Proliferation-stimulating effects of icaritin and desmethylicaritin in MCF-7 cells
Proliferation-stimulating effects of icaritin and desmethylicaritin in MCF-7 cells
复制标题
DOI：
10.1016/j.ejphar.2004.10.002
复制
发表时间：
2004-11-19
影响因子：
5
通讯作者：
Lou, YJ
中科院分区：
文献类型：
--
作者：
Wang, ZQ;Lou, YJ
淫羊藿苷、淫羊藿苷和去甲基淫羊藿苷是淫羊藿中与染料木素和大豆苷元结构相似的成分。使用改良的MCF-7细胞增殖测定（E-SCREEN评估系统），测试这些化合物的雌激素样活性。淫羊藿苷和去甲基淫羊藿苷，而不是淫羊藿苷，强烈刺激MCF-7/BUS细胞的增殖。细胞周期分析显示，增殖刺激作用与S期MCF-7/BUS细胞数量的显著增加和G2/ M群体的显著增加相关，其作用与雌二醇相似。这些作用是剂量依赖性的（范围从1 nM到10 μ M），并且可以被特异性雌激素受体拮抗剂ICI 182，780 [7 α-[9（4，4，5，5，5-五氟戊基）亚磺酰基]壬基）-雌甾-1，3，5（10）-三烯-3，17 β-二醇）]显著抑制。淫羊藿苷或去甲基淫羊藿苷处理24 h内可增加雌激素受体调节的孕激素受体和PS2 mRNA水平，ICI 182，780也可逆转这种作用。结果表明，淫羊藿苷和去甲基淫羊藿苷是新的植物雌激素，淫羊藿苷和去甲基淫羊藿苷的雌激素效应是由雌激素受体介导的。(C)2004 Elsevier B. V.保留所有权利。
Icariin, icaritin and desmethylicaritin are constituents of Epimedium with a similar structure to genistein and daidzein. Using the modified MCF-7 cell proliferation assay (E-SCREEN assessment system), these compounds were tested for their estrogen-like activities. Icaritin and desmethylicaritin, but not icariin, strongly stimulated the proliferation of MCF-7/BUS cells. Cell cycle analysis revealed that the proliferation stimulatory effect was associated with a marked increase in the number of MCF-7/BUS cells in S phase and a significant increase in the G2/ M population, with effects similar to those of estradiol. These actions were dose dependent (range from 1 nM to 10 muM) and could be significantly inhibited by the specific estrogen receptor antagonist ICI 182,780 [7 alpha-[9(4,4,5,5,5-pentafluoropentyl)sulfinyl]nonyl)-estra-1,3,5(10)-triene-3,17beta-diol)]. The estrogen receptor-regulated progesterone receptor and PS2 mRNA levels were increased by treatment with icaritin or desmethylicaritin within 24 h and the effects were also reversed by ICI 182,780. It was concluded that icaritin and desmethylicaritin are novel phytoestrogens and that the estrogenic effects of icaritin and desmethylicaritin are mediated by the estrogen receptor. (C) 2004 Elsevier B.V. All rights reserved.