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
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Animals
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Antioxidants / pharmacology*
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Aporphines / pharmacology*
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Brazil
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Cell Line
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Cytochrome P-450 CYP1A1 / antagonists & inhibitors
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Cytochrome P-450 Enzyme System / metabolism
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Glutathione Transferase / metabolism
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In Vitro Techniques
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Mice
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Mice, Inbred C57BL
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Microsomes, Liver / drug effects
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Microsomes, Liver / enzymology
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Mixed Function Oxygenases / metabolism*
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Pharmaceutical Preparations / metabolism*
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Plants, Medicinal / chemistry*
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Tumor Cells, Cultured
Substances
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Antioxidants
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Aporphines
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Pharmaceutical Preparations
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boldine
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Cytochrome P-450 Enzyme System
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Mixed Function Oxygenases
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Cyp2c13 protein, rat
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Cytochrome P-450 CYP1A1
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Glutathione Transferase