目的:研究不同产地的10种卷柏雌激素样活性。方法:采用MCF-7细胞增殖实验与小鼠子宫增重实验结合,进行不同产地卷柏雌激素样活性筛选;结合血清药理学实验综合评价雌激素样活性;以p ERE-TAL-luc、pβgal-Control、p CXN2-h ERα或p CXN2-h ERβ转染HEK293细胞,雌激素应答元件(ERE)调控的报告基因瞬时表达检测,探讨卷柏发挥雌激素样作用的途径。结果:卷柏属植物卷柏(JB6)和江南卷柏(JB7)能明显升高小鼠的子宫系数,与空白组相比有显著性差异(P〈0.01);JB6和JB7可显著促进MCF-7细胞增殖;JB6和JB7不论由雌激素受体(ER)α或ERβ介导均具有雌激素活性,与ERα的亲和力高于ERβ。结论:JB6和JB7具有雌激素样活性,其中JB6的雌激素样作用强于JB7。卷柏激活基因转录发挥雌激素样作用主要是通过ERα介导的。
Objective: To research the estrogenic activity of ten kinds of Selaginella tamariscina from ten different place of origin. Methods: The estrogenic activity of ten kinds of Selaginella tamariscina from different regions was screened by the method of combining the experiment of cell proliferation test of MCF-7 with the experiment of murine uterus weight. The estrogenic activity was comprehensively evaluated by serum pharmacology experiment, pERE-TAL-Iuc, p β gal-Control and pCXN2-hER α or pCXN2-hER β were transfected into HEK293 cells. The pathway by which Selaginella tamariscina exerted estrogenic activity was tested by the transient expression detection of reporter gene controlled by ERE. Results: Selaginella tamariscina (P. Beauv.) Spring (JB6) and Selaginella moeIlendorffii Hieron (JB7) could increase the murine uterus coefficient, and there was significant difference compared with the normal group (P〈0.01). JB6 and JB7 could promote the proliferation of MCF- 7 cells. JB6 and JB7 had the estrogenic activity regardless of whether mediated by ERα or ER β, and the affinity with ER α was higher than ER β. Conclusion: JB6 and JB7 has the estrogenic activity, and the estrogenic activity of JB6 is stronger than JB7. Selaginella tamariscina exerts estrogenic activity by activating gene transcription mediated by ERα.