山西医科大学学报2017，Vol.48Issue(4)：301-305,5.DOI:10.13753/j.issn.1007-6611.2017.04.001
奎尼丁对HEK293细胞hERG电流和hERG蛋白的影响
Effects of quinidine on hERG potassium current and hERG channel protein in HEK293 cell line
摘要
Abstract
Objective To explore the effect of quinidine on ether-a-go-go related gene(hERG)current and hERG channel protein and its possible mechanism of quinidine-induced long QT syndrome.Methods HEK293 cells were transiently transfected with plasmid containing hERG gene via Lipofectamine.The hERG current was observed by whole-cell patch-clamping and the expression of hERG channel protein was detected by Western blot analysis.①HEK293 cells were transfected with plasmid,and after 48 h the cells were treated with different concentrations(0,1,3,10 μmol/L)of quinidine and patch clamp experiments were operated for instantaneous effect of quinidine.②HEK293 cells were transfected into plasmid for 24 h,then treated with different concentrations of quinidine(1,3,10 μmol/L)for 24 h,and then the patch clamp and Western blot were operated to observe the chronic effect of quinidine.Results After HEK293 cells were transfected into the plasmid for 48 h,the hERG current was significantly inhibited after treated with different concentrations of quinidine.The maximal density of tail currents were(55.9±3.8)pA/pF,(35.7±3.2)pA/pF and(15.5±1.4)pA/pF in 1 μmol/L,3 μmol/L and 10 μmol/L quinidine groups,respectively(P<0.05 vs 0 μmol/L).HEK293 cells were transfected into plasmid for 24 h and cultured with different concentrations of quinidine for 24 h,the hERG current showed no significant change.Western blot result showed that there was no significant change in the expression of hERG protein in HEK293 cells cultured with different concentrations of quinidine.Conclusion Quinidine shows an immediate and direct inhibitory effect on hERG potassium current,but it does not affect the expression of hERG channel protein.The direct inhibition of hERG channel is the basic mechanism of long QT syndrome caused by quinidine.关键词
长QT间期综合征/奎尼丁/hERG/HEK293Key words
long QT syndrome/quinidine/hERG/HEK293分类
医药卫生引用本文复制引用
霍建华,郭雪艳,强华,刘平,白玲,马爱群..奎尼丁对HEK293细胞hERG电流和hERG蛋白的影响[J].山西医科大学学报,2017,48(4):301-305,5.基金项目
国家自然科学基金资助项目(30801133) （30801133）
陕西省自然科学基础研究计划项目(2014JM2-8154) （2014JM2-8154）
