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Inhibitory effects of neferine on Nav1.5 channels expressed in HEK293 cells

Journal of Huazhong University of Science and Technology [Medical Sciences] volume 36, pages 487–493 (2016)Cite this article

Summary

Neferine, a bisbenzylisoquinoline alkaloid in Lotus Plumule, was proved to have a wide range of biological activities. In the present study, using whole-cell patch-clamp technique, we investigated the effects of neferine on Nav1.5 channels that are stably expressed in HEK 293 cells. We found that neferine potently and reversibly inhibited Nav1.5 currents in a concentration dependent manner with a half-maximal inhibition (IC50) being 26.15 μmol/L. The inhibitory effects of neferine on Nav1.5 currents were weaker than those of quinidine at the same concentration. The steady-state inactivation curve was significantly shifted towards hyperpolarizing direction in the presence of 30 μmol/L neferine, while the voltage-dependent activation was unaltered. Neferine prolonged the time to peak of activation, increased the inactivation time constants of Nav1.5 currents and markedly slowed the recovery from inactivation. The inhibitory effect of neferine could be potentiated in a frequency-dependent manner. These results suggested that neferine can block Nav1.5 channels under the open state and inactivating state and it is an open channel blocker of Nav1.5 channels.

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Affiliations

  1. Department of Pharmacology, School of Basic Medicine, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430030, China

    Chen Wang, Huan Wang, Jun-hua Xiao, Jia-ling Wang, Ji-zhou Xiang & Qiang Tang

  2. Department of Pharmacology, The Third Affiliated Hospital of Zhengzhou University, Zhengzhou, 450052, China

    Chen Wang

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  1. Chen Wang
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  2. Huan Wang
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  3. Jun-hua Xiao
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  4. Jia-ling Wang
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  5. Ji-zhou Xiang
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  6. Qiang Tang
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Correspondence to Qiang Tang.

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Wang, C., Wang, H., Xiao, Jh. et al. Inhibitory effects of neferine on Nav1.5 channels expressed in HEK293 cells. J. Huazhong Univ. Sci. Technol. [Med. Sci.] 36, 487–493 (2016). https://doi.org/10.1007/s11596-016-1613-8

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  • DOI: https://doi.org/10.1007/s11596-016-1613-8

Keywords

  • neferine
  • Nav1.5 channel
  • whole-cell patch-clamp
  • HEK293 cells