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Nav1.5电生理特性的影响

孙健芳1, 徐艺珈2, 王占友1   

  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 Nav1.5

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

  1. 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: 针对塞来昔布对与心脏毒性密切相关的钠离子通道Nav1.5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Nav1.5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Nav1.5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Nav1.5的激活及失活过程,使其难以恢复到静息状态.塞来昔布对Nav1.5峰电流的明显抑制作用,表明其潜在的心脏风险可能与Nav1.5密切相关.

关键词: 塞来昔布, 心血管风险, 全细胞膜片钳, Nav1.5, 电生理特性

Abstract: The effect of celecoxib on electrophysiological property of Nav1.5 was studied,which was associated with cardiac toxicity. The effects of celecoxib on the electrophysiological properties of Nav 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 Nav1.5 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 Nav1.5, making it somewhat difficult to recover from the inactivation to the resting state. The prominent inhibition of celecoxib on Nav1.5 indicated that there might be a close relationship between potential cardiovascular risks and Nav1.5.

Key words: celecoxib, cardiovascular risk, whole cell patch clamp, Nav1.5, electrophysiological property

中图分类号: