Park Joonwoo, Shim Myeongkuk, Rhyu Mee-Ra, Lee YoungJoo
College of Life Science, Institute of Biotechnology, Department of Bioscience and Biotechnology, Sejong University, Seoul, Korea.
Pharmazie. 2012 Nov;67(11):947-50.
Cimicifuga racemosa extracts have long been used to treat female reproductive disorders both in Asia and Europe. Here in this study, we examined the possible estrogen receptor (ER)alpha effects of Cimicifuga heracleifolia var. bifida ethanol extract (C-Ex), which has been used traditionally in Asia, in MCF-7 cells. The activity of C-Ex was characterized in a transient transfection system, using ERa and estrogen-responsive luciferase plasmids in HEK 293 cells and endogenous target genes were studied in MCF-7 cells. C-Ex failed to activate ERalpha and at a concentration of 0.005-0.5 mg/ml as examined by reporter activity. In addition, no statistically significant antiestrogenic activity was observed. However, to our interest, C-Ex enhanced expression of VEGF at 0.5 mg/ml concentration and repressed ERalpha both at the mRNA and protein levels in MCF-7 cells. These results suggested that C-Ex does not activate or inactivate ERalpha in a direct manner, but the extracts may affect factors in ER signal transduction pathway.
升麻提取物在亚洲和欧洲长期以来都被用于治疗女性生殖系统紊乱。在本研究中，我们检测了传统上在亚洲使用的二裂叶升麻乙醇提取物（C-Ex）对MCF-7细胞中雌激素受体（ER）α的可能作用。C-Ex的活性在瞬时转染系统中进行表征，在HEK 293细胞中使用ERα和雌激素反应性荧光素酶质粒，并在MCF-7细胞中研究内源性靶基因。通过报告基因活性检测，C-Ex在0.005-0.5mg/ml浓度下未能激活ERα。此外，未观察到统计学上显著的抗雌激素活性。然而，有趣的是，C-Ex在0.5mg/ml浓度下增强了MCF-7细胞中VEGF的表达，并在mRNA和蛋白质水平上抑制了ERα。这些结果表明，C-Ex不会直接激活或失活ERα，但该提取物可能影响ER信号转导途径中的因子。
