Pinto B, Bertoli A, Noccioli C, Garritano S, Reali D, Pistelli L
Dipartimento di Patologia Sperimentale, Biotecnologie Mediche, Infettivologia ed Epidemiologia, University of Pisa, Pisa, Italy.
Phytother Res. 2008 Mar;22(3):362-6. doi: 10.1002/ptr.2327.
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.
天然黄酮类化合物因其雌激素和抗雌激素特性目前备受关注。从地中海地区的两种豆科植物（莫里西染料木和麻黄状染料木）中分离出六种异黄酮（异樱黄素、异樱黄素7 - O - β - D - 葡萄糖苷、异樱黄素4',7 - 二 - O - β - D - 葡萄糖苷、染料木黄酮、染料木黄酮7 - O - β - D - 葡萄糖苷、大豆苷元）、四种黄酮（木犀草素、木犀草素7 - O - β - D - 葡萄糖苷、木犀草素4'- O - β - D - 葡萄糖苷、甘草黄酮C），以及从Bituminaria bituminosa（豆科）中分离出的两种结构相关的紫檀烷（比图卡品A和刺桐黄酮C），通过基于酵母的雌激素受体检测法（酿酒酵母RMY326 ER - ERE）测试其拮抗活性。大多数化合物以浓度依赖的方式抑制雌二醇诱导的转录活性。特别是，对于黄酮木犀草素，观察到其对诱导的β - 半乳糖苷酶活性有77%的抑制作用。有趣的是，甘草黄酮C在浓度高达10(-4) M时表现出剂量依赖性拮抗活性，但在更高浓度下刺激β - 半乳糖苷酶表达，导致呈U形的剂量反应曲线。
