Document Detail


Anthraflavic acid is a potent and specific inhibitor of cytochrome P-448 activity.
MedLine Citation:
PMID:  3689794     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Consideration of the computer-optimised dimensions of anthraflavic acid indicates that it is essentially a planar molecule with a large area/depth ratio, that would preferentially interact with the polycyclic aromatic hydrocarbon-induced family of cytochrome P-450 proteins (cytochromes P-448). Anthraflavic acid was a potent inhibitor of the O-deethylations of ethoxycoumarin and ethoxyresorufin, both catalysed primarily by cytochromes P-448, in Arochlor-1254-induced hepatic microsomes. Similarly anthraflavic acid markedly inhibited the mutagenicity of 2-amino-6-methyldipyrido[1,2-a:3',2'-d]imidazole (Glu-P-I) in the Ames test. In contrast, it has no effect on the dealkylation of pentoxyresorufin, a reaction catalysed primarily by the phenobarbital-induced cytochromes P-450, and NADPH-dependent reduction of cytochrome c. It is concluded that anthraflavic acid is a potent and specific inhibitor of cytochrome P-448 activity.
Authors:
A D Ayrton; D F Lewis; C Ioannides; R Walker
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Biochimica et biophysica acta     Volume:  916     ISSN:  0006-3002     ISO Abbreviation:  Biochim. Biophys. Acta     Publication Date:  1987 Dec 
Date Detail:
Created Date:  1988-02-08     Completed Date:  1988-02-08     Revised Date:  2014-01-10    
Medline Journal Info:
Nlm Unique ID:  0217513     Medline TA:  Biochim Biophys Acta     Country:  NETHERLANDS    
Other Details:
Languages:  eng     Pagination:  328-31     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Animals
Anthraquinones / pharmacology*
Computer Simulation
Coumarins / metabolism
Cytochromes / antagonists & inhibitors*
Male
Microsomes, Liver / enzymology
Mixed Function Oxygenases / metabolism
Models, Molecular
NADP / metabolism
Oxazines / metabolism
Rats
Rats, Inbred Strains
Chemical
Reg. No./Substance:
0/Anthraquinones; 0/Coumarins; 0/Cytochromes; 0/Oxazines; 31005-02-4/7-ethoxycoumarin; 53-59-8/NADP; 5725-91-7/ethoxyresorufin; 84-60-6/2,6-dihydroxyanthraquinone; EC 1.-/Mixed Function Oxygenases; EC 1.14.14.1/Cyp1a2 protein, rat

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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