2. Academic Validation
  3. Chalcones are potent inhibitors of aromatase and 17beta-hydroxysteroid dehydrogenase activities

Chalcones are potent inhibitors of aromatase and 17beta-hydroxysteroid dehydrogenase activities

  • Life Sci. 2001 Jan 5;68(7):751-61. doi: 10.1016/s0024-3205(00)00974-7.
J C Le Bail 1,  C Pouget,  C Fagnere,  J P Basly,  A J Chulia,  G Habrioux
Affiliations

Affiliation

  • 1 UPRES EA 1085, Biomolecules et cibles cellulaires tumorales-Prolifération cellulaire et inhibition enzymatique Laboratoire de Biochimie, Faculté de Pharmacie, Limoges, France.
PMID: 11205867 DOI: 10.1016/s0024-3205(00)00974-7
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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