Effect of 7-O-beta-D-glucopyranosylchrysin and its aglycone chrysin isolated from Podocytisus caramanicus on estrogen receptor alpha transcriptional activity.
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.
Berthier
Alexandre
A
EA3922 Estrogènes, Expression Génique et Pathologies du Système Nerveux Central, IFR 133, Université de Franche-Comté, UFR Sciences et Techniques, Besançon, France.
Girard
Corinne
C
Grandvuillemin
Aurélie
A
Muyard
Frédéric
F
Skaltsounis
Alexios-Leandros
AL
Jouvenot
Michèle
M
Delage-Mourroux
Régis
R
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*
C526876:7-O-beta-D-glucopyranosylchrysin; D000972:Antineoplastic Agents, Phytogenic; D047628:Estrogen Receptor alpha; D005419:Flavonoids; D005960:Glucosides; C043561:chrysin