Document Detail


Uptake, production and metabolism of cysteinyl leukotrienes in the isolated perfused rat liver. Inhibition of leukotriene uptake by cyclosporine.
MedLine Citation:
PMID:  2549977     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
1. The isolated perfused rat liver efficiently takes up cysteinyl leukotrienes (LTs) C4, D4, E4 and N-acetyl-LTE4 from circulation. More than 70% of these cysteinyl LTs are excreted from liver into bile within 1 h of onset of a 5 min infusion, while about 5% remain in the liver. About 20% of infused N-acetyl-LTE4 escapes hepatic first-pass extraction under our conditions. 2. Metabolites of LTC4 appearing in bile within 20 min of the onset of infusion include mainly LTD4 and N-acetyl-LTE4, but also omega-hydroxy-N-acetyl-LTE4 and omega-carboxy-N-acetyl-LTE4. Metabolites generated from omega-carboxy-N-acetyl-LTE4 by beta-oxidation from the omega-end represent the major biliary LTs secreted at later times. 3. Stimulation of the isolated perfused liver by the combined infusion of the phorbol ester 12-O-tetradecanoylphorbol-13-acetate (TPA) and the Ca2+ ionophore A23187 results in a transient increase of endogenous cysteinyl LT production, which is independent of extrahepatic cells. 4. The immunosuppressive drug cyclosporine causes a dose-dependent inhibition of hepatobiliary cysteinyl LT excretion, probably by interference with the sinusoidal uptake system for cysteinyl LTs.
Authors:
W Hagmann; S Parthé; I Kaiser
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  The Biochemical journal     Volume:  261     ISSN:  0264-6021     ISO Abbreviation:  Biochem. J.     Publication Date:  1989 Jul 
Date Detail:
Created Date:  1989-10-12     Completed Date:  1989-10-12     Revised Date:  2009-11-18    
Medline Journal Info:
Nlm Unique ID:  2984726R     Medline TA:  Biochem J     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  611-6     Citation Subset:  IM    
Affiliation:
Deutsches Krebsforschungszentrum, Heidelberg, Federal Republic of Germany.
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MeSH Terms
Descriptor/Qualifier:
Animals
Cyclosporins / pharmacology*
Leukotriene E4
Liver / drug effects,  metabolism*
Male
Perfusion
Rats
Rats, Inbred Strains
SRS-A / analogs & derivatives,  biosynthesis,  metabolism*
Chemical
Reg. No./Substance:
0/Cyclosporins; 0/SRS-A; 75715-89-8/Leukotriene E4; 80115-95-3/N-acetylleukotriene E4
Comments/Corrections

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