雷洛昔芬对血管内皮细胞雌激素应答元件转录活性的影响  

Effect of selective estrogen receptor modulator raloxifene on estrogen responsive element transcriptional activity in vascular endothelial cells

作　　者：贺红[1] 杨发林[2] 吴逸南 王欣[4] 许伟华[4] 

机构地区：[1]山东大学齐鲁医院心内科,山东济南250000 [2]山东大学齐鲁医院检验科,山东济南250012 [3]山东省铁路中心医院内科,山东济南250000 [4]山东大学第二医院内科,山东济南250000

出　　处：《中国病理生理杂志》2004年第8期1434-1436,共3页Chinese Journal of Pathophysiology

摘　　要：目的 :研究选择性雌激素受体调节剂 (SERM)雷洛昔芬 (raloxifene)对血管内皮细胞雌激素应答元件(ERE)转录活性的影响。方法 :首先构建ERE荧光素酶报告基因质粒 (ERE -TK -Luc) ,然后采用真核细胞转染技术将ERE -TK -Luc与内参照质粒PRL -SV4 0一起转染体外培养的血管内皮细胞 ,检测raloxifene刺激的转染细胞荧光素酶的相对活性 ,与未用药的转染细胞进行比较。并同时采用raloxifene与雌二醇 (E2 )共同处理细胞 ,观察ralox ifene对E2 作用的影响。结果 :在raloxifene处理的转染细胞中荧光素酶表达量低于未用药的转染细胞 ,raloxifene浓度为 10 -7mol/L时更明显 (P <0 0 1) ;E2 可使转染细胞荧光素酶表达量明显高于未给药组 (P <0 0 1) ,而raloxifene与E2 同时处理则细胞荧光素酶表达水平与对照组相近 (P <0 0 1)。结论AIM: To assess the effect of raloxifene, a selective estrogen modulator, on the transcriptional activity of estrogen responsive element (ERE) in vascular endothelial cells. METHODS: Vascular endothelial cells were transfected with ERE-TK-Luc reporter plasmid and PRL-SV40 control plasmid via FuGENE 6. The activities of firefly luciferase and renilla luciferase were measured with dual-luciferase reporter assay system. The transcriptional activity in transfected cells treated with raloxifene was compared with that in untreated cells. Furthermore, raloxifene was used to cotreat the cells with estradiol (E_2) and the influence of raloxifene to the effect of E_2 was assessed. RESULTS: Compared to untreated cells, the luciferase activity in cells treated with raloxifene decreased and showed significance at concentration of 10^(-7)mol/L (P<0.01). The luciferase activity in cells increased when treated with E_2 (P<0.01), while raloxifene reversed the increase significantly (P<0.01). CONCLUSION: Raloxifene inhibits the ERE transcription activity in vascular endothelial cells.

关 键 词：选择性雌激素受体调节剂 雷洛昔芬 血管内皮细胞 

分 类 号：R363[医药卫生—病理学]