Potential of 4′-(p-toluenesulfonylamide)-4-hydroxychalcone to inhibit the human cytochrome P450 2J2 isoform

Boram Lee; Wonku Kang; Jongcheol Shon; Ki Hun Park; Kyung Sik Song; Kwang Hyeon Liu

doi:10.1007/s13765-013-4307-y

Potential of 4′-(p-toluenesulfonylamide)-4-hydroxychalcone to inhibit the human cytochrome P450 2J2 isoform

Boram Lee, Wonku Kang, Jongcheol Shon, Ki Hun Park, Kyung Sik Song, Kwang Hyeon Liu

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

9 Scopus citations

Abstract

Human CYP2J2 isoform, the only member of the human CYP2J subfamily, is also over-expressed in human liver carcinoma tissues and hepatocarcinoma cells, and promotes tumor growth and proliferation. 4′-(p-Toluenesulfonylamide)-4-hydroxychalcone (TSAHC) is a synthetic sulfonylamino chalcone compound, which has anti-cancer effect. Inhibitory potential of a promising anti-cancer agent TSAHC against CYP2J2 activity was evaluated using human liver microsomes. TSAHC inhibited CYP2J2-mediated astemizole O-demethylation activity with K_i value of 2.03±0.40 μM in a competitive mode, suggesting that TSAHC is a potential candidate for further evaluation for its CYP2J2 targeting anti-cancer activities. Studies are presently underway to estimate TSAHC as potential therapeutic agent for cancer.

Original language	English
Pages (from-to)	31-34
Number of pages	4
Journal	Journal of the Korean Society for Applied Biological Chemistry
Volume	57
Issue number	1
DOIs	https://doi.org/10.1007/s13765-013-4307-y
State	Published - Feb 2014

Keywords

CYP2J2
cytotoxicity
drug interactions
human liver microsomes
TSAHC

UN SDGs

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

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10.1007/s13765-013-4307-y

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title = "Potential of 4′-(p-toluenesulfonylamide)-4-hydroxychalcone to inhibit the human cytochrome P450 2J2 isoform",

abstract = "Human CYP2J2 isoform, the only member of the human CYP2J subfamily, is also over-expressed in human liver carcinoma tissues and hepatocarcinoma cells, and promotes tumor growth and proliferation. 4′-(p-Toluenesulfonylamide)-4-hydroxychalcone (TSAHC) is a synthetic sulfonylamino chalcone compound, which has anti-cancer effect. Inhibitory potential of a promising anti-cancer agent TSAHC against CYP2J2 activity was evaluated using human liver microsomes. TSAHC inhibited CYP2J2-mediated astemizole O-demethylation activity with Ki value of 2.03±0.40 μM in a competitive mode, suggesting that TSAHC is a potential candidate for further evaluation for its CYP2J2 targeting anti-cancer activities. Studies are presently underway to estimate TSAHC as potential therapeutic agent for cancer.",

keywords = "CYP2J2, cytotoxicity, drug interactions, human liver microsomes, TSAHC",

author = "Boram Lee and Wonku Kang and Jongcheol Shon and Park, {Ki Hun} and Song, {Kyung Sik} and Liu, {Kwang Hyeon}",

year = "2014",

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doi = "10.1007/s13765-013-4307-y",

language = "English",

volume = "57",

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journal = "Journal of the Korean Society for Applied Biological Chemistry",

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T1 - Potential of 4′-(p-toluenesulfonylamide)-4-hydroxychalcone to inhibit the human cytochrome P450 2J2 isoform

AU - Lee, Boram

AU - Kang, Wonku

AU - Shon, Jongcheol

AU - Park, Ki Hun

AU - Song, Kyung Sik

AU - Liu, Kwang Hyeon

PY - 2014/2

Y1 - 2014/2

N2 - Human CYP2J2 isoform, the only member of the human CYP2J subfamily, is also over-expressed in human liver carcinoma tissues and hepatocarcinoma cells, and promotes tumor growth and proliferation. 4′-(p-Toluenesulfonylamide)-4-hydroxychalcone (TSAHC) is a synthetic sulfonylamino chalcone compound, which has anti-cancer effect. Inhibitory potential of a promising anti-cancer agent TSAHC against CYP2J2 activity was evaluated using human liver microsomes. TSAHC inhibited CYP2J2-mediated astemizole O-demethylation activity with Ki value of 2.03±0.40 μM in a competitive mode, suggesting that TSAHC is a potential candidate for further evaluation for its CYP2J2 targeting anti-cancer activities. Studies are presently underway to estimate TSAHC as potential therapeutic agent for cancer.

AB - Human CYP2J2 isoform, the only member of the human CYP2J subfamily, is also over-expressed in human liver carcinoma tissues and hepatocarcinoma cells, and promotes tumor growth and proliferation. 4′-(p-Toluenesulfonylamide)-4-hydroxychalcone (TSAHC) is a synthetic sulfonylamino chalcone compound, which has anti-cancer effect. Inhibitory potential of a promising anti-cancer agent TSAHC against CYP2J2 activity was evaluated using human liver microsomes. TSAHC inhibited CYP2J2-mediated astemizole O-demethylation activity with Ki value of 2.03±0.40 μM in a competitive mode, suggesting that TSAHC is a potential candidate for further evaluation for its CYP2J2 targeting anti-cancer activities. Studies are presently underway to estimate TSAHC as potential therapeutic agent for cancer.

KW - CYP2J2

KW - cytotoxicity

KW - drug interactions

KW - human liver microsomes

KW - TSAHC

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U2 - 10.1007/s13765-013-4307-y

DO - 10.1007/s13765-013-4307-y

M3 - Article

AN - SCOPUS:84897771092

SN - 1738-2203

VL - 57

SP - 31

EP - 34

JO - Journal of the Korean Society for Applied Biological Chemistry

JF - Journal of the Korean Society for Applied Biological Chemistry

IS - 1

ER -

Potential of 4′-(p-toluenesulfonylamide)-4-hydroxychalcone to inhibit the human cytochrome P450 2J2 isoform

Abstract

Keywords

UN SDGs

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