title: In vivo effect of borneol on rat hepatic CYP2B expression and activity.
abstract: CYP2B subfamily accounts for 2-10% of total hepatic CYP450 enzymes and participate in the metabolism of around 8% of clinical drugs. Borneol has been widely used in traditional Chinese medicine for thousands of years. There are many studies about borneol-induced promoting penetration role for a number of drugs through various physiologic barriers, whereas there is no report involved the effect of borneol on hepatic CYP2B. The present work studied the in vivo effect of borneol on the expression and activity of rat hepatic CYP2B. The results indicated that the oral administration of borneol (33, 100 and 300 mg/kg/d) to rats for consecutive 7 days increased the hepatic CYP2B1/2 activity by 1.4-, 1.7- and 2.8-fold, hepatic CYP2B1 mRNA expression by 6.3-, 8.7- and 18.1-fold, and hepatic CYP2B1/2 protein expression by 1.2-, 1.9- and 2.6-fold, respectively compared to the control. Additionally, in the borneol pre-dosing (300 mg/kg/d for consecutive 7 days) rats, the increased Clintand decreased AUC0-24of bupropion were observed as compared to the control. Moreover, there were no obvious effects on CAR protein level in rat liver microsome and nucleus following the borneol treatment. Taken together, our observations indicate that borneol is an in vivo inducer of rat hepatic CYP2B with different regulatory mechanism from phenobarbital-like inducers which caused CYP2B induction with CAR activation.
authors.affiliation: Hubei Province Key Laboratory of Biotechnology of Chinese Traditional Medicine, Hubei Collaborative Innovation Center for Green Transformation of Bio-resources, Hubei University, Wuhan 430062, China.
authors.forename: Jing-Ya
authors.initials: JY
authors.lastname: Chen
authors.affiliation: Hubei Province Key Laboratory of Biotechnology of Chinese Traditional Medicine, Hubei Collaborative Innovation Center for Green Transformation of Bio-resources, Hubei University, Wuhan 430062, China.
authors.forename: Xiang-Tao
authors.initials: XT
authors.lastname: Huang
authors.affiliation: Hubei Province Key Laboratory of Biotechnology of Chinese Traditional Medicine, Hubei Collaborative Innovation Center for Green Transformation of Bio-resources, Hubei University, Wuhan 430062, China.
authors.forename: Jun-Jun
authors.initials: JJ
authors.lastname: Wang
authors.affiliation: Hubei Province Key Laboratory of Biotechnology of Chinese Traditional Medicine, Hubei Collaborative Innovation Center for Green Transformation of Bio-resources, Hubei University, Wuhan 430062, China. Electronic address: cy101610@qq.com.
authors.forename: Yong
authors.initials: Y
authors.lastname: Chen
mesh_terms: D000284:Administration, Oral; D000818:Animals; D016642:Bupropion / Q000031:analogs & derivatives / Q000032:analysis / Q000493:pharmacokinetics; D001892:Camphanes / Q000008:administration & dosage / Q000494:pharmacology*; D002467:Cell Nucleus / Q000187:drug effects / Q000378:metabolism; D000090702:Constitutive Androstane Receptor; D000072467:Cytochrome P450 Family 2 / Q000378:metabolism*; D008099:Liver / Q000187:drug effects / Q000201:enzymology*; D008297:Male; D008862:Microsomes, Liver / Q000187:drug effects / Q000378:metabolism; D021381:Protein Transport / Q000187:drug effects; D017208:Rats, Wistar; D018160:Receptors, Cytoplasmic and Nuclear / Q000378:metabolism; D012044:Regression Analysis; D015203:Reproducibility of Results
chemical_list: D001892:Camphanes; D000090702:Constitutive Androstane Receptor; D018160:Receptors, Cytoplasmic and Nuclear; C580748:hydroxybupropion; D016642:Bupropion; D000072467:Cytochrome P450 Family 2; C022871:isoborneol
keywords: Borneol; CYP2B; Constitutive androstane receptor; Rat liver