College of Life Science, Institute of Biotechnology, Department of Bioscience and Biotechnology, Sejong University, Seoul 143-747.
Biomol Ther (Seoul). 2012 Mar;20(2):183-8. doi: 10.4062/biomolther.2012.20.2.183.
In this study, we examined the estrogenic activity of bavachin, a component of Psoralea corylifolia that has been used as a traditional medicine in Asia. Bavachin was purified from ethanolic extract of Psoralea corylifolia and characterized its estrogenic activity by ligand binding, reporter gene activation, and endogenous estrogen receptor (ER) target gene regulation. Bavachin showed ER ligand binding activity in competitive displacement of [(3)H] E2 from recombinant ER. The estrogenic activity of bavachin was characterized in a transient transfection system using ERα or ERβ and estrogen-responsive luciferase plasmids in CV-1 cells with an EC50 of 320 nM and 680 nM, respectively. Bavachin increased the mRNA levels of estrogen-responsive genes such as pS2 and PR, and decreased the protein level of ERα by proteasomal pathway. However, bavachin failed to activate the androgen receptor in CV-1 cells transiently transfected with the corresponding receptor and hormone responsive reporter plasmid. These data indicate that bavachin acts as a weak phytoestrogen by binding and activating the ER.
在这项研究中，我们研究了补骨脂素的雌激素活性，补骨脂素是Psoralea corylifolia 的一种成分，在亚洲被用作传统药物。补骨脂素从 Psoralea corylifolia 的乙醇提取物中被分离出来，并通过配体结合、报告基因激活和内源性雌激素受体 (ER) 靶基因调控来表征其雌激素活性。补骨脂素在从重组 ER 中竞争置换 [(3)H] E2 时显示出 ER 配体结合活性。在使用 ERα 或 ERβ 和雌激素反应性 luciferase 质粒的瞬时转染系统中，补骨脂素的雌激素活性的特征在于在 CV-1 细胞中，EC50 分别为 320 nM 和 680 nM。补骨脂素增加了雌激素反应基因如 pS2 和 PR 的 mRNA 水平，并通过蛋白酶体途径降低了 ERα 的蛋白水平。然而，补骨脂素未能激活在瞬时转染相应受体和激素反应报告质粒的 CV-1 细胞中的雄激素受体。这些数据表明，补骨脂素通过结合和激活 ER 作为一种弱植物雌激素发挥作用。
