Selective inhibitory effects of mollugin on CYP1A2 in human liver microsomes

Title
Selective inhibitory effects of mollugin on CYP1A2 in human liver microsomes
Author(s)
정태천김희연[김희연]최현규장영동김동현[김동현]이승호이상규[이상규]
Keywords
RUBIA-CORDIFOLIA; IN-VITRO; EXTRACT; CONSTITUENTS
Issue Date
201301
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Citation
FOOD AND CHEMICAL TOXICOLOGY, v.51, pp.33 - 37
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 (0-25 mu M) in HLM resulted in strong inhibition of CYP1A2-catalyzed phenacetin O-deethylation, showing IC50 values of 1.03 and 3.55 mu M 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. (C) 2012 Elsevier Ltd. All rights reserved.
URI
http://hdl.handle.net/YU.REPOSITORY/26869http://dx.doi.org/10.1016/j.fct.2012.09.013
ISSN
0278-6915
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약학대학 > 약학부 > Articles
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