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

Research output: Contribution to journalArticle

Abstract

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.

Original languageEnglish
Pages (from-to)1733-1736
Number of pages4
JournalChemical Communications
Volume56
Issue number11
DOIs
StatePublished - 7 Feb 2020

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