环维黄杨星D对心肌钙离子通道的作用  

Effects of Cyclovirobuxine-D on Calcium Channels of Myocardium

作　　者：赖顺果[1] 杜一鸣 章蕴毅[1] 

机构地区：[1]复旦大学药学院药理教研室,上海200032 [2]麒麟鲲鹏药业有限公司,上海201203

出　　处：《复旦学报（医学版）》2005年第2期225-228,共4页Fudan University Journal of Medical Sciences

摘　　要：目的　研究环维黄杨星 D(CVB D)对心肌钙离子通道的作用 ,探讨其抗心律失常的电生理机制。方法　取豚鼠室间隔标本 ,37℃恒温 ,通混合氧 ,稳定 4 5min ,再以KCl 3mol/L灌充的微电极记录电刺激产生的动作电位 (AP) ,标本分为 3组 :(1)CVB D组 :每 5min依次累积加入浓度为 3× 10 -8,1× 10 -7,3× 10 -7,1×10 -6,3× 10 -6,1× 10 -5mol/L的CVB D ,分别记录AP ;(2 )CVB D +维拉帕米 (Ver)组 :加入维拉帕米 0 .1μmol/L ,10min时记录AP ,然后每 5min依次累积加入浓度为 3× 10 -8,1× 10 -7,3× 10 -7,1× 10 -6,3× 10 -6,1× 10 -5mol/L的CVB D ,分别记录AP ;(3)Ver组 :加入维拉帕米 0 .1μmol/L ,分别纪录 (2 )中相应时间点的AP。统计给药前后AP幅度 (APA)和时程 (APD)的变化。结果　CVB D对APA影响不大 ,但能显著延长APD ,延长幅度随着剂量的加大而增大 ;但在有维拉帕米存在的情况下 ,CVB D却能使APA和APD缩减 ,尤其是较高浓度1× 10 -6,3× 10 -6,1× 10 -5mol/L时 ,缩减幅度较为明显 ;而单纯加入维拉帕米后 ,APA和APD的改变轻微。结论　CVB D能影响细胞膜上的钙离子通道 ,促进细胞外钙离子内流 ,从而延长APD。当膜钙离子通道被阻断后 ,CVB D却缩短APD。因此可以认为CVB D除影响膜钙离子通道外 。Purpose To study the effects of cyclovirobuxine-D (CVB-D) on calcium channels of myocardium and evaluate the electrophysiological mechanism of antiarrhythmia. Methods Preparations of interventricular septum from guinea pig were gased with mixed oxygen and stabilized for 45 minutes while the bath temperature was 37?℃ constantly.Action potential (AP) caused by electricity was recorded via micropipette filled with 3 mol/L KCl.The preparations were divided into three groups:(1) CVB-D group:CVB-D of different concentrations (3×10 -8,1×10 -7,3×10 -7,1×10 -6,3×10 -6,1×10 -5)mol/L was added into the bath cumulately and AP was recorded every five minutes.(2) CVB-D+ verapamil (Ver) group:verapamil of 0.1 μmol/L was added into the bath firstly,10 minues later AP was recorded,then CVB-D of different concentrations (3×10 -8,1×10 -7,3×10 -7,1×10 -6,3×10 -6,1×10 -5)mol/L was added into the bath cumulately and AP was recorded every five minutes.(3) Ver group:verapamil of 0.1 μmol/L was added into the bath,AP,at the same time point as group (2),was recorded.The action potential amplitude (APA) and action potential duration (APD) of pre-administration with those of post-administration were compared. Results CVB-D had few effects on APA,but it could prolong APD prominently with dose-dependent manner.CVB-D was able to curtail both APA and APD while verapamil existed,especially at high concentrations (1×10 -6,3×10 -6,1×10 -5)mol/L.However,verapamil had slight effects on APA and APD. Conclusions CVB-D has effects on calcium channels in cell membrane,it hastens calcium ion flowing into the cell and thus prolongs APD.When calcium channels are blocked,CVB-D could shorten APD,which indicates that CVB-D has effects on other channels,such as potassium channels,etc.According to these results,it is worth concerning that combined medication of CVB-D and verapamil clinically might induce arrhythmia.

关 键 词：钙离子通道 环维黄杨星D 心肌 mol/L 维拉帕米 电生理机制 抗心律失常 微电极记录 APD 钙离子内流 APA 动作电位 显著延长 联合用药 室间隔 混合氧 电刺激 浓度 幅度 给药前 细胞外 钾通道 标本 累积 

分 类 号：R972[医药卫生—药品] R542.2[医药卫生—药学]