Chemoprotective activity of boldine: modulation of drug-metabolizing enzymes.
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.
Department of Natural Drugs, Academy of Sciences, Czech Republic.
R
R
Kubínová
M
M
Machala
K
K
Minksová
J
J
Neca
V
V
Suchý
D000818:Animals; D000975:Antioxidants / Q000494:pharmacology*; D001060:Aporphines / Q000494:pharmacology*; D001938:Brazil; D002460:Cell Line; D019363:Cytochrome P-450 CYP1A1 / Q000037:antagonists & inhibitors; D003577:Cytochrome P-450 Enzyme System / Q000378:metabolism; D005982:Glutathione Transferase / Q000378:metabolism; D066298:In Vitro Techniques; D051379:Mice; D008810:Mice, Inbred C57BL; D008862:Microsomes, Liver / Q000187:drug effects / Q000201:enzymology; D006899:Mixed Function Oxygenases / Q000378:metabolism*; D004364:Pharmaceutical Preparations / Q000378:metabolism*; D010946:Plants, Medicinal / Q000737:chemistry*; D014407:Tumor Cells, Cultured
D000975:Antioxidants; D001060:Aporphines; D004364:Pharmaceutical Preparations; C011686:boldine; D003577:Cytochrome P-450 Enzyme System; D006899:Mixed Function Oxygenases; C113764:Cyp2c13 protein, rat; D019363:Cytochrome P-450 CYP1A1; D005982:Glutathione Transferase