蒺藜皂苷和多非利特对心律失常作用靶点的影响

doi:国家自然科学基金资助课题（30371739，3047

蒺藜皂苷和多非利特对心律失常作用靶点的影响

曲极冰,李红，李晶，陈立，杨世杰^*

吉林大学基础医学院药理学教研室，吉林长春130021

收稿日期:2005-03-20 修回日期:1900-01-01 出版日期:2005-09-28 发布日期:2005-09-28
通讯作者: 杨世杰

Effects of Gross Saponin of Tribulus Terrestris and Dofetilide on arrhythmic targets

QU Ji-bing, Li Hong, Li Jing, CHEN Li, YANG Shi-jie^*

Department of Pharmacology, School of Basic Medical Sciences,Jilin University, Changchun 130021, China

Received:2005-03-20 Revised:1900-01-01 Online:2005-09-28 Published:2005-09-28
Contact: YANG Shi-jie

摘要/Abstract

摘要： 目的：探讨蒺藜皂苷（GSTT）与多非利特（Dofetilide）抗心律失常作用及其机制。方法：采用结扎大鼠左冠状动脉前降支制备缺血性心律失常模型观察两药的抗心律失常作用；分离豚鼠心肌细胞并使用膜片钳记录Ikr和Ik1电流，探讨两药抗心律失常机制。结果：与模型组比较，10 mg·kg^-1多非利特组明显减少心肌缺血诱发大鼠心律失常次数，差异具有显著性（P<0.01），而20 mg·kg^-1 和 40 mg·kg^-1 GSTT组对大鼠心肌缺血引起的心律失常次数虽有减少趋势，但无统计学意义（P>0.05）；50 mg·L^-1和100 mg·L^-1 GSTT对Ikr、Ik1电流无明显影响，而5 μmol·L^-1多非利特可明显抑制Ikr和Ik1电流，与对照组比较差异具有显著性（P<0.01）。结论：多非利特对大鼠冠脉结扎诱发的缺血性心律失常有明显疗效，多非利特抗心律失常作用机制为抑制Ikr和Ik1；而GSTT对上述靶点无明显影响，未见GSTT明显抗心律失常作用。

关键词: 多非利特, 心律失常, Ikr, Ik1

Abstract: Objective To study the effects of Gross Saponin of Tribulus Terrestris(GSTT) and Dofetilide on arrhythmias and their mechanisms of antiarrhythmias. Methods Antiarrhythmic effects of GSTT and Dofetilide were observed by arrhythmic models of ligating rat left anterior descending coronary arteries and their antiarrhythmic mechanisms were investigated by isolating cardiac muscle cells in guinea pig and recording delayed outward potassium current(Ikr) and inwardly rectifying potassium current (Ik1) using whole-cell patch clamp technique. Results The number of arrhythmias was decreased significantly by Dofetilide with the dosage of 10 mg·kg^-1，compared with the controls（P<0.01）, however GSTT with the dosage of 20 and 40 mg·kg^-1 did not affect the number of arrhythmias（P>0.05）. Ikr and Ik1 could not be influenced by 50 and 100 mg·L^-1 GSTT, but 5 μmol·L^-1 Dofetilide could significantly reduce Ikr and Ik1 compared with the controls（P<0.01）. Conclusion The antiarrhythmic mechanisms of Dofetilide are probably related with its inhibiting Ikr and Ik1, GSTT has no effects on arrhythmias because it can not influence Ikr and Ik1.

Key words: Dofetilide, arrhythmias, Ikr, Ik1

中图分类号:

R965

曲极冰,李红，李晶，陈立，杨世杰. 蒺藜皂苷和多非利特对心律失常作用靶点的影响[J]. J4, 2005, 31(5): 665-667.

QU Ji-bing, Li Hong, Li Jing, CHEN Li, YANG Shi-jie. Effects of Gross Saponin of Tribulus Terrestris and Dofetilide on arrhythmic targets[J]. J4, 2005, 31(5): 665-667.

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