五甲基槲皮素对豚鼠心肌收缩力和电生理特性的影响  

Effects of Pentamethylquercetin on Contractility and Electrophysiology of Cardiac Muscle in Guinea Pigs

作　　者：张晓华[1] 刘祖梅[1] 何婷[1] 杨斐[1] 金满文[1] 

机构地区：[1]华中科技大学同济医学院基础医学院药理学系,武汉430030

出　　处：《华中科技大学学报（医学版）》2008年第6期757-760,768,共5页Acta Medicinae Universitatis Scientiae et Technologiae Huazhong

基　　金：国家自然科学基金资助项目(No.04510096)

摘　　要：目的比较研究五甲基槲皮素(PMQ)和槲皮素(QUE)对离体豚鼠心肌收缩力和电生理特性的影响并探讨其机制。方法测定离体豚鼠右心房肌自律性及左心房肌收缩力;同步记录豚鼠心乳头肌动作电位和收缩力;全细胞膜片钳技术记录豚鼠心室肌细胞L型钙电流(ICa.L)。结果10、30、100μmol/LPMQ和QUE均可增强左心房肌收缩力;PMQ对右心房自律性无明显作用,QUE则可提高右心房自律性。30、100μmol/LPMQ对豚鼠心乳头肌动作电位无明显影响,QUE可延长豚鼠心室肌动作电位时程;QUE增强乳头肌收缩力的作用强于PMQ。PMQ与QUE均抑制ICa.L,后者作用更强。结论PMQ与QUE均可增强豚鼠心肌收缩力;PMQ与QUE对豚鼠右心房自律性的作用趋势相反;PMQ对乳头肌动作电位无明显作用,对心室肌细胞ICa.L的抑制作用弱于QUE。首次揭示了PMQ在心脏方面的作用,为该类药物在临床的应用提供了有价值的参考信息。Objective To investigate the effects of 3, 3′, 4′ , 5, 7-pentamethylquercetin （PMQ） on contractility and electrophysiology of cardiac muscle in guinea pigs. Methods The effects of PMQ on contractility of left atrium and autorhythmicity of right atrium were investigated. Action potentials and contractility of isolated papillary muscle in guinea pigs were simultaneously examined by using standard microelectrode technique. The effects of PMQ on voltage-dependent L-type Ca^2＋ current of cardiomyocytes were assessed by applying whole-cell patch clamp techniques. Results Ten, 30 and 100 μmol/LPMQ or QUE produced positive inotropic effects in left atriums. PMQ had no effects on autorhythmicity but QUE produced a positive chronotropic action of right atrium. Ten and 30 μmol/L QUE increased the contractility and prolonged the APD of papillary muscles. Thirty and 100μmol/L PMQ increased the contractility but had no effects on parameters of action potential of papillary muscles. PMQ decreased ICa. L in ventricular myocytes of guinea pigs, but the potency was much weaker than QUE. Conclusion Both PMQ and QUE produce positive inotropic effects of cardiac muscles in guinea pigs. The effect of PMQ on autorhythmicity of right atrium is opposite to QUE. PMQ has no effects on action potential of cardiac papillary muscle and its effects inhibiting L-type calcium current were weaker than QUE.

关 键 词：五甲基槲皮素 槲皮素 收缩力 动作电位 钙电流 

分 类 号：R972[医药卫生—药品]