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

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


Journal:
JOURNAL OF HUAZHONG UNIVERSITY OF SCIENCE AND TECHNOLOGY-MEDICAL SCIENCES


Issue Date:
2016


Abstract(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 Na(v)1.5 channels that are stably expressed in HEK 293 cells. We found that neferine potently and reversibly inhibited Na(v)1.5 currents in a concentration dependent manner with a half-maximal inhibition (IC50) being 26.15 mu mol/L. The inhibitory effects of neferine on Na(v)1.5 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 mu mol/L neferine, while the voltage-dependent activation was unaltered. Neferine prolonged the time to peak of activation, increased the inactivation time constants of Na(v)1.5 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 Na(v)1.5 channels under the open state and inactivating state and it is an open channel blocker of Na(v)1.5 channels.


Page:
487---493


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