E0703对雌激素受体(ER)不同亚型的选择性激活作用

目的探讨E0703(雌二醇衍生物)对雌激素受体不同亚型(α和β)的选择性激活作用。方法将报告基因质粒pTAL-SEAP-ERE和校正质粒pSV-β-gal共转染已稳定转染了雌激素受体α/β的人胚肾细胞(HEK293),加入E0703进行报告基因的诱导表达。采用EMSA试验观察E0703对ERα与雌激素反应元件(ERE)的结合增强作用。结果E0703对ERα具有较强的激活作用(最低激活浓度为10-8mol·L-1),激活强度略低于E2;E0703在10-10、10-9、10-8、10-7mol·L-1浓度下对ERβ没有激活作用;EMSA试验证明,E0703能够增强ERα与雌激素反应元件的结合增强作用。结论E0703对雌激素受体α具有选择性激活作用。

The selective activation effect of E0703 on different estrogen receptor subtypes

Aim To investigate the selective activation effect of E0703 on different estrogen receptor subtype.Methods Reporter gene plasmid pTAL-SEAP-ERE and rectification plasmid pSV-β-gal were co-transfected into HEK293 cells which had been stably transfected with estrogen receptor(ER)α or β.The expression of reporter gene was detected by SEAP chemoluminescence detection system.Enhancement of the binding effect between ERα and ERE induced by E0703 was investigated by EMSA.Results ERα was activated by E0703 at a lowest concentration of 10-8 mol·L-1,while ERβ was not activated under the concentration of 10-10,10-9,10-8 and 10-7 mol·L-1.EMSA assay also showed that the binding effect between ERα and ERE was induced by E0703.Conclusion E0703 can selectively activate ERα.