Chemoprotective activity of boldine: modulation of drug-metabolizing enzymes

Pharmazie. 2001 Mar;56(3):242-3.

Abstract

Possible chemoprotective effects of the naturally occurring alkaloid boldine, a major alkaloid of boldo (Peumus boldus Mol.) leaves and bark, including in vitro modulations of drug-metabolizing enzymes in mouse hepatoma Hepa-1 cell line and mouse hepatic microsomes, were investigated. Boldine manifested inhibition activity on hepatic microsomal CYP1A-dependent 7-ethoxyresorufin O-deethylase and CYP3A-dependent testosterone 6 beta-hydroxylase activities and stimulated glutathione S-transferase activity in Hepa-1 cells. In addition to the known antioxidant activity, boldine could decrease the metabolic activation of other xenobiotics including chemical mutagens.

MeSH terms

  • Animals
  • Antioxidants / pharmacology*
  • Aporphines / pharmacology*
  • Brazil
  • Cell Line
  • Cytochrome P-450 CYP1A1 / antagonists & inhibitors
  • Cytochrome P-450 Enzyme System / metabolism
  • Glutathione Transferase / metabolism
  • In Vitro Techniques
  • Mice
  • Mice, Inbred C57BL
  • Microsomes, Liver / drug effects
  • Microsomes, Liver / enzymology
  • Mixed Function Oxygenases / metabolism*
  • Pharmaceutical Preparations / metabolism*
  • Plants, Medicinal / chemistry*
  • Tumor Cells, Cultured

Substances

  • Antioxidants
  • Aporphines
  • Pharmaceutical Preparations
  • boldine
  • Cytochrome P-450 Enzyme System
  • Mixed Function Oxygenases
  • Cyp2c13 protein, rat
  • Cytochrome P-450 CYP1A1
  • Glutathione Transferase