The neuromuscular blockade produced by pure alkaloid, mitragynine and methanol extract of kratom leaves (Mitragyna speciosa Korth.)

J Ethnopharmacol. 2010 Jun 16;129(3):344-9. doi: 10.1016/j.jep.2010.03.035. Epub 2010 Apr 3.

Abstract

Aim of the study: The effects of pure alkaloid, mitragynine and a methanolic extract of kratom leaves were investigated on neuromuscular junction and compound nerve action potential.

Materials and methods: Wistar rats were killed by cervical dislocation and decapitated. The phrenic nerve-hemidiaphragms, hemidiaphragms and sciatic nerve were isolated.

Results: Kratom methanolic extract present at 0.1-1 mg/mL and mitragynine (0.0156 mg/mL) decreased the muscle twitch on the isolated phrenic nerve-hemidiaphragm and hemidiaphragm preparation. Muscle relaxation caused by kratom extract (1 mg/mL) was greater than the effect of mitragynine. Pancuronium and succinylcholine potentiated the effect of kratom extract. It also had a direct relaxation effect on the hemidiaphragm muscle. The muscle relaxation caused by kratom extract was not antagonized by neostigmine, tetraethylammonium and calcium chloride. High concentrations of kratom extract (10-40 mg/mL) and mitragynine (2 mg/mL) blocked the nerve conduction, amplitude and duration of compound nerve action potential.

Conclusions: The mechanism of action of kratom extract might not act as a competitive antagonist of acetylcholine yet its dominant effect was at the neuromuscular junction and not at the skeletal muscle or somatic nerve.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Diaphragm / drug effects
  • Female
  • In Vitro Techniques
  • Male
  • Mitragyna / chemistry*
  • Muscle Relaxation / drug effects*
  • Muscle, Skeletal / drug effects
  • Muscle, Skeletal / innervation
  • Neuromuscular Blockade / methods*
  • Neuromuscular Junction / drug effects*
  • Phrenic Nerve / drug effects
  • Plant Extracts / isolation & purification
  • Plant Extracts / pharmacology*
  • Plant Leaves / chemistry
  • Rats
  • Rats, Wistar
  • Sciatic Nerve / drug effects
  • Secologanin Tryptamine Alkaloids / isolation & purification
  • Secologanin Tryptamine Alkaloids / pharmacology*

Substances

  • Plant Extracts
  • Secologanin Tryptamine Alkaloids
  • mitragynine