Document Detail

Inhibition of human colonic (Na+ + K+)-ATPase by arachidonic and linoleic acid.
MedLine Citation:
PMID:  3016558     Owner:  NLM     Status:  MEDLINE    
The sodium pump, (Na+ + K+)-ATPase, which is involved in the transport of cations and water movement by the colonic mucosa, may be decreased in various diarrhoeal states. In this study, we have measured 3H-ouabain binding and (Na+ + K+)-ATPase activity in human colonic biopsy homogenates and the influence of various inflammatory and antiinflammatory compounds on these parameters. 3H-ouabain binds to one site of high affinity (KD 1.9 +/- 0.2 X 10(-9) mol/l) with a maximal binding capacity of 7.5 +/- 0.8 X 10(14) binding sites/g protein. Both arachidonic and linoleic acid inhibited (Na+ + K+)-ATPase activity (IC50 arachidonic acid: 7.5 X 10(-5) mol/l, linoleic acid: 6.5 X 10(-5) mol/l) and Mg2+-ATPase activity (IC50 arachidonic acid: 9 X 10(-5) mol/l, linoleic acid: 4 X 10(-5) mol/l). Arachidonic acid inhibited 3H-ouabain binding, (IC50 3.2 X 10(-5) mol/l). The following antiinflammatory compounds, at concentrations up to 1 X 10(-3) mol/l, did not influence ATPase activity directly nor reverse the arachidonic acid-induced inhibition: indomethacin (cyclooxygenase inhibitor), nordihydroguaiaretic acid (lipoxygenase inhibitor), sulphasalazine and its metabolites: 5-aminosalicylic acid, N-acetylaminosalicylic acid and sulphapyridine. These results indicate that human colonic (Na+ + K+)-ATPase is inhibited by the prostanoid precursors, arachidonic and linoleic acid. From a therapeutic point of view (effect on colonic (Na+ + K+)-ATPase and perhaps diarrhoea), the suppression of the production of these prostanoid precursors by drugs may, therefore, be beneficial in the treatment of inflammatory bowel disease.
H Allgayer; L Brown; W Kruis; E Erdmann; G Paumgartner
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Publication Detail:
Type:  In Vitro; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Naunyn-Schmiedeberg's archives of pharmacology     Volume:  332     ISSN:  0028-1298     ISO Abbreviation:  Naunyn Schmiedebergs Arch. Pharmacol.     Publication Date:  1986 Apr 
Date Detail:
Created Date:  1986-09-16     Completed Date:  1986-09-16     Revised Date:  2007-11-15    
Medline Journal Info:
Nlm Unique ID:  0326264     Medline TA:  Naunyn Schmiedebergs Arch Pharmacol     Country:  GERMANY, WEST    
Other Details:
Languages:  eng     Pagination:  398-402     Citation Subset:  IM    
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MeSH Terms
Anti-Inflammatory Agents / pharmacology*
Arachidonic Acid
Arachidonic Acids / pharmacology*
Colon, Sigmoid / enzymology,  metabolism
Intestinal Mucosa / enzymology*,  metabolism
Linoleic Acid
Linoleic Acids / pharmacology*
Ouabain / metabolism,  pharmacology
Sodium-Potassium-Exchanging ATPase / antagonists & inhibitors*
Reg. No./Substance:
0/Anti-Inflammatory Agents; 0/Arachidonic Acids; 0/Linoleic Acids; 2197-37-7/Linoleic Acid; 506-32-1/Arachidonic Acid; 630-60-4/Ouabain; EC ATPase

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