A comprehensive assay for nine major cytochrome P450 enzymes activities with 16 probe reactions on human liver microsomes by a single LC/MS/MS run to support reliablein vitroinhibitory drug–drug interaction evaluation

Xenobiotica ◽  
2015 ◽  
Vol 45 (11) ◽  
pp. 961-977 ◽  
Author(s):  
Ying Peng ◽  
Hui Wu ◽  
Xueyuan Zhang ◽  
Fengyi Zhang ◽  
Huanhuan Qi ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Drug Interaction ◽  
Human Liver ◽  
Liver Microsomes ◽  
Human Liver Microsomes ◽  
Cytochrome P450 Enzymes ◽  
Enzymes Activities ◽  
Drug Drug Interaction

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

2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Qun Zhang ◽  
Zengqiang Qu ◽  
Yanqing Zhou ◽  
Jin Zhou ◽  
Junwei Yang ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Drug Interaction ◽  
Liver Microsomes ◽  
In Vitro Study ◽  
Inhibitory Effect ◽  
Dependent Manner ◽  
Cytochrome P450 Enzymes ◽  
Drug Drug Interaction ◽  
Dose Dependent

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.

Metabolism of (-)-cis- and (-)-trans-rose oxide by cytochrome P450 enzymes in human liver microsomes

2015 ◽  
Vol 36 (9) ◽  
pp. 565-574 ◽  
Author(s):  
Hiroshi Nakahashi ◽  
Yuuki Yamamura ◽  
Atsushi Usami ◽  
Pramoch Rangsunvigit ◽  
Pomthong Malakul ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Human Liver ◽  
Liver Microsomes ◽  
Human Liver Microsomes ◽  
Cytochrome P450 Enzymes ◽  
Cis And Trans

Identification of cytochrome P450 enzymes responsible for metabolism of cannabidiol by human liver microsomes

Life Sciences ◽  
2011 ◽  
Vol 89 (5-6) ◽  
pp. 165-170 ◽  
Author(s):  
Rongrong Jiang ◽  
Satoshi Yamaori ◽  
Shuso Takeda ◽  
Ikuo Yamamoto ◽  
Kazuhito Watanabe
Keyword(s):  
Cytochrome P450 ◽  
Human Liver ◽  
Liver Microsomes ◽  
Human Liver Microsomes ◽  
Cytochrome P450 Enzymes
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