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 |
Externí odkaz: |
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