Resveratrol, a polyphenolic compound found in grapes and wine, is an agonist for the estrogen receptor
Resveratrol, a polyphenolic compound found in grapes and wine, is an agonist for the estrogen receptor
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DOI：
10.1073/pnas.94.25.14138
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发表时间：
1997-12-09
影响因子：
11.1
通讯作者：
Jameson, JL
中科院分区：
文献类型：
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作者：
Gehm, BD;McAndrews, JM;Jameson, JL
据报道，葡萄和葡萄酒中含有的植物化学物质白藜芦醇具有多种抗炎、抗血小板和抗癌作用。基于其结构与合成雌激素二乙基己烯雌酚的相似性，我们研究了白藜芦醇是否可能是一种植物雌激素。当浓度（约3-10 μ M）与其其他生物学效应所需的浓度相当时，白藜芦醇抑制标记雌二醇与雌激素受体的结合，并激活转染到人乳腺癌细胞的雌激素应答报告基因的转录。这种转录激活依赖于雌激素受体，需要报告基因中的雌激素反应元件，并被特异性雌激素拮抗剂抑制。在某些细胞类型（如MCF-7细胞）中，白藜芦醇作为Ii超激动剂发挥作用（即产生比雌二醇更大的最大转录反应），而在另一些细胞类型中，白藜芦醇产生的激活作用等于或低于雌二醇。白藜芦醇还增加了天然雌激素调节基因的表达，并刺激了雌激素依赖性T47D乳腺癌细胞的增殖。我们认为白藜芦醇是一种植物雌激素，在不同的试验中表现出不同程度的雌激素受体激动作用。系统。白藜芦醇的雌激素作用扩大了其生物作用的范围，可能与报道的饮用葡萄酒对心血管的益处有关。
The phytochemical resveratrol, which is found in grapes and wine, has been reported to have a variety of anti-inflammatory, anti-platelet, and anticarcinogenic effects. Based on its structural similarity to diethylstilbestrol, a synthetic estrogen, we examined whether resveratrol might be a phytoestrogen, At concentrations (approximate to 3-10 mu M) comparable to those required for its other biological effects, resveratrol inhibited the binding of labeled estradiol to the estrogen receptor and it activated transcription of estrogen-responsive reporter genes transfected into human breast cancer cells. This transcriptional activation was estrogen receptor-dependent, required an estrogen response element in the reporter gene, and was inhibited by specific estrogen antagonists. In some cell types (e.g., MCF-7 cells), resveratrol functioned as Ii superagonist (i.e., produced a greater maximal transcriptional response than estradiol) whereas in others it produced activation equal to or less than that of estradiol, Resveratrol also increased the expression of native estrogen-regulated genes, and it stimulated the proliferation of estrogen-dependent T47D breast cancer cells. Wt conclude that resveratrol is a phytoestrogen and that it exhibits variable degrees of estrogen receptor agonism in different test. systems. The estrogenic actions of resveratrol broaden the spectrum of its biological actions and may be relevant to the reported cardiovascular benefits of drinking wine.