| Inhibition of human colonic (Na+ + K+)-ATPase by arachidonic and linoleic acid. | |
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MedLine Citation:
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PMID: 3016558 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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H Allgayer; L Brown; W Kruis; E Erdmann; G Paumgartner |
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Publication Detail:
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Type: In Vitro; Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Naunyn-Schmiedeberg's archives of pharmacology Volume: 332 ISSN: 0028-1298 ISO Abbreviation: Naunyn Schmiedebergs Arch. Pharmacol. Publication Date: 1986 Apr |
Date Detail:
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Created Date: 1986-09-16 Completed Date: 1986-09-16 Revised Date: 2007-11-15 |
Medline Journal Info:
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Nlm Unique ID: 0326264 Medline TA: Naunyn Schmiedebergs Arch Pharmacol Country: GERMANY, WEST |
Other Details:
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Languages: eng Pagination: 398-402 Citation Subset: IM |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Anti-Inflammatory Agents
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pharmacology* Arachidonic Acid Arachidonic Acids / pharmacology* Colon, Sigmoid / enzymology, metabolism Humans Intestinal Mucosa / enzymology*, metabolism Linoleic Acid Linoleic Acids / pharmacology* Ouabain / metabolism, pharmacology Sodium-Potassium-Exchanging ATPase / antagonists & inhibitors* |
| Chemical | |
Reg. No./Substance:
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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 3.6.3.9/Sodium-Potassium-Exchanging ATPase |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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