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引用本文:王秀秀,邹丽,钱薇,顾有为,李立明,许正新.荭草苷对大鼠心室肌细胞钠通道的影响[J].中国现代应用药学,2019,36(18):2256-2261.
WANG Xiuxiu,ZOU Li,QIAN Wei,GU Youwei,LI Liming,XU Zhengxin.Effects of Orientin on Sodium Channel Currents in Ventricular Myocytes of Rats[J].Chin J Mod Appl Pharm(中国现代应用药学),2019,36(18):2256-2261.
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荭草苷对大鼠心室肌细胞钠通道的影响
王秀秀1, 邹丽1, 钱薇1, 顾有为1, 李立明1, 许正新1,2,3,4
1.扬州大学医学院药理教研室, 江苏 扬州 225000;2.江苏省重点动物传染病和人畜共患病预防控制共创中心, 江苏 扬州 225001;3.江苏省中西医结合老年病防治重点实验室, 江苏 扬州 225001;4.江苏省非编码RNA基础与临床转化重点实验室, 江苏 扬州 225009
摘要:
目的 研究荭草苷(orientin,Ori)对大鼠心室肌细胞钠通道电流(INa)的影响,探讨Ori在离子通道层面的抗心律失常机制。方法 使用Langendorff恒温恒压灌流装置、单酶解消化法分离大鼠心室肌细胞,应用全细胞膜片钳技术记录、观察不同浓度Ori作用前后大鼠心室肌细胞钠通道电流(INa)的变化。结果 低于2 μmol·L-1的Ori对INa无明显影响,3,10,30 μmol·L-1的Ori使INa的I-V曲线显著上移,峰值钠电流(INa-Peak)由给药前的(-81.49±3.9)pA/pF依次变为(-74.38±4.1)pA/pF,(-63.05±2.8)pA/pF和(-55.35±3.2)pA/pF;Ori使激活曲线右移、失活曲线左移,失活后恢复曲线显著右移,最大半数激活电位(V1/2-ac)由给药前的(-53.66±4.12)mV分别变为(-44.64±1.9)mV,(-38.95±1.7)mV和(-30.21±1.5)mV;最大半数失活电位(V1/2-in)由给药前的(-51.68±0.76)mV分别变为(-60.17±1.5)mV,(-68.51±1.4)mV和(-75.22±1.37)mV,恢复时间(τ)由给药前的(18.38±0.84)ms分别变为(24.53±1.4)ms,(35.25±1.3)ms和(68.75±1.58)ms。结论 Ori能浓度依赖性抑制大鼠心室肌细胞的INa,并能显著影响其激活、失活及失活后恢复的动力学特征。
关键词:  荭草苷  全细胞膜片钳  心室肌细胞  钠通道电流  心律失常
DOI:10.13748/j.cnki.issn1007-7693.2019.18.004
分类号:R285.5
基金项目:扬州大学大学生科研创新计划项目(x20180729)
Effects of Orientin on Sodium Channel Currents in Ventricular Myocytes of Rats
WANG Xiuxiu1, ZOU Li1, QIAN Wei1, GU Youwei1, LI Liming1, XU Zhengxin1,2,3,4
1.Department of Pharmacology, School of Medicine, Yangzhou University, Yangzhou 225000, China;2.Jiangsu Key Laboratory of Animal Infectious Diseases and Zoonosis Prevention and Control, Yangzhou 225001, China;3.Key Laboratory of Integrative Medicine Prevention and Treatment in Jiangsu Province, Yangzhou 225001, China;4.Jiangsu Key Laboratory of Non-coding RNA Basic and Clinical Transformation, Yangzhou 225009, China
Abstract:
OBJECTIVE To study the effects of orientin(Ori) on the sodium channel currents(INa) of ventricular myocardial cells in rats, and to explore its anti-arrhythmic mechanisms at the ion channel level. METHODS Ventricular myocardial cells were enzymatically isolated from rats by Langendorff with constant pressure and temperature. The whole-cell patch clamp techniques were used to observe the changes of INa at different concentrations of ori. RESULTS There was no significant effect on INa, when the concentration of Ori was <2 μmol·L-1. I-V curve of INasignificantly moved up under the influence of 3, 10 and 30 μmol·L-1 Ori, and the peak sodium current(INa-Peak)was reduced from (-81.49±3.9)pA/pF to (-74.38±4.1)pA/pF, (-63.05±2.8)pA/pF and (-55.35±3.2)pA/pF. Ori moved the steady-state activation curve of INa to the right, the steady-state inactivation curve to the left, and the recovery curve to the right. The half activation voltage(V1/2-ac)changed from (-53.66±4.12)mV to (-44.64±1.9)mV, (-38.95±1.7)mV and (-30.21±1.5)mV. The half inactivation voltage(V1/2-in)changed from (-51.68±0.76)mV to (-60.17±1.5)mV, (-68.51±1.4)mV and (-75.22±1.37)mV. And the recovery time(τ)changed from (18.38±0.84)ms to (24.53±1.4)ms, (35.25±1.3)ms and (68.75±1.58)ms. CONCLUSION Ori block INa of rat ventricular myocytes in a concentration-dependent manner. It also has a significant effect on the kinetics characteristics of activation, inactivation and the recovery.
Key words:  orientin  whole-cell patch clamp  ventricular myocytes  sodium channel current  arrhythmia
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