Chinese Journal of Pharmacovigilance ›› 2016, Vol. 13 ›› Issue (12): 705-707.

• Orginal Article •     Next Articles

Inhibitory Effect of Asarone Injection on P450 Enzyme Activities in Vitro

YE Lin-hu1, KONG Ling-ti2, HE Mei1, WANG Yu-qi1, HE Ying-jun1, Chen Cui1   

  1. 1 Department of Pharmacy, First People's Hospital of Bijie, Guizhou Bijie 551700, China;
    2 Department of Pharmacy, First Affiliated Hospital of Bengbu Medical College, Anhui Bengbu 233000, China
  • Received:2017-01-13 Revised:2017-01-13 Online:2016-12-20 Published:2017-01-13

Abstract: objective To evaluate inhibitory effect of asarone injection on the activities of human liver microsomes cytochrome P450 (CYP) enzymes including CYP2D6, CYP3A4, CYP2C19, CYP2E1 and CYP2C9 in vitro for predicting potential metabolic drug interactions.Methods Human liver microsomes and five probes were incubated with different concentrations of asarone injection at 37℃ in presence of NADPH. The concentrations of produced metabolites in the reaction solution were determined by an LC-MS/MS method, and compared for evaluating the activity of isoenzymes. Results The inhibitory effects of asarone injection on the isoenzymes were mainly dependent on the concentrations. The injection inhibited CYP2D6,CYP3A4,CYP2C19,CYP2E1 and CYP2C9 activities with IC50 values of 26.44, 36.16, 52.00, 102.40 and 55.86 μg·mL-1, respectively. Conclusion Asarone injection was found to have inhibitory effect on P450 activities. Extreme caution should be taken regarding the use of this injection to avoid the potential risks of metabolic drug interactions with conventional drugs in the clinic.

Key words: asarone injection, cytochrome P450, inhibitory effect, drug interaction

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