Characterization of the metabolic contributions of cytochrome P450 isoforms to bicyclol using the relative activity factor method

Bicyclol is a hepatoprotective agent widely used for treating chronic hepatitis and drug-induced liver injuries in clinics. The purpose of the study was to elucidate the contribution of CYP450 enzymes to the metabolism of bicyclol using the relative activity factor approach. After incubation with hu...

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Bibliographic Details
Published in:Journal of asian natural products research 2024-08, Vol.26 (8), p.918-929
Main Authors: Luo, Li-jun, Liu, Xiao, Li, Yan, Li, Yang, Sheng, Li
Format: Article
Language:English
Subjects:
Cytochrome P450
Cytochromes P450
Drug interaction
Drug metabolism
drug-drug interaction
drug-metabolizing enzyme
enzyme contribution
Enzymes
Hepatitis
Hepatoprotectant
Isoforms
Liver
Microsomes
relative activity factor
Toxicity
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Summary:Bicyclol is a hepatoprotective agent widely used for treating chronic hepatitis and drug-induced liver injuries in clinics. The purpose of the study was to elucidate the contribution of CYP450 enzymes to the metabolism of bicyclol using the relative activity factor approach. After incubation with human liver microsomes and recombinant human liver CYP450 enzymes, the calculated contribution of CYP3A4 and 2C19 to the metabolism of bicyclol was 85.6-90.3% and 9.2-9.7%, respectively. The metabolism was interrupted in the presence of CYP3A4 and 2C19 selective inhibitors. These findings help to predict or avoid metabolic drug-drug interactions or toxicity in clinical applications of bicyclol.
ISSN:1028-6020
1477-2213
1477-2213
DOI:10.1080/10286020.2024.2340072