Institute of Pharmacy, Martin Luther University Halle-Wittenberg, Halle/Saale, Germany.
Phytochemistry. 2011 Dec;72(18):2396-405. doi: 10.1016/j.phytochem.2011.08.013. Epub 2011 Sep 1.
Phytoestrogens are plant-derived food ingredients assumed to contribute to the prevention of hormone-dependent cancers, osteoporosis, cardiovascular disease, and menopausal symptoms. Lignans occur in numerous food plants and various structures; they are common constituents of human diet, and estrogen activity has been assessed for lignan metabolites formed in the mammalian intestine. We examined natural lignans and semisynthetic norlignans for estrogen and antiestrogen activity. A transformed yeast strain (Saccharomyces cerevisiae) expressing the estrogen receptor alpha and a reporter system was applied as test system. Some plant lignans showed estrogen activity while others and the semisynthetic norlignans were moderately active antiestrogens. Docking of lignans to protein models of estrogen receptor alpha in the active and inactive form sustained the results of the yeast estrogen assay and supported the concept of plant lignans as phytoestrogens.
植物雌激素是源自植物的食物成分，被认为有助于预防激素依赖性癌症、骨质疏松症、心血管疾病和更年期症状。木脂素存在于许多食物植物和各种结构中；它们是人类饮食的常见成分，并且已经评估了在哺乳动物肠道中形成的木脂素代谢物的雌激素活性。我们研究了天然木脂素和半合成去甲木脂素的雌激素和抗雌激素活性。应用表达雌激素受体 α 和报告系统的转化酵母菌株（酿酒酵母）作为测试系统。一些植物木脂素表现出雌激素活性，而其他植物木脂素和半合成去甲木脂素则具有中度的抗雌激素活性。木脂素与雌激素受体 α 的蛋白质模型的对接在活性和非活性形式中支持了酵母雌激素测定的结果，并支持了植物木脂素作为植物雌激素的概念。
