Differential binding with ERα and ERβ of the phytoestrogen-rich plant Pueraria mirifica
Differential binding with ERα and ERβ of the phytoestrogen-rich plant Pueraria mirifica
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DOI：
10.1590/s0100-879x2009007500026
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发表时间：
2010-02-01
影响因子：
2.3
通讯作者：
Cherdshewasart, W.
中科院分区：
文献类型：
--
作者：
Boonchird, C.;Mahapanichkul, T.;Cherdshewasart, W.
利用酵母雌激素筛选（YES）检测富雌激素植物葛根的雌激素活性变化，该筛选包括人雌激素受体（hER） hER α和hER β、人转录中介因子2 （hTIF2）或人类固醇受体辅激活因子1 (hSRC1)，以及β -半乳苷酶表达盒。通过测定块茎提取物的β -半乳糖苷酶活性（EC50）与17 β -雌二醇的关系来表达相对雌激素效价。24种和22种植物块茎乙醇提取物分别与hER - α和hER - β相互作用，hER - β比hER - α具有更高的相对雌激素效力。植物提取物的抗雌激素活性也通过植物提取物与17 - β -雌二醇孵育在YES测定之前确定。所测植物提取物具有抗雌激素活性。在实验之前，块茎提取物的雌激素和抗雌激素活性都被大鼠肝脏s9组分代谢激活，表明肝酶的积极影响。经hplc分析的薯类样品中葛根素、大豆苷元、genistin、大豆苷元、染料木素5种主要异黄酮含量与雌激素效价的相关性分析均为阴性。
Variations in the estrogenic activity of the phytoestrogen-rich plant, Pueraria mirifica, were determined with yeast estrogen screen (YES) consisting of human estrogen receptors (hER) hER alpha and hER beta and human transcriptional intermediary factor 2 (hTIF2) or human steroid receptor coactivator 1 (hSRC1), respectively, together with the beta-galactosidase expression cassette. Relative estrogenic potency was expressed by determining the beta-galactosidase activity (EC50) of the tuber extracts in relation to 17 beta-estradiol. Twenty-four and 22 of the plant tuber ethanolic extracts interacted with hER alpha and hER beta, respectively, with a higher relative estrogenic potency with hER beta than with hER alpha. Antiestrogenic activity of the plant extracts was also determined by incubation of plant extracts with 17 beta-estradiol prior to YES assay. The plant extracts tested exhibited antiestrogenic activity. Both the estrogenic and the antiestrogenic activity of the tuber extracts were metabolically activated with the rat liver S9-fraction prior to the assay indicating the positive influence of liver enzymes. Correlation analysis between estrogenic potency and the five major isoflavonoid contents within the previously HPLC-analyzed tuberous samples namely puerarin, daidzin, genistin, daidzein, and genistein revealed a negative result.