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

Estrogenic activities of Psoralea corylifolia L. seed extracts and main constituents
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DOI:
10.1016/j.phymed.2011.02.002
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发表时间:
2011-03-15
期刊:
影响因子:
7.9
通讯作者:
Kim, Suna
Kim, Suna
中科院分区:
医学1区
文献类型:
--
作者:
Lim, Sun-Hye;Ha, Tae-Youl;Kim, Suna

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采用多种体外实验方法研究了补骨脂L乙醇提取物及其活性成分的雌激素样活性。乙醇提取物中的主要成分为白蜡酚、补骨脂素、异巴巴查尔酮、异巴伐木烯和巴伐豆素。在分级过程中,己烷和氯仿部分在酵母反式激活试验和E-Screen试验中显示出雌激素活性。在酵母反式激活实验中,乙醇提取物、正己烷和氯仿在浓度为1.0 ng/ml时显示出较高的活性,其中浓度为10(-6)M的巴克奇酚的活性最高,尤其是高于相同浓度的染料木素。在E-Screen实验中,Bakuchiol(10(-6)M)的细胞增殖活性与Genistein(10(-6)M)相似。在ER结合实验中,Bakuchiol表现出最强的ER结合亲和力(对ERα的IC50=1.01×10(-6)M,对ERβ的IC50=1.20×10(-6)M),并且对ERα的亲和力是对ERβ的5倍。(C)2011年爱思唯尔股份有限公司。版权所有。
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 (IC50 for ER alpha = 1.01 x 10(-6) M, IC50 for ER beta = 1.20 x 10(-6) M) and bakuchiol showed five times higher affinity for ER alpha than for ER beta. (C) 2011 Elsevier GmbH. All rights reserved.