Effect of natural borneol on the activities of cytochrome p450 isoforms in rats

Abstract

Abstract: AIM: To study the effect of natural borneol on the activities of cytochrome P450 enzymes CYP1A2, CYP2C6/11, CYP2E1 and CYP3A by a cocktail approach in rats. METHODS: The rats were randomly divided into two groups.One group of rats were treated with natural borneol suspension containing 0.8% CMC-Na (90 mg/kg) by intragastric injection once a day for 7 days.At the same time, the rats in the other group received 0.8% CMC-Na solution serving as control group.On the 8th day, all rats in each group were intravenously injected with cocktail probe drugs (10 mg/kg theophylline, 2.5 mg/kg tolbutamide, 10 mg/kg chlorzoxazone, 5 mg/kg dapsone).Blood samples were drawn into heparinized tubes at different time points.The plasma concentration of probe drugs were determined by ultra performance liquid chromatography (UPLC) and the main pharmacokinetic parameters were calculated by WinNonlin 5.0.1. RESULTS: In natural borneol group, the t_1/2, AUC_0-t, AUC_0-∞ and MRT_0-∞ of tolbutamide were significantly lower than those in Control group (P<0.05). There were no significant differences in the pharmacokinetic parameters of theophylline, chlorzoxazone and dapsone between control group and natural borneol group.CONCLUSION: Natural borneol can induce the activity of CYP2C6/11, but has no influence on the activities of CYP1A2, CYP2E1 and CYP3A.

Key words: Natural borneol, Cytochrome P450, Probe cocktail

CLC Number:

R969.1

WU Chun, GAO Jing-wen, YAO Mei-cun, HOU Xue-ying, ZHOU Yu-ting, DENG Xue-jiao, LIAO Qiong-feng, XIE Zhi-yong. Effect of natural borneol on the activities of cytochrome p450 isoforms in rats[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2013, 18(2): 121-127.

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