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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

黄汾生, 胡谦, 施玉

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

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。该工作利用分化的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[I_(Na)]和延迟整流钾流[I_(K)]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I_(Na)，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I_(K)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I_(K)，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I_(K)幅度的抑制效应迅速降低。

关键词： 青蒿素衍生物; 普普卡因; 全细胞记录; I_(Na); I_(K) NG108-15细胞系

The inhibitory effects of artemisininderivatives on Na~(+)and K~(+)channels incomparison with those of procaine

Huang Fensheng, Hu Qian, Shi Yuliang

Key Laboratory of Neurobiology，Shanghai Institute of Physiology，Chinese Academy of Sciences. Shanghai 200031,Chian

Abstract

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 I_(Na) and I_(K) 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 [I_(Na)] 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 #mu#mol/L procaine showed only a slight inhibition of I_(K),whereas all the five derivatives at the same concentration not only decreased I_(K) cleary, but also accelerated its inactivation. Except for SM541,the inhibitory effects on I_(K) decreased rapidly with perfusion of the rest 4 derivatives.

Key words: Artemisinin-derivatives;Procaine;Whole cell recording;I_(Na);I_(K)

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引用本文：

黄汾生, 胡谦, 施玉. 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 [J]. 生理学报 1998; 50 (2): .

Huang Fensheng, Hu Qian, Shi Yuliang . The inhibitory effects of artemisininderivatives on Na~(+)and K~(+)channels incomparison with those of procaine. Acta Physiol Sin 1998; 50 (2): (in Chinese with English abstract).