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  • P-ISSN2233-4203
  • E-ISSN2093-8950

Inhibitory Potential of Bilobetin Against CYP2J2 Activities in Human Liver Microsomes

Mass Spectrometry Letters, (P)2233-4203; (E)2093-8950
2020, v.11 no.4, pp.113-117
https://doi.org/10.5478/MSL.2020.11.4.113
Zhexue Wu (Kyungpook National University)
Su-Nyeong Jang (BK21 FOUR Community-Based Intelligent Novel Drug Discovery Education Unit)
So-Young Park (BK21 FOUR Community-Based Intelligent Novel Drug Discovery Education Unit)
Nguyen Minh Phuc (BK21 FOUR Community-Based Intelligent Novel Drug Discovery Education Unit)
Kwang-Hyeon Liu (BK21 FOUR Community-Based Intelligent Novel Drug Discovery Education Unit)

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Abstract

Cytochrome P450 2J2 (CYP2J2) is a member of the cytochrome P450 superfamily, and is known to be arachidonic acid epoxygenase that mediates the formation of four bioactive regioisomers of epoxyeicosatrienoic acids (EETs). CYP2J2 is also involved in the metabolism of drugs such as albendazole, astemizole, danazol, ebastine, and terfenadine. CYP2J2 is highly expressed in the heart and cancer tissues. In this study, the inhibitory potential of ten natural products against CYP2J2 activity was evaluated using human liver microsomes and tandem mass spectrometry. Among them, bilobetin, which is a kind of biflavo-noid, exhibits a strong inhibitory effect against the CYP2J2-mediated astemizole O-demethylation (IC 50 = 0.73 µM) and terfena- dine hydroxylation (IC 50 = 0.89 µM). This result suggests that bilobetin can be used as strong CYP2J2 inhibitor in drug metabolism study.

Submission Date
2020-12-13
Revised Date
2020-12-29
Accepted Date
2020-12-29

Mass Spectrometry Letters