Crebanine inhibits voltage-dependent Na～+ current in guinea-pig ventricular myocytes

作     者：HE Xiao-Shan LIN Qing MA Yun-Shu YU Ze-Pu 

作者机构：Yunnan University of Traditional Chinese Medicine 

出 版 物：《Chinese Journal of Natural Medicines》 (中国天然药物（英文版）)

年 卷 期：2014年第12卷第1期

页      面：20-23页

核心收录：

学科分类：0710[理学-生物学] 1008[医学-中药学(可授医学、理学学位)] 1007[医学-药学(可授医学、理学学位)] 1006[医学-中西医结合] 1005[医学-中医学] 1002[医学-临床医学] 0703[理学-化学] 100602[医学-中西医结合临床] 10[医学] 

基　　金：supported by the Natural Science Foundation of Yunnan Province(No.2002C0006Z) National Natural Science Foundation of China(No.81060371) 

主　　题：中药学 中药材 植物药 药理分析 

摘      要：AIM: To study the effects of crebanine on voltage-gated Na+ channels in cardiac tissues. METHODS: Single ventricular myocytes were enzymatically dissociated from adult guinea-pig heart. Voltage-dependent Na+ current was recorded using the whole cell voltage-clamp technique. RESULTS: Crebanine reversibly inhibited Na+ current with an IC50 value of 0.283 mmol?L-1(95% confidence range: 0.248-0.318 mmol?L-1). Crebanine at 0.262 mmol?L-1 caused a negative shift(about 12 mV) in the voltage-dependence of steady-state inactivation of Na+ current, and retarded its recovery from inactivation, but did not affect its activation curve. CONCLUSION: In addition to blocking other voltage-gated ion channels, crebanine blocked Na+ channels in guinea-pig ventricular myocytes. Crebanine acted as an inactivation stabilizer of Na+ channels in cardiac tissues.