Planta Med 2007; 73(14): 1447-1451
DOI: 10.1055/s-2007-990248
Pharmacology
Original Paper
© Georg Thieme Verlag KG Stuttgart · New York

Effect of 7-O-β-D-Glucopyranosylchrysin and its Aglycone Chrysin Isolated from Podocytisus caramanicus on Estrogen Receptor α Transcriptional Activity

Alexandre Berthier1 , Corinne Girard2 , Aurélie Grandvuillemin2 , Frédéric Muyard2 , Alexios-Leandros Skaltsounis3 , Michèle Jouvenot1 , Régis Delage-Mourroux1
  • 1EA3922 ”Estrogènes, Expression Génique et Pathologies du Système Nerveux Central”, IFR 133, Université de Franche-Comté, UFR Sciences et Techniques, Besançon, France
  • 2Laboratoire de Pharmacognosie, EA 3921 ”Optimisation Métabolique et Cellulaire”, IFR 133, Université de Franche-Comté, UFR des Sciences Médicales et Pharmaceutiques, Besançon, France
  • 3Division of Pharmacognosy and Natural Products Chemistry, School of Pharmacy, University of Athens, Athens, Greece
Further Information

Publication History

Received: March 12, 2007 Revised: August 29, 2007

Accepted: September 21, 2007

Publication Date:
19 October 2007 (online)

Abstract

A screening of Greek Fabaceae extracts identified the methanolic extract of Podocytisus caramanicus Boiss. & Heldr. as having proliferative activity on human breast cancer cells (MCF-7). Using transient transfection experiments, we have first used three compounds described for their estrogen-like properties, E2, genistein (Gen) and biochanin A (Bch), as controls to evaluate our cellular model. Secondly, we have demonstrated that the 7-O-β-D-glucopyranosylchrysin (Glc-chr), the most abundant flavone of the extract, and its aglycone chrysin were able to increase estrogen receptor α transcriptional activity in MCF-7 cells. We have also shown that the estrogenic activity of Glc-chr could be completely suppressed by the pure estrogen antagonist ICI 182,780 suggesting that the effect of Glc-chr is mediated by ERα.

Abbreviations

CSFCS:charcoal-stripped fetal calf serum

E2:estradiol

ER:estrogen receptor

ERE:estrogen response element

FCS:fetal calf serum

FM:full medium

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Prof. Régis Delage-Mourroux

EA3922 ”Estrogènes, Expression Génique et Pathologies du Système Nerveux Central”

IFR 133

Université de Franche-Comté

UFR Sciences et Techniques

16, route de Gray

25030 Besançon cedex

France

Phone: +33-38-166-6544

Fax: +33-38-166-6267

Email: regis.delage-mourroux@univ-fcomte.fr