Cytotoxic effect and electrophysiological activity of (S)-bgugaine, an alkylpyrrolidine alkaloid against MRC-5 fibroblasts

Phytomedicine. 2000 Apr;7(2):145-9. doi: 10.1016/S0944-7113(00)80087-2.

Abstract

(+)-S-bgugaine [1], is an alkaloid prepared by enantioselective synthesis. This alkaloid is an isomer of R-bgugaine [2], an alkaloid isolated from Arisarum vulgare, an Araceae toxic plant of Morocco. The cytotoxic effect and the electrophysiological activity of (+)-S-bgugaine [1] against MRC-5 fibroblasts of (+)-S-bgugaine 1, were studied. (+)-S-bgugaine [1] showed a cytotoxic potential at 40 microg/ml against these MRC-5 cells. The electrophysiological study on MRC-5 cells was carried out using the technique of patch-clamp and showed that the activity of compound 1 involved a reduction of outward potassic current at the concentration of 100 microM (28.1 microg/ml) and was accentuated by 200 microM (56.2 microg/ml). In this study we show that S-bgugaine [1], decreases the outward potassic current.

MeSH terms

  • Alkaloids / chemistry
  • Alkaloids / pharmacology*
  • Alkaloids / toxicity
  • Cell Line
  • Cell Survival / drug effects*
  • Fibroblasts / cytology
  • Fibroblasts / drug effects
  • Fibroblasts / physiology
  • Humans
  • Lung
  • Membrane Potentials / drug effects*
  • Molecular Conformation
  • Patch-Clamp Techniques
  • Pyrrolidines / chemistry
  • Pyrrolidines / pharmacology*
  • Pyrrolidines / toxicity
  • Stereoisomerism

Substances

  • Alkaloids
  • Pyrrolidines
  • bgugaine