淫羊藿苷衍生物的制备及其雌激素样作用研究

被引：35

作者：

叶海涌

刘健

楼宜嘉

机构：

[1] 浙江大学药学院

[2] 浙江大学药学院浙江杭州

[3] 浙江杭州

来源：

浙江大学学报(医学版) | 2005年 / 02期

关键词：

淫羊藿苷; 淫羊藿素; 去甲淫羊藿素; MCF-7细胞; T47D细胞; 植物雌激素;

D O I：

暂无

中图分类号：

R284.1 [化学分析与鉴定]; R285 [中药药理学];

学科分类号：

1008 ;

摘要：

目的研究淫羊藿苷(icariin,ICA)及其衍生物淫羊藿素(icaritin,ICT)和去甲淫羊藿素(desmethyli-caritin,DICT)的雌激素样作用及其相关的构效关系。方法ICA经纤维素酶水解成ICT,进一步在BBr3和CH2Cl2的体系中反应生成DICT;用不同浓度的化合物与雌激素敏感性人乳腺癌细胞株MCF-7和T47D分别共培养6d和9d,MTT法检测其对细胞的促增殖率,以此评价化合物雌激素样作用的强弱。结果ICT、DICT促细胞增殖作用显著,10-6mol/L浓度时促MCF-7细胞增殖作用分别是雌二醇(10-9mol/L)的90.0%和94.0%(P<0.01);促T47D细胞增殖作用分别是雌二醇的65.6%,50.0%(P<0.01)。ICA未呈现促MCF-7细胞和T47D细胞增殖作用。ICT、DICT的促细胞增殖作用被10-7mol/L雌激素受体完全拮抗剂ICI182、780完全抑制。结论ICT和DICT具有促MCF-7细胞和T47D细胞增殖的雌激素样作用,而ICA未体现该作用。

引用

收藏

页码：40 / 45

页数：6

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