小檗碱对腹主动脉狭窄性心肌病大鼠心肌细胞钾电流的抑制作用  

Effects of Berberine on Potassium Current in Myocardial Cells of Cardiomyopathic Rats Induced by Abdominal Aorta Constriction

作　　者：张伟东[1] 林木森[1] 于锋[1] 

机构地区：[1]中国药科大学药理研究室,江苏南京210009

出　　处：《药学进展》2010年第2期75-80,共6页Progress in Pharmaceutical Sciences

基　　金：国家自然科学基金资助项目(No.30572193);教育部博士学科点专项科研基金资助项目(No.20050316009)

摘　　要：目的:研究小檗碱对腹主动脉狭窄性心肌病模型大鼠的心肌细胞中瞬时外向钾电流(Ito)和内向整流钾电流(IK1)的抑制作用,并探讨其作用机制。方法:对大鼠进行腹主动脉狭窄手术建立心肌病模型,以急性酶解法分离大鼠单个左心室肌细胞,用全细胞膜片钳技术记录钾电流。结果:相比于假手术组,心肌病模型组大鼠心肌细胞Ito和IK1的电流密度明显增加;小檗碱(10～100μmol.L-1)可浓度依赖性降低模型组大鼠心肌细胞Ito电流密度,IC50为(43.61±4.31)μmol.L-1,并使Ito稳态失活曲线向负电位方向移动,半数失活电压减少,而对Ito稳态激活曲线和Ito失活后恢复曲线无明显影响;此外,小檗碱可显著降低模型组大鼠心肌细胞IK1电流密度。结论:小檗碱对腹主动脉狭窄所致心肌病中出现异常增大的Ito和IK1离子流有明显阻断作用。Objective：To investigate the effects of berberine on the transient outward potassium current（Ito） and inward rectified potassium current（IK1） in isolated hypertrophied rat myocardial cells.Methods：SD rats were randomly divided into two groups：control group and cardiomyopathy group.Abdominal aorta constriction operation was conducted in cardiomyopathy group to establish myocardial cells hypertrophied model.The single myocardial cells of rats were obtained by enzymatic dissociation,then Ito and IK1 were recorded by using whole cell patch clamp technique.Results：Compared with control group,the current density of Ito and IK1 in model group increased significantly;Berberine（10～100 μmol ·L-1） concentration-dependently reduced Ito of myocardial cells in model group,and IC50 was（43.61±4.31） μmol ·L-1.Berberine shifted the inactivation curve of Ito to more negative potential.However,it did not affect the activation and deinactivation curve of Ito.Moreover,it could reduce IK1 of myocardial cells in model group.Conclusion：Berberine can inhibit Ito and IK1 of myocardial cells of cardiomyopathic rats induced by abdominal aorta constriction.

关 键 词：小檗碱 心肌病大鼠模型 腹主动脉狭窄 心肌细胞 瞬时外向钾电流 内向整流钾电流 

分 类 号：R285[医药卫生—中药学]