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Published in: BMC Complementary Medicine and Therapies 1/2021

Open Access 01-12-2021 | Research

In vitro study on the effect of cornin on the activity of cytochrome P450 enzymes

Authors: Qun Zhang, Zengqiang Qu, Yanqing Zhou, Jin Zhou, Junwei Yang, Shengjian Li, Qiuping Xu, Xuedong Zhou

Published in: BMC Complementary Medicine and Therapies | Issue 1/2021

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Abstract

Background

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. 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.

Methods

Cornin (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.

Results

Cornin 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.

Conclusions

The 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.
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Metadata
Title
In vitro study on the effect of cornin on the activity of cytochrome P450 enzymes
Authors
Qun Zhang
Zengqiang Qu
Yanqing Zhou
Jin Zhou
Junwei Yang
Shengjian Li
Qiuping Xu
Xuedong Zhou
Publication date
01-12-2021
Publisher
BioMed Central
Published in
BMC Complementary Medicine and Therapies / Issue 1/2021
Electronic ISSN: 2662-7671
DOI
https://doi.org/10.1186/s12906-021-03309-y

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