| Literature DB >> 11205867 |
J C Le Bail1, C Pouget, C Fagnere, J P Basly, A J Chulia, G Habrioux.
Abstract
Chalcones were tested for estimating anti-aromatase, anti-3beta-hydroxysteroid dehydrogenase delta5/delta4 isomerase (3beta-HSD) and anti-17beta-hydroxysteroid dehydrogenase (17beta-HSD) activities in human placental microsomes. In the present study, we have demonstrated for the first time that chalcones are potent inhibitors of aromatase and 17beta-hydroxysteroid dehydrogenase activities: these enzymes being considered as important targets in the metabolic pathways of human mammary hormone-dependent cells. Our results showed that naringenin chalcone and 4-hydroxychalcone were the most effective aromatase and 17beta-hydroxysteroid dehydrogenase inhibitors with IC50 values of 2.6 and 16 microM respectively. In addition, inhibitory effects of some flavones and flavanones were compared to those of the corresponding chalcones. A structure-activity relationship was established and regions or/and substituents essential for these inhibitory activities were determined.Entities:
Mesh：
Substances：
Year: 2001 PMID： 11205867 DOI： 10.1016/s0024-3205(00)00974-7
Source DB: PubMed Journal: Life Sci ISSN： 0024-3205 Impact factor: 5.037