1. Academic Validation
  2. Estradiol-antagonistic activity of phenolic compounds from leguminous plants

Estradiol-antagonistic activity of phenolic compounds from leguminous plants

  • Phytother Res. 2008 Mar;22(3):362-6. doi: 10.1002/ptr.2327.
B Pinto 1 A Bertoli C Noccioli S Garritano D Reali L Pistelli
Affiliations

Affiliation

  • 1 Dipartimento di Patologia Sperimentale, Biotecnologie Mediche, Infettivologia ed Epidemiologia, University of Pisa, Pisa, Italy. b.pinto@med.unipi.it
Abstract

Natural Flavonoids are currently receiving much attention because of their estrogenic and antiestrogenic properties. Six Isoflavones (isoprunetin, isoprunetin 7-O-beta-D-glucopyranoside, isoprunetin 4',7-di-O-beta-D-glucopyranoside, genistein, genistein 7-O-beta-D-glucopyranoside, daidzein), four Flavones (luteolin, luteolin 7-O-beta-D-glucopyranoside, luteolin 4'-O-beta-D-glucopyranoside, licoflavone C), isolated from Genista morisii and G. ephedroides (two Leguminosae plants of the Mediterranean area) together with two structurally related pterocarpans, bitucarpin A and erybraedyn C, isolated from Bituminaria bituminosa (Leguminosae), were tested for the antagonist activity by a yeast based Estrogen Receptor assay (Saccharomyces cerevisiae RMY326 ER-ERE). Most compounds inhibited the estradiol-induced transcriptional activity in a concentration dependent manner. In particular, for the flavone luteolin 77% inhibition of the induced beta-galactosidase activity was observed. Interestingly, licoflavone C exhibited a dose-dependent antagonistic activity at concentrations up to 10(-4) M, but stimulated beta-galactosidase expression at higher concentrations resulting in a U-shaped-like dose-response curve.

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