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

Autor: Chou FP; Department of Biological Science and Technology, National Chiao Tung University, Hsin-Chu, Taiwan, Republic of China. tkwmll@mail.nctu.edu.tw., Hsu WC, Huang SC, Chang CY, Chiou YS, Tsai CT, Lyu JW, Chen WT, Wu TK
Jazyk: angličtina
Zdroj: Chemical communications (Cambridge, England) [Chem Commun (Camb)] 2020 Feb 06; Vol. 56 (11), pp. 1733-1736.
DOI: 10.1039/c9cc09415f
Abstrakt: 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.
Databáze: MEDLINE