| Essential fatty acids are antagonists of the leukotriene B4 receptor. | |
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MedLine Citation:
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PMID: 7630916 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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A series of essential fatty acids and fatty acid derivatives were evaluated for their ability to inhibit [3H] leukotriene B4 (LTB4) binding to pig neutrophil membranes. The fatty acids varied in chain length, extent of unsaturation, position of unsaturation, and isomerization. Generally, fatty acids with two or more unsaturated sites and chain lengths of 18-22 were potent inhibitors of [3H]LTB4 binding; both n-3 and n-6 fatty acids were inhibitory. The most potent compounds tested were homogammalinolenic acid and ricinelaidic acid which gave Ki values of 1 microM and 2 microM in the binding assay. Ricinelaidic acid was also tested for its ability to inhibit LTB4-mediated chemotaxis (IC50 = 10 microM) and LTB4-induced calcium fluxes (IC50 = 7 microM) in isolated human neutrophils. Ricinelaidic acid did not show agonist activity in these assays. In an in vivo model of LTB4-induced bronchoconstriction, ricinelaidic acid and homogammalinolenic acid gave 46% and 53% inhibition, respectively, at a 1 mg/kg i.v. dose. These results indicate that essential fatty acids are LTB4 receptor antagonists, which may account in part for their reported anti-inflammatory activities. |
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Authors:
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K A Yagaloff; L Franco; B Simko; B Burghardt |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Prostaglandins, leukotrienes, and essential fatty acids Volume: 52 ISSN: 0952-3278 ISO Abbreviation: Prostaglandins Leukot. Essent. Fatty Acids Publication Date: 1995 May |
Date Detail:
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Created Date: 1995-09-05 Completed Date: 1995-09-05 Revised Date: 2004-11-17 |
Medline Journal Info:
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Nlm Unique ID: 8802730 Medline TA: Prostaglandins Leukot Essent Fatty Acids Country: SCOTLAND |
Other Details:
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Languages: eng Pagination: 293-7 Citation Subset: IM |
Affiliation:
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Department of Metabolic Disease Research, Hoffmann-La Roche, Nutley, NJ 07110, USA. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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8,11,14-Eicosatrienoic Acid
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pharmacology Animals Bronchoconstriction / drug effects Calcium / metabolism Cell Membrane / metabolism Chemotaxis, Leukocyte / drug effects Fatty Acids, Essential / pharmacology* Fatty Acids, Unsaturated / pharmacology Humans Leukotriene B4 / metabolism, pharmacology Neutrophils / metabolism Receptors, Leukotriene B4 / antagonists & inhibitors* Ricinoleic Acids / pharmacology Swine Tritium |
| Chemical | |
Reg. No./Substance:
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0/Fatty Acids, Essential; 0/Fatty Acids, Unsaturated; 0/Receptors, Leukotriene B4; 0/Ricinoleic Acids; 10028-17-8/Tritium; 141-22-0/ricinoleic acid; 71160-24-2/Leukotriene B4; 7324-41-6/8,11,14-Eicosatrienoic Acid; 7440-70-2/Calcium |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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