Estrogen-like activity of ginsenoside Rg1 derived from Panax notoginseng
Estrogen-like activity of ginsenoside Rg1 derived from Panax notoginseng
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DOI：
10.1210/jc.87.8.3691
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发表时间：
2002-08-01
影响因子：
5.8
通讯作者：
Wong, MS
中科院分区：
文献类型：
--
作者：
Chan, RYK;Chen, WF;Wong, MS
人参皂苷已被证实对中枢神经系统、心血管系统和内分泌系统有药理作用。我们假设人参皂苷可能通过与雌激素受体结合来调节它们的一些作用，因为它们在各种生理系统中具有雌激素的许多保护作用。本研究旨在确定人参皂苷Rg1是否能像雌激素类似物一样刺激人乳腺癌细胞生长，并激活HeLa细胞中雌激素反应元件-荧光素酶活性。Rg1，而不是它的苷元，以剂量依赖的方式刺激[甲基-(3)H]胸苷结合在雌激素受体阳性的MCF-7中(10（-15)-10(-7)W.）。3 × 10(-13) m Rg1对MCF-7细胞增殖的刺激可以被10(-6)m雌激素拮抗剂ICI 182780阻断。此外，Rg1在HeLa细胞中刺激雌激素反应元件-荧光素酶报告基因活性，最佳剂量为3 × 10(-10) m。这种刺激也可以被10(-6)m ICI 182780阻断。此外，Rg1对雌激素受体阴性的人乳腺癌细胞（MDA-MB-231）中[甲基-(3)H]胸苷的掺入没有影响。此外，Rg1未能取代[3 111 17 -雌二醇]与MCF-7细胞裂解物的特异性结合，这表明Rg1不需要与雌激素受体直接相互作用来发挥雌激素作用。我们的研究结果表明人参皂苷Rg1具有雌激素样活性，应该被归类为一类新的强效植物雌激素。
Ginsenosides have demonstrated pharmacological effects in the central nervous, cardiovascular, and endocrine systems. We hypothesize that ginsenosides might mediate some of their actions by binding to the estrogen receptor, as they share many of the protective actions of estrogen in various physiological systems. The present study is aimed to determine whether ginsenoside Rg1 can act like an estrogen analog in stimulating human breast cancer cell growth as well as in the activation of estrogen response element-luciferase activity in HeLa cell. Rg1, but not its aglycone, stimulates [methyl-(3)H] thymidine incorporation in estrogen receptor-positive MCF-7 in a dose-dependent manner (10(-15)-10(-7) W. The stimulation of MCF-7 cell proliferation by 3 x 10(-13) m Rg1 can be blocked by 10(-6) m of the estrogen antagonist ICI 182780. Moreover, Rg1 stimulates estrogen response element-luciferase reporter gene activity in HeLa cells with an optimal dose of 3 x 10(-10) m. Such stimulation can also be blocked by 10(-6) m ICI 182780. In addition, Rg1 has no effect on [methyl-(3)H]thymidine incorporation in estrogen receptor-negative human breast cancer cells (MDA-MB-231). Furthermore, Rg1 failed to displace the specific binding of [3 111 17beta-estradiol to MCF-7 cell lysates, suggesting that no direct interaction of Rg1 with estrogen receptor is needed for its estrogenic action. Our results indicate that ginsenosides Rg1 has estrogen-like activity and should be classified as a novel class of potent phytoestrogen.