title: Effect of 7-O-beta-D-glucopyranosylchrysin and its aglycone chrysin isolated from Podocytisus caramanicus on estrogen receptor alpha transcriptional activity.
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, E (2), genistein (Gen) and biochanin A (Bch), as controls to evaluate our cellular model. Secondly, we have demonstrated that the 7- O-beta- D-glucopyranosylchrysin (Glc-chr), the most abundant flavone of the extract, and its aglycone chrysin were able to increase estrogen receptor alpha 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 ERalpha.
authors.affiliation: EA3922 Estrogènes, Expression Génique et Pathologies du Système Nerveux Central, IFR 133, Université de Franche-Comté, UFR Sciences et Techniques, Besançon, France.
authors.forename: Alexandre
authors.initials: A
authors.lastname: Berthier
authors.forename: Corinne
authors.initials: C
authors.lastname: Girard
authors.forename: Aurélie
authors.initials: A
authors.lastname: Grandvuillemin
authors.forename: Frédéric
authors.initials: F
authors.lastname: Muyard
authors.forename: Alexios-Leandros
authors.initials: AL
authors.lastname: Skaltsounis
authors.forename: Michèle
authors.initials: M
authors.lastname: Jouvenot
authors.forename: Régis
authors.initials: R
authors.lastname: Delage-Mourroux
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D001943:Breast Neoplasms / Q000235:genetics / Q000473:pathology; D045744:Cell Line, Tumor; D047628:Estrogen Receptor alpha / Q000378:metabolism*; D007887:Fabaceae / Q000737:chemistry*; D005419:Flavonoids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D005960:Glucosides / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D015394:Molecular Structure; D014158:Transcription, Genetic / Q000187:drug effects*
chemical_list: C526876:7-O-beta-D-glucopyranosylchrysin; D000972:Antineoplastic Agents, Phytogenic; D047628:Estrogen Receptor alpha; D005419:Flavonoids; D005960:Glucosides; C043561:chrysin