塞来昔布对心脏钠离子通道Nav1.5电生理特性的影响

doi:10.12068/j.issn.1005-3026.2019.03.028

东北大学学报:自然科学版 ›› 2019, Vol. 40 ›› Issue (3): 452-456.DOI: 10.12068/j.issn.1005-3026.2019.03.028

• 生物工程 • 上一篇

塞来昔布对心脏钠离子通道Na_v1.5电生理特性的影响

孙健芳¹，徐艺珈²，王占友¹

(1. 东北大学生命科学与健康学院，辽宁沈阳110169; 2. 沈阳药科大学生命科学与生物制药学院，辽宁沈阳110016)

收稿日期:2018-07-15 修回日期:2018-07-15 出版日期:2019-03-15 发布日期:2019-03-08
通讯作者: 孙健芳
作者简介:孙健芳(1988-)，男，辽宁沈阳人，东北大学博士研究生；王占友(1966-)，男，辽宁鞍山人，东北大学教授，博士生导师.
基金资助:
辽宁省教育厅创新团队项目(LT2015010).

Effect of Celecoxib on Electrophysiological Property of Cardiac Sodium Channel Na_v1.5

SUN Jian-fang¹， XU Yi-jia²， WANG Zhan-you¹

1. School of Life and Health Sciences， Northeastern University， Shenyang 110169， China; 2. School of Life Sciences and Biopharmaceutical Science， Shenyang Pharmaceutical University， Shenyang 110016， China.

Received:2018-07-15 Revised:2018-07-15 Online:2019-03-15 Published:2019-03-08
Contact: WANG Zhan-you
About author:-
Supported by:
-

摘要/Abstract

摘要： 针对塞来昔布对与心脏毒性密切相关的钠离子通道Na_v1.5电生理特性的影响进行了研究.采用全细胞膜片钳技术，检测塞来昔布对Na_v1.5的电生理特性的影响，包括电流峰值、电压依赖性激活、电压依赖性失活以及恢复动力学.研究结果表明，塞来昔布对Na_v1.5的峰电流具有抑制作用，且呈浓度依赖性，其抑制作用的IC₅₀值为1.54×10^-8mol/L;塞来昔布促进了Na_v1.5的激活及失活过程，使其难以恢复到静息状态.塞来昔布对Na_v1.5峰电流的明显抑制作用，表明其潜在的心脏风险可能与Na_v1.5密切相关.

关键词: 塞来昔布, 心血管风险, 全细胞膜片钳, Na_v1.5, 电生理特性

Abstract: The effect of celecoxib on electrophysiological property of Na_v1.5 was studied，which was associated with cardiac toxicity. The effects of celecoxib on the electrophysiological properties of Na_v 1.5， including peak current， voltage-dependent activation， voltage-dependent inactivation and recovery kinetics， were investigated by whole cell patch clamp technique. The results showed that celecoxib inhibited the peak currents of Na_v1.5 in a concentration-dependent manner with a calculated IC₅₀ value of 1.54×10^-8mol/L. Moreover， celecoxib promoted the activation and inactivation phase of Na_v1.5， making it somewhat difficult to recover from the inactivation to the resting state. The prominent inhibition of celecoxib on Na_v1.5 indicated that there might be a close relationship between potential cardiovascular risks and Na_v1.5.

Key words: celecoxib, cardiovascular risk, whole cell patch clamp, Na_v1.5, electrophysiological property

中图分类号:

Q513

孙健芳，徐艺珈，王占友. 塞来昔布对心脏钠离子通道Na_v1.5电生理特性的影响[J]. 东北大学学报:自然科学版, 2019, 40(3): 452-456.

SUN Jian-fang， XU Yi-jia， WANG Zhan-you. Effect of Celecoxib on Electrophysiological Property of Cardiac Sodium Channel Na_v1.5[J]. Journal of Northeastern University Natural Science, 2019, 40(3): 452-456.

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塞来昔布对心脏钠离子通道Na_v1.5电生理特性的影响

Effect of Celecoxib on Electrophysiological Property of Cardiac Sodium Channel Na_v1.5

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塞来昔布对心脏钠离子通道Nav1.5电生理特性的影响

Effect of Celecoxib on Electrophysiological Property of Cardiac Sodium Channel Nav1.5

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塞来昔布对心脏钠离子通道Na_v1.5电生理特性的影响

Effect of Celecoxib on Electrophysiological Property of Cardiac Sodium Channel Na_v1.5