Simultaneous Evaluation of Inhibition on Human CYP450 of Asarum Volatile Oil by a Cocktail Approach

Lei ZHANG, Li-Fang ZHOU, Tong ZHANG, Ai-Hong YANG


In this study, the cocktail method was used to study the inhibitory effect of the volatile oil components including asarinin, methyl eugenol, asarone, safrole and myristicin on the CYP450 enzymes. Five kinds of probe substrates metabolized by different CYP450 enzymes were administered simultaneously in the system of co-incubation of the drug with human liver microsomes. The effect of the drug on the metabolism of the probe substrate was determined by the change of the metabolites of the probe substrate using UPLC/MS, and the inhibition of the enzyme was determined. The results showed that four drugs have an inhibitory effect on the metabolism of CYP450 enzymes except methyl eugenol, and myristicin has the strongest inhibitory effect on CYP1A2.


Cocktail, Asarum volatile oil, CYP450, Probe substrate


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