Chalcones are potent inhibitors of aromatase and 17beta-hydroxysteroid dehydrogenase activities |
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| Authors: | Le Bail J C Pouget C Fagnere C Basly J P Chulia A J Habrioux G |
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| Institution: | UPRES EA 1085, Biomolecules et cibles cellulaires tumorales-Prolifération cellulaire et inhibition enzymatique Laboratoire de Biochimie, Faculté de Pharmacie, Limoges, France. |
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| 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. |
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