Abstract
BackgroundCornin is a commonly used herb in cardiology for its cardioprotective effect. The effect of herbs on the activity of cytochrome P450 enzymes (CYP450s) can induce adverse drug-drug interaction even treatment failure. Therefore, it is necessary to investigate the effect of cornin on the activity of CYP450s, which can provide more guidance for the clinical application of cornin.MethodsCornin (100 μM) was incubated with eight isoforms of CYP450s, including CYP1A2, 2A6, 3A4, 2C8, 2C9, 2C19, 2D6, and 2E1, in pooled human liver microsomes. The inhibition model and corresponding parameters were also investigated.ResultsCornin exerted significant inhibitory effect on the activity of CYP3A4, 2C9, and 2E1 in a dose-dependent manner with the IC50 values of 9.20, 22.91, and 14.28 μM, respectively (p < 0.05). Cornin inhibited the activity of CYP3A4 non-competitively with the Ki value of 4.69 μM, while the inhibition of CYP2C9 and 2E1 by cornin was competitive with the Ki value of 11.31 and 6.54 μM, respectively. Additionally, the inhibition of CYP3A4 by cornin was found to be time-dependent with the KI/Kinact value of 6.40/0.055 min− 1·μM− 1.ConclusionsThe inhibitory effect of cornin on the activity of CYP3A4, 2C9, and 2E1 indicated the potential drug-drug interaction between cornin and drugs metabolized by these CYP450s, which needs further investigation and validation.
Highlights
Cornin is a commonly used herb in cardiology for its cardioprotective effect
This study investigated the effects of cornin on the activities of these cytochrome P450 enzymes (CYP450s) isoforms in pooled human liver microsomes (HLMs) with the employment of the enzyme kinetic study that included probe substrates and reactions
Effects of cornin on the activities of CYP450s As shown in Fig. 2a, the activities of CYP3A4, 2C9, and 2E1 were significantly inhibited by cornin compared with the blank control (p < 0.05), while other CYP isoforms were not affected by cornin (p > 0.001)
Summary
Cornin is a commonly used herb in cardiology for its cardioprotective effect. The effect of herbs on the activity of cytochrome P450 enzymes (CYP450s) can induce adverse drug-drug interaction even treatment failure. It is necessary to investigate the effect of cornin on the activity of CYP450s, which can provide more guidance for the clinical application of cornin. Cytochrome P450 enzymes (CYP450s) are a family of Cornin is a herb that is extracted from the fruit of Verbena officinalis L. and is commonly used in cardiology, which can exert cardioprotective effects [4]. It is urgent to investigate the interaction between cornin and CYP450s and determine the effect of cornin on the activities of CYP450s, such studies could provide guidance for improving clinical application of herbs
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