Puerarin blocks Na+ current in rat ventricular myocytes

Acta Pharmacol Sin. 2003 Dec;24(12):1212-6.

Abstract

Aim: To study the effect of puerarin (Pue) on Na+ channel in rat ventricular myocytes.

Methods: Whole-cell patch-clamp technique was applied on isolated cardiomyocytes from rats.

Results: Pue inhibited cardiac INa in a positive rate-dependent and dose-dependent manner, with an IC(50) of 349 micromol/L. The kinetics of blockage of cardiac sodium channel by Pue resembled the ClassIa/Ic of antiarrhythmic agents. Pue 300 micromol/L did not alter the shape of the I-V curve of INa, but markedly shifted the steady-state inactivation curve of INa towards more negative potential by 15.9 mV, and postponed the recovery of INa inactivation state from (21.9+/-1.6) ms to (54.4+/-3.4) ms (P<0.01). It demonstrated that the steady state of inactivation was affected by Pue significantly.

Conclusion: Pue protected ventricular myocytes against cardiac damage and arrhythmias by inhibiting recovery from inactivation of cardiac Na+ channels.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Separation
  • Female
  • Heart Ventricles / cytology
  • Isoflavones / pharmacology*
  • Male
  • Myocardium / cytology
  • Myocytes, Cardiac / drug effects*
  • Myocytes, Cardiac / metabolism
  • Rats
  • Rats, Sprague-Dawley
  • Sodium Channel Blockers / pharmacology*
  • Sodium Channels / drug effects*

Substances

  • Isoflavones
  • Sodium Channel Blockers
  • Sodium Channels
  • puerarin