Evidence for estrogen receptor beta-selective activity of Vitex agnus-castus and isolated flavones.
Recent cell culture experiments indicated that extracts of Vitex agnus-castus (VAC) may contain yet unidentified phytoestrogens. Estrogenic actions are mediated via estrogen receptors (ER). To investigate whether VAC compounds bind to the currently known isoforms ERalpha or ERss, ligand binding assays (LBA) were performed. Subtype specific ER-LBA revealed a binding of VAC to ERss only. To isolate the ERss-selective compounds, the extract was fractionated by bio-guidance. The flavonoid apigenin was isolated and identified as the most active ERss-selective phytoestrogen in VAC. Other isolated compounds were vitexin and penduletin. These data demonstrate that the phytoestrogens in VAC are ERss-selective.
Jarry
Hubertus
H
Klinische und Experimentelle Endokrinologie, Universitätsfrauenklinik Göttingen, Göttingen, Germany. hubjarry@med.uni-goettingen.de
Spengler
Barbara
B
Porzel
Andrea
A
Schmidt
Juergen
J
Wuttke
Wolfgang
W
Christoffel
Volker
V
D047310:Apigenin; D004305:Dose-Response Relationship, Drug; D047629:Estrogen Receptor beta; D005419:Flavonoids / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D007529:Isoflavones / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D048789:Phytoestrogens; D008517:Phytotherapy; D010936:Plant Extracts / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use; D028321:Plant Preparations / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D011960:Receptors, Estrogen / Q000187:drug effects*; D020950:Vitex
D047629:Estrogen Receptor beta; D005419:Flavonoids; D007529:Isoflavones; D048789:Phytoestrogens; D010936:Plant Extracts; D028321:Plant Preparations; D011960:Receptors, Estrogen; D047310:Apigenin; C032731:vitexin