Crebanine inhibits voltage-dependent Na+ current in guinea-pig ventricular myocytes

Chin J Nat Med. 2014 Jan;12(1):20-3. doi: 10.1016/S1875-5364(14)60004-2.

Abstract

Aim: To study the effects of crebanine on voltage-gated Na(+) channels in cardiac tissues.

Methods: Single ventricular myocytes were enzymatically dissociated from adult guinea-pig heart. Voltage-dependent Na(+) current was recorded using the whole cell voltage-clamp technique.

Results: Crebanine reversibly inhibited Na(+) current with an IC50 value of 0.283 mmol·L(-1) (95% confidence range: 0.248-0.318 mmol·L(-1)). Crebanine at 0.262 mmol·L(-1) caused a negative shift (about 12 mV) in the voltage-dependence of steady-state inactivation of Na(+) current, and retarded its recovery from inactivation, but did not affect its activation curve.

Conclusion: In addition to blocking other voltage-gated ion channels, crebanine blocked Na(+) channels in guinea-pig ventricular myocytes. Crebanine acted as an inactivation stabilizer of Na(+) channels in cardiac tissues.

Keywords: Arrhythmia; Crebanine; Myocardium; Patch-clamp techniques; R285; Sodium channels.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Aporphines / pharmacology*
  • Cells, Cultured
  • Down-Regulation / drug effects
  • Drugs, Chinese Herbal / pharmacology*
  • Female
  • Guinea Pigs
  • Heart Ventricles / cytology
  • Heart Ventricles / drug effects*
  • Heart Ventricles / metabolism
  • Male
  • Myocytes, Cardiac / drug effects*
  • Myocytes, Cardiac / metabolism
  • Stephania / chemistry
  • Voltage-Gated Sodium Channel Blockers / pharmacology*
  • Voltage-Gated Sodium Channels / metabolism*

Substances

  • Aporphines
  • Drugs, Chinese Herbal
  • Voltage-Gated Sodium Channel Blockers
  • Voltage-Gated Sodium Channels
  • crebanine