Markiewicz L, Garey J, Adlercreutz H, Gurpide E
Department of Obstetrics, Gynecology & Reproductive Science, Mount Sinai School of Medicine, New York, NY 10029-6574.
J Steroid Biochem Mol Biol. 1993 May;45(5):399-405. doi: 10.1016/0960-0760(93)90009-l.
Some of the isoflavonoids present in human diet as well as in urine are expected to exert biologic effects as they have been reported to bind to estrogen receptors and to be estrogenic in other species. This report describes the in vitro assessment of estrogenic effects of isoflavonoids using human endometrial cells and tissue. The relative estrogenic potencies (EC50 values) of estradiol, 3 dietary isoflavonoids (coumestrol, genistein and daidzein) and one of their metabolites (equol), were estimated by using a recently developed multiwell plate in vitro bioassay based on the estrogen-specific enhancement of alkaline phosphatase (AlkP) activity in human endometrial adenocarcinoma cells of the Ishikawa-Var I line. The maximal AlkP activity elicited by the isoflavonoids tested was as high as that achieved with estradiol and their effects were suppressed by the antiestrogens 4-hydroxytamoxifen and ICI 164,384. These results indicate that estradiol and the isoflavonoids exert their effects on AlkP by similar interactions with the estrogen receptor, with potencies depending on binding affinities. The estrogenic effect of equol was confirmed by another in vitro bioassay, based on the estrogen-stimulated enhancement of prostaglandin F2 alpha output by fragments of human secretory endometrium.
人类饮食以及尿液中存在的一些异黄酮类化合物，据报道它们可与雌激素受体结合并在其他物种中具有雌激素活性，因此有望发挥生物学效应。本报告描述了使用人子宫内膜细胞和组织对异黄酮类化合物雌激素效应进行的体外评估。通过基于石川 - Var I系人子宫内膜腺癌细胞中碱性磷酸酶（AlkP）活性的雌激素特异性增强而开发的新型多孔板体外生物测定法，估算了雌二醇、3种膳食异黄酮（香豆雌酚、染料木黄酮和大豆苷元）及其一种代谢产物（雌马酚）的相对雌激素效价（EC50值）。所测试的异黄酮类化合物引发的最大AlkP活性与雌二醇所达到的活性一样高，并且它们的作用被抗雌激素药物4 - 羟基他莫昔芬和ICI 164,384所抑制。这些结果表明，雌二醇和异黄酮类化合物通过与雌激素受体的类似相互作用对AlkP发挥作用，其效价取决于结合亲和力。基于人分泌期子宫内膜碎片雌激素刺激的前列腺素F2α产量增加，通过另一种体外生物测定法证实了雌马酚的雌激素效应。
