上海交通大学学报（医学版）

上海交通大学学报（医学版） >

2017 , Vol. 37 >Issue 2: 177

DOI: https://doi.org/10.3969/j.issn.1674-8115.2017.02.009

论著（基础研究）

包公藤甲素衍生物(S)-OTS·HCl的心脏电生理效应

  • 王红卫 ,
  • 张颖 ,
  • 李慈珍 ,
  • 刘远谋 ,
  • 杨智昉
展开
  • 1. 上海健康医学院基础医学院生理教研室，上海 201318；2. 上海交通大学基础医学院实验中心，上海 200025；3. 上海交通大学基础医学院生理教研室，上海 200025
王红卫（1967—），男，副教授，硕士；电子信箱：jywanghw@shsmu.edu.cn。

网络出版日期: 2017-02-28

基金资助

上海科学技术委员会重点资助项目（06JC14045）；上海教育委员会科研创新项目（13yz150）；上海健康医学院附属卫生学校课题（FA1-390316-117067）

收起

Cardiac electrophysiological effect of (S)-OTS·HCl, a derivative of Baogongteng A

  • WANG Hong-wei ,
  • ZHANG Ying ,
  • LI Ci-zhen ,
  • LIU Yuan-mou ,
  • YANG Zhi-fang
Expand
  • 1. Department of Physiology, Shanghai University of Medicine and Health Science, Shanghai 201318, China; 2. Experimental Center, Basic Medicine Faculty of Shanghai Jiao Tong University, Shanghai 200025, China; 3. Department of Physiology, Basic Medicine Faculty of Shanghai Jiao Tong University,Shanghai 200025, China

Online published: 2017-02-28

Supported by

Key Project of Science and Technology Commission of Shanghai Municipality, 06JC14045; Scientific Research Innovation Project of Shanghai Education
Committee, 13yz150; Subject of Health School Affiliated to Shanghai University of Medicine and Health Sciences, FA1-3903-16-117067

Fold

摘要

目的 ·研究(S)-OTS · HCl对心脏生物电活动的影响。方法 ·运用细胞内生物电记录、心电图及Langendorff心脏灌流技术，在离体和在体情况下研究(S)-OTS · HCl对豚鼠和家兔心脏的作用。结果 · (S)-OTS · HCl可与M2型胆碱能受体结合，并在动物整体心电图记录中剂量依赖性地延长RR间期。(S)-OTS · HCl对心室肌的静息电位（RP）、动作电位幅值（APA）和动作电位最大上升速率（Vmax）没有影响，但(S)-OTS · HCl（1×10-5 mol/L）可显著缩短动作电位时程APD50和APD90分别至91.6%和90.9%。当(S)-OTS · HCl（1×10-7 mol/L）灌流家兔窦房结标本时，可使4期自动除极速率缩短至13.7%，也可有效抑制钙通道，并使窦房结自律性动作电位的APA和Vmax减小。离体心肌收缩力亦随(S)-OTS · HCl的剂量增加而降低。结论 · (S)-OTS · HCl是一个作用较强的胆碱能受体激动剂，能与心肌M2受体结合，产生负性变时、变力和变传导效应。

关键词： (S)-OTS ·; HCl；胆碱能受体激动剂；动作电位；心电图

本文引用格式

王红卫 , 张颖 , 李慈珍 , 刘远谋 , 杨智昉 . 包公藤甲素衍生物(S)-OTS·HCl的心脏电生理效应[J]. 上海交通大学学报（医学版）, 2017 , 37(2) : 177 . DOI: 10.3969/j.issn.1674-8115.2017.02.009

Abstract

Objective · To study the electrophysiological effect of (S)-OTS·HCl on the heart. Methods · The conventional intracellular recording, electrocardiograph (ECG) and Langendorff cardiac perfusion technique were employed to investigate the effect of (S)-OTS·HCl on in-vivo and in-vitro hearts of guinea pigs and rabbits. Results · (S)-OTS·HCl could bind to M2 muscarinic receptors and dose-dependently prolong the RR intervals significantly in vivo. It had no effect on resting potential (RP), action potential amplitude (APA), and maximum upstroke velocity of phase 0 (Vmax) of ventricular myocytes. Instead, 1×10-5 mol/L (S)-OTS·HCl could shorten the action potential duration at 50 percent repolarization (APD50) and APD90 to 91.6% and 90.9%, respectively. And the spontaneous depolarization rate of phase 4 (SDR) of sinus nodes was reduced to its 13.7% when rabbit sinus nodes were exposed to 1×10-7 mol/L (S)-OTS·HCl. (S)-OTS·HCl could inhibit Ca2+channel effectively. It decreased APA and Vmax of sinus nodes and attenuated the cardiac contractility in vitro. Conclusion · (S)-OTS·HCl is a potent cholinergic agonist and has negative chronotropic, dromotropic, and inotropic effects on hearts via binding to M2 muscarinic receptors.

Key words： (S)-OTS·HCl; cholinergic agonist; action potential; electrocardiograph

Options
文章导航

/

〈 〉