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Selective inhibitory effects of mollugin on CYP1A2 in human liver microsomes.

Abstract
Mollugin originally isolated from Rubia cordifolia is a pharmacological compound for its anti-inflammation, anti-cancer, and anti-viral activity. In the present study, a cocktail probe assay was performed for determination of the selective inhibitory effect of mollugin on cytochrome P450 (CYP) enzymes in human liver microsomes (HLM). Incubation of isoform-specific substrate probes CYPs with mollugin (0-25μM) in HLM resulted in strong inhibition of CYP1A2-catalyzed phenacetin O-deethylation, showing IC(50) values of 1.03 and 3.55μM without and with pre-incubation, respectively. Mollugin-caused inhibition of phenacetin O-deethylation was concentration-dependent in HLMs, but not time-dependent. In addition, the Lineweaver-Burk plot indicated a typical competitive inhibition. Inhibitory effects of mollugin on human recombinant cDNA-expressed CYP1A1 and 1A2 were comparable. Taken together, the results suggested that mollugin might cause herb-drug interaction through selective inhibition of CYP1A2 in humans receiving herbal medications, including R. cordifolia.
AuthorsHeeyeon Kim, Hyun Kyu Choi, Tae Cheon Jeong, Yurngdong Jahng, Dong Hyun Kim, Seung-Ho Lee, Sangkyu Lee
JournalFood and chemical toxicology : an international journal published for the British Industrial Biological Research Association (Food Chem Toxicol) Vol. 51 Pg. 33-7 (Jan 2013) ISSN: 1873-6351 [Electronic] England
PMID23000442 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2012 Elsevier Ltd. All rights reserved.
Chemical References
  • Cytochrome P-450 CYP1A2 Inhibitors
  • Drugs, Chinese Herbal
  • Enzyme Inhibitors
  • Pyrans
  • Recombinant Proteins
  • rubimaillin
  • CYP1A1 protein, human
  • CYP1A2 protein, human
  • Cytochrome P-450 CYP1A1
  • Cytochrome P-450 CYP1A2
Topics
  • Cytochrome P-450 CYP1A1 (genetics, metabolism)
  • Cytochrome P-450 CYP1A2 (genetics, metabolism)
  • Cytochrome P-450 CYP1A2 Inhibitors
  • Drugs, Chinese Herbal (pharmacology)
  • Enzyme Inhibitors (pharmacology)
  • Herb-Drug Interactions
  • Humans
  • Inhibitory Concentration 50
  • Microsomes, Liver (drug effects, enzymology)
  • Pyrans (pharmacology)
  • Recombinant Proteins (genetics, metabolism)

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