Inhibitory potential of bilobetin against cyp2j2 activities in human liver microsomes

Zhexue Wu; Su Nyeong Jang; So Young Park; Nguyen Minh Phuc; Kwang Hyeon Liu

doi:10.5478/MSL.2020.11.4.113

Inhibitory potential of bilobetin against cyp2j2 activities in human liver microsomes

Zhexue Wu
, Su Nyeong Jang
, So Young Park
, Nguyen Minh Phuc
, Kwang Hyeon Liu

Kyungpook National University
Vietnam Hightech of Medicinal and Pharmaceutical JSC

Research output: Contribution to journal › Article › peer-review

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 (IC₅₀ = 0.73 µM) and terfena-dine hydroxylation (IC₅₀ = 0.89 µM). This result suggests that bilobetin can be used as strong CYP2J2 inhibitor in drug metabolism study.

Original language	English
Pages (from-to)	113-117
Number of pages	5
Journal	Mass Spectrometry Letters
Volume	11
Issue number	4
DOIs	https://doi.org/10.5478/MSL.2020.11.4.113
State	Published - 31 Dec 2020

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

Bilobetin
CYP2J2
Human liver microsomes
Liquid chromatography-tandem mass spectrometry
Natural products

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10.5478/MSL.2020.11.4.113

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title = "Inhibitory potential of bilobetin against cyp2j2 activities in human liver microsomes",

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 (IC50 = 0.73 µM) and terfena-dine hydroxylation (IC50 = 0.89 µM). This result suggests that bilobetin can be used as strong CYP2J2 inhibitor in drug metabolism study.",

keywords = "Bilobetin, CYP2J2, Human liver microsomes, Liquid chromatography-tandem mass spectrometry, Natural products",

author = "Zhexue Wu and Jang, \{Su Nyeong\} and Park, \{So Young\} and Phuc, \{Nguyen Minh\} and Liu, \{Kwang Hyeon\}",

year = "2020",

month = dec,

day = "31",

doi = "10.5478/MSL.2020.11.4.113",

language = "English",

volume = "11",

pages = "113--117",

journal = "Mass Spectrometry Letters",

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TY - JOUR

T1 - Inhibitory potential of bilobetin against cyp2j2 activities in human liver microsomes

AU - Wu, Zhexue

AU - Jang, Su Nyeong

AU - Park, So Young

AU - Phuc, Nguyen Minh

AU - Liu, Kwang Hyeon

PY - 2020/12/31

Y1 - 2020/12/31

N2 - 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 (IC50 = 0.73 µM) and terfena-dine hydroxylation (IC50 = 0.89 µM). This result suggests that bilobetin can be used as strong CYP2J2 inhibitor in drug metabolism study.

AB - 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 (IC50 = 0.73 µM) and terfena-dine hydroxylation (IC50 = 0.89 µM). This result suggests that bilobetin can be used as strong CYP2J2 inhibitor in drug metabolism study.

KW - Bilobetin

KW - CYP2J2

KW - Human liver microsomes

KW - Liquid chromatography-tandem mass spectrometry

KW - Natural products

UR - https://www.scopus.com/pages/publications/85101543811

U2 - 10.5478/MSL.2020.11.4.113

DO - 10.5478/MSL.2020.11.4.113

M3 - Article

AN - SCOPUS:85101543811

SN - 2233-4203

VL - 11

SP - 113

EP - 117

JO - Mass Spectrometry Letters

JF - Mass Spectrometry Letters

IS - 4

ER -

Inhibitory potential of bilobetin against cyp2j2 activities in human liver microsomes

Abstract

UN SDGs

Keywords

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