Interaction of phytoestrogens with estrogen receptors α and β (II)
Interaction of phytoestrogens with estrogen receptors α and β (II)
复制标题
DOI：
10.1248/bpb.25.48
复制
发表时间：
2002-01-01
影响因子：
2
通讯作者：
Masamune, Y
中科院分区：
文献类型：
--
作者：
Morito, K;Aomori, T;Masamune, Y
我们在与人雌激素受体 (hER) α 或 hER β 蛋白的竞争结合测定中以及在使用酵母系统的基因表达测定中研究了异黄酮衍生物的雌激素活性。香雌酚与两种 hER 的结合强度与 17 β-雌二醇一样强。 Biochanin A、5-OMe-金雀异黄素、芒柄花素和鸢尾黄素与 hER β 结合良好，但仅在 5-OMe-金雀异黄素、芒柄花素和鸢尾黄素中观察到与 hER α 的显着结合。 7-OMe-genistein 和 irisolidone 与两种受体的结合都很差。在糖苷类中，西索托林与两种受体结合，且结合力强于染料木苷。香雌酚与金雀异黄素一样强烈地诱导转录。鸢尾皂甙元还诱导两种 hER 的转录。虽然生物鸡素 A、5-OMe-金雀异黄素、7-OMe-金雀异黄素、伊立索酮和芒柄花素轻微诱导 hER P 转录，但它们在 17 β-雌二醇诱导转录中充当拮抗剂。结果表明，异黄酮的甲基化或糖化通常会抑制其植物雌激素活性。
We investigated the estrogenic activities of isoflavone derivatives in competition binding assays with human estrogen receptor (hER) alpha or hER beta protein, and in a gene expression assay using a yeast system. Coumestrol binds as strongly as 17 beta -estradiol to both hERs. Biochanin A, 5-OMe-genistein, formononetin, and tectorigenin bind well to hER beta, but significant binding to hER alpha is only observed with 5-OMe-genistein, formononetin and tectorigenin. The binding of 7-OMe-genistein and irisolidone is poor to both receptors. Among the glucosides, sissotorin binds both receptors and the binding is stronger than genistin. Coumestrol induces transcription as strongly as genistein. Tectorigenin also induces transcription with both hERs. Though biochanin A, 5-OMe-genistein, 7-OMe-genistein, irisolidone and formononetin slightly induce transcription with hER P, they act as antagonists in the induction of transcription by 17 beta -estradiol. The results show that methylation or glucoidation of isoflavones generally inhibits their phytoestrogenic activities.