatic Neoplasms D043823:Taxoids D020946:Taxus
apoptosis Ehrlich ascites carcinoma acute oral toxicity anticancer brevifoliol analogues