补骨脂种子提取物及其主要成分的雌激素活性。

Estrogenic activities of Psoralea corylifolia L. seed extracts and main constituents.

机构信息

Food Function Research Group, Korea Food Research Institute, Seongnam-Si, Republic of Korea.

出版信息

Phytomedicine. 2011 Mar 15;18(5):425-30. doi: 10.1016/j.phymed.2011.02.002. Epub 2011 Mar 6.

DOI:10.1016/j.phymed.2011.02.002

Abstract

Estrogenic activities of ethanol extract and its active components from Psoralea corylifolia L. were studied using various in vitro assays. The main components from ethanol extract were analyzed to be bakuchiol, psoralen, isobavachalcone, isobavachromene, and bavachinin. In a fractionation procedure, hexane and chloroform fractions showed estrogenic activity in yeast transactivation assay and E-screen assay. In yeast transactivation assay, ethanol extract, hexane, and chloroform fractions showed significantly higher activities at a concentration of 1.0 ng/ml, and bakuchiol at the concentration of 10(-6) M was showed the highest activity, especially, which was higher than genistein at the same concentration. In E-screen assay, cell proliferation of bakuchiol (10(-6) M) showed similar estrogenic activity with genistein (10(-6) M). In ER binding assay, bakuchiol displayed the strongest ER-binding affinity (IC(50) for ERα=1.01×10(-6) M, IC(50) for ERβ=1.20×10(-6) M) and bakuchiol showed five times higher affinity for ERα than for ERβ.

摘要

采用多种体外检测方法研究了补骨脂中乙醇提取物及其活性成分的雌激素活性。从乙醇提取物中分析得到的主要成分有补骨脂酚、补骨脂素、异补骨脂查尔酮、异补骨脂素和补骨脂定。在分级程序中，正己烷和氯仿部分在酵母转录激活测定和 E-screen 测定中显示出雌激素活性。在酵母转录激活测定中，乙醇提取物、正己烷和氯仿部分在浓度为 1.0ng/ml 时表现出明显更高的活性，而浓度为 10(-6)M 的补骨脂酚表现出最高的活性，特别是其活性高于相同浓度的染料木黄酮。在 E-screen 测定中，补骨脂酚（10(-6)M）的细胞增殖显示出与染料木黄酮（10(-6)M）相似的雌激素活性。在 ER 结合测定中，补骨脂酚显示出最强的 ER 结合亲和力（IC(50)对于 ERα=1.01×10(-6)M，IC(50)对于 ERβ=1.20×10(-6)M），并且补骨脂酚对 ERα 的亲和力比 ERβ 高五倍。