青蒿素衍生物对Na^+和K^+通道的抑制及其与普鲁卡因作用的比较  

THE INHIBITORY EFFECTS OF ARTEMISININ-DERIVATIVES ON Na^+ AND K^+ CHANNELS IN COMPARISON WITH THOSE OF PROCAINE

作　　者：黄汾生[1] 胡谦 施玉 

机构地区：[1]中国科学院上海生理研究所神经生物学开放实验室,上海200031

出　　处：《生理学报》1998年第2期145-152,共8页Acta Physiologica Sinica

基　　金：国家"八.五"攀登项目!"脑功能及其细胞和分子机制"支持课题

摘　　要：抗疟新药青蒿素（Artemisinin）的某些含氮衍生物在动物实验中还显示局部麻醉效应。本工作利用分化的NG108-15细胞，在全细胞电压箝位下，比较了五种青篙素衍生物和普鲁卡因对电压门控钢流（INa）和延迟整流钾流（IK）的作用。所观察的五种衍生物均部分可逆地和剂量依赖地抑制INa，其中含芳香环的SM541作用最强，效应与普鲁卡因的相近。300μmol／L普鲁卡因对IK只有微弱的抑制作用；而五种衍生物在相同浓度下均明显抑制IK，并加快它的失活；其中除SM541外，还观察到在药物持续灌流下，对IK幅度的抑制效应迅速降低。Some derivatives of artemisinin have been shown to have local anesthesia action. By using patch-clamp whole cell recording configuration, the effects of five artemisininderivatives on the voltage-gated INa and IK have been studied on differentiated NG108-15 cells with reference to procaine. The results showed that all the five artemisininderivaives clearly inhibited the voltage-gated sodium current (INa) of the cells in a dosedependent manner and the effect was partially reversibly. Among the five artemisininderivatives, SM541 has been shown to be most potent, approaching that of procaine.However, 300 μmol/L procaine showed only a slight inhibition of IK,whereas all the five derivatives at the same concentration not only decreased IK cleary, but also accelerated its inactivation. Except for SM541,the inhibitory effects on IK decreased rapidly with perfusion of the rest 4 derivatives.

关 键 词：青蒿素衍生物 普鲁卡因 钠通道 钾通道 

分 类 号：R978.61[医药卫生—药品]