Abstract
Chalcones were tested for estimating anti-aromatase, anti-3β-hydroxysteroid dehydrogenase Δ 5/Δ 4 isomerase (3β-HSD) and anti-17β-hydroxysteroid dehydrogenase (17β-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 17β-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 17β-hydroxysteroid dehydrogenase inhibitors with IC 50 values of 2.6 and 16 μM 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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