Estradiol‐antagonistic activity of phenolic compounds from leguminous plants

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.

Antiestrogenic and antigenotoxic activity of bee pollen from Cystus incanus and Salix alba as evaluated by the yeast estrogen screen and the micronucleus assay in human lymphocytes

“…This can depend, as well as on the nature of the compound, on the concentration range at which they are analyzed, on the cell system and the biomarker used and if a single phytochemical is assayed in an extract containing other identified or undetermined secondary metabolites. In this view, previous evidence indicates that single polyphenols or extracts can be simultaneously estrogenic and antiestrogenic [4,23,24] or exert antigenotoxic or genotoxic activity at low or high concentrations, respectively [6,25].…”

“…Bee pollen is also a very important source of vitamins and polyphenolic compounds, particularly flavonoids [1,2]. Some classes of these substances, similarly to natural estrogens (phytoestrogens), are able to bind intracellular estrogen receptors (ERs) thus causing estrogenic/antiestrogenic effects [3,4]. In addition, they exhibit a broad spectrum of biological effects which can be beneficial or harmful for human health.…”

Genista sessilifolia DC. extracts induce apoptosis across a range of cancer cell lines

“…) whose anti‐cancer potential has already been recognized . Interestingly, fractions 20–22 main component was isoprunetin whose anti‐cancer and anti‐oestrogenic potentials have also been suggested.…”

So Uncommon and so Singular, but Underexplored: An Updated Overview on Ethnobotanical Uses, Biological Properties and Phytoconstituents of Sardinian Endemic Plants

“…Consequently, phytoestrogens can act as agonists, partial agonists and antagonists [160,163]. Some isoflavones and flavones isolated from the aerial parts of Genista morisii and Genista ephedroides were in vitro evaluated for their estrogenic [164] and anti-estrogenic activities [165] by a yeast-based estrogen receptor assay. The licoflavone C and the isoflavone genistein showed the highest estrogenic activity detected by β-galactosidase activity induction.…”