Pregnenolonyl-α-glucoside exhibits marked anti-cancer and CYP17A1 enzymatic inhibitory activities

Feng Pai Chou, Wen Chen Hsu, Sheng Cih Huang, Chin Yuan Chang, Ya Sheng Chiou, Chia Tse Tsai, Jason Wenjay Lyu, Wei Ting Chen, Tung Kung Wu*

*Corresponding author for this work

研究成果: Article同行評審

摘要

We report here that pregnenolonyl-α-glucoside (2), a steryl glycoside synthesized directly from pregnenolone and glucose via a consecutive multienzyme-catalyzed process, exhibits marked dose-dependent cytotoxic activity against HT29, AGS, and ES-2 cells with IC50 values of 23.5 to 50.9 μM. An in vitro CYP17A1 binding pattern assay and protein-ligand docking model support that 2, like abiraterone, binds in the active site heme iron pocket of CYP17A1.

原文English
頁(從 - 到)1733-1736
頁數4
期刊Chemical Communications
56
發行號11
DOIs
出版狀態Published - 7 二月 2020

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