Browsing by Author "Chiou, Ya-Sheng"

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An enzymatic approach to configurationally rare trans-androsteronyl--glucoside and Its potential anticancerapplication
(2017-01)
Chou, Feng-Pai
;
Tsai, Chia-Tse
;
Chiou, Ya-Sheng
;
Chen, Yi-Ju
;
Li, Meng-Erh
Enzymatic glycosylation of sterols/steroids with glycosyltransferase HP0421 shows protein plasticity on generation of configurationally rare steryl--glucosides. Investigation of trans-androsteronyl--glucoside on tamoxifen-treated MCF-7 breast cancer cells shows dose-dependent depression of cell viability and enhanced drug effectiveness, illustrating a new avenue for the production of novel steryl--glucosides with useful biological activities.
Pregnenolonyl-alpha-glucoside exhibits marked anti-cancer and CYP17A1 enzymatic inhibitory activities
(2020-02-07)
Chou, Feng-Pai
;
Hsu, Wen-Chen
;
Huang, Sheng-Cih
;
Chang, Chin-Yuan
;
Chiou, Ya-Sheng
We report here that pregnenolonyl-alpha-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 mu M. 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.