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Potential of decursin to inhibit the human cytochrome P450 2J2 isoform.

Abstract
CYP2J2 enzyme is highly expressed in human tumors and carcinoma cell lines, and epoxyeicosatrienoic acids, CYP2J2-mediated metabolites, have been implicated in the pathologic development of human cancers. To identify a CYP2J2 inhibitor, 50 natural products obtained from plants were screened using astemizole as a CYP2J2 probe substrate in human liver microsomes. Of these, decursin noncompetitively inhibited CYP2J2-mediated astemizole O-demethylation and terfenadine hydroxylation activities with Ki values of 8.34 and 15.8μM, respectively. It also showed cytotoxic effects against human hepatoma HepG2 cells in a dose-dependent manner while it did not show cytotoxicity against mouse hepatocytes. The present data suggest that decursin is a potential candidate for further evaluation for its CYP2J2 targeting anti-cancer activities. Studies are currently underway to test decursin as a potential therapeutic agent for cancer.
AuthorsBoram Lee, Zhexue Wu, Sang Hyun Sung, Taeho Lee, Kyung-Sik Song, Min Young Lee, Kwang-Hyeon Liu
JournalFood and chemical toxicology : an international journal published for the British Industrial Biological Research Association (Food Chem Toxicol) Vol. 70 Pg. 94-9 (Aug 2014) ISSN: 1873-6351 [Electronic] England
PMID24788058 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2014 Elsevier Ltd. All rights reserved.
Chemical References
  • Benzopyrans
  • Biological Products
  • Butyrates
  • CYP2J2 protein, human
  • Cytochrome P-450 Enzyme Inhibitors
  • Isoenzymes
  • Cytochrome P-450 Enzyme System
  • decursin
  • Cytochrome P-450 CYP2J2
Topics
  • Animals
  • Benzopyrans (pharmacology)
  • Biological Products (pharmacology)
  • Butyrates (pharmacology)
  • Cell Survival (drug effects)
  • Chromatography, Liquid
  • Cytochrome P-450 CYP2J2
  • Cytochrome P-450 Enzyme Inhibitors (pharmacology)
  • Cytochrome P-450 Enzyme System (metabolism)
  • Hep G2 Cells
  • Hepatocytes (drug effects, metabolism)
  • Humans
  • Hydroxylation
  • Isoenzymes (metabolism)
  • Male
  • Mice
  • Mice, Inbred ICR
  • Microsomes, Liver (drug effects, enzymology)
  • Tandem Mass Spectrometry

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