Induction of cytochrome P450 2B6 activity by the herbal medicine baicalin as measured by bupropion hydroxylation

• Published in: European journal of clinical pharmacology Vol. 65; no. 4; pp. 403 - 409
• Main Authors: Fan, Lan, Wang, Jin-Chao, Jiang, Feng, Tan, Zhi-Rong, Chen, Yao, Li, Qing, Zhang, Wei, Wang, Guo, Lei, He-Ping, Hu, Dong-Li, Wang, Dan, Zhou, Hong-Hao
• Format: Journal Article
• Language: English
• Published: Berlin/Heidelberg Berlin/Heidelberg : Springer-Verlag 01.04.2009; Springer-Verlag; Springer; Springer Nature B.V
• Subjects: Adult; Antidepressants; Area Under Curve; Aryl Hydrocarbon Hydroxylases - biosynthesis; Aryl Hydrocarbon Hydroxylases - drug effects; Baicalin; Biological and medical sciences; Biomedical and Life Sciences; Biomedicine; Bupropion; Bupropion - analogs & derivatives; Bupropion - blood; Bupropion - metabolism; Bupropion - pharmacokinetics; CYP2B6; Cytochrome P-450 CYP2B6; Dopamine Uptake Inhibitors - metabolism; Enzyme Induction - drug effects; Flavonoids - chemistry; Flavonoids - pharmacology; Genotype & phenotype; Glucuronidase - antagonists & inhibitors; Haplotypes; Herb-drug interaction; Herb-Drug Interactions; Herbal medicine; Humans; Hydroxybupropoion; Hydroxylation - drug effects; Induction; Male; Medical sciences; Neuropharmacology; Oxidoreductases, N-Demethylating - biosynthesis; Oxidoreductases, N-Demethylating - drug effects; pharmacokinetics; Pharmacokinetics and Disposition; Pharmacology; Pharmacology. Drug treatments; Pharmacology/Toxicology; Plant Extracts - chemistry; Plant Extracts - pharmacology; Polymorphism, Single Nucleotide; Prescription drugs; Time Factors; Bupropion; Herb-drug interaction; Pharmacokinetics; Hydroxybupropoion; Induction; Baicalin; Human; induction; Hero-drug interaction; Hydroxyoupropoion; Hydroxylation; Healthy subject; Enzyme; Pharmacognosy; Isozyme; Psychotropic; Cytochrome P450; Male; Metabolism; Biological activity; Medicinal plant; CYP2B6; Plant origin; Drug interaction; Cytochrome P450 2B6
• ISSN: 0031-6970; 1432-1041
• DOI: 10.1007/s00228-008-0594-3

Purpose This study investigated the effect of the herbal medicine baicalin on bupropion hydroxylation, a probe reaction for CYP2B6 activity related to different CYP2B6 genotype groups. Method Seventeen healthy male volunteers (6 CYP2B6*1/*1, 6 CYP2B6*1/*6, and 5 CYP2B6*6/*6) received orally administered bupropion alone and during daily treatment with baicalin. Blood samples were taken up to 72 h after each bupropion dose, and pharmacokinetics profiles were determined on days 1 and 25 for bupropion and hydroxybupropion. Result Baicalin administration increased hydroxybupropion maximum plasma concentration (C max) by 73% [90% confidence interval (CI), 44-108%; P < 0.01] and the area under the concentration time curve extrapolated to infinity (AUC₀₋[infinity]) of hydroxybupropion by 87% (90% CI, 48-137%; P < 0.01), with no change in the elimination half-life of hydroxybupropion. Baicalin increased the AUC₀₋[infinity] ratio of hydroxybupropion to bupropion by 63% (90% CI, 38-92%; P < 0.01). Conclusion Baicalin significantly induced CYP2B6-catalyzed bupropion hydroxylation, and the effects of baicalin on other CYP2B6 substrate drugs deserve further investigation.