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Brevifoliol ester induces apoptosis in prostate cancer cells by activation of caspase pathway
Author(s) -
Bhukya Balakishan,
Fatima Kaneez,
Nagar Abhishek,
Lakshmi Vijaya,
Dubey Poornima,
Kumar Shailesh,
Kumar Yogesh,
Luqman Suaib,
Chanda Debabrata,
Tandon Sudeep,
Shanker Karuna,
Khan Feroz,
Negi Arvind S.
Publication year - 2020
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.13631
Subject(s) - apoptosis , in vivo , cytotoxicity , chemistry , taxoid , ehrlich ascites carcinoma , prostate cancer , cell cycle checkpoint , cell culture , cell cycle , mtt assay , cancer research , cancer cell , pharmacology , cancer , in vitro , biochemistry , biology , medicine , docetaxel , genetics , microbiology and biotechnology
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.