Potential anti-inflammatory actions of the elmiric (lipoamino) acids
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Authors
Burstein, Sumner H.Adams, Jeffrey K.
Bradshaw, Heather B.
Fraioli, Cristian
Rossetti, Ronald G.
Salmonsen, Rebecca
Shaw, John W.
Walker, J. Michael
Zipkin, Robert E.
Zurier, Robert
UMass Chan Affiliations
Department of Medicine, Division of RheumatologyDepartment of Biochemistry and Molecular Pharmacology
Document Type
Journal ArticlePublication Date
2007-03-27Keywords
AlanineAnimals
*Anti-Inflammatory Agents
Cell Line
Cell Proliferation
Chromatography, Thin Layer
Drug Evaluation, Preclinical
Edema
Fatty Acids
Glycine
Indicators and Reagents
Macrophages
Magnetic Resonance Spectroscopy
Male
Mice
Phorbol Esters
Prostaglandin Antagonists
Spectrophotometry, Ultraviolet
Structure-Activity Relationship
Life Sciences
Medicine and Health Sciences
Metadata
Show full item recordAbstract
A library of amino acid-fatty acid conjugates (elmiric acids) was synthesized and evaluated for activity as potential anti-inflammatory agents. The compounds were tested in vitro for their effects on cell proliferation and prostaglandin production, and compared with their effects on in vivo models of inflammation. LPS stimulated RAW 267.4 mouse macrophage cells were the in vitro model and phorbol ester-induced mouse ear edema served as the principal in vivo model. The prostaglandin responses were found to be strongly dependent on the nature of the fatty acid part of the molecule. Polyunsaturated acid conjugates produced a marked increase in media levels of i15-deoxy-PGJ(2) with minimal effects on PGE production. It is reported in the literature that prostaglandin ratios in which the J series predominates over the E series promote the resolution of inflammatory conditions. Several of the elmiric acids tested here produced such favorable ratios suggesting that their potential anti-inflammatory activity occurs via a novel mechanism of action. The ear edema assay results were generally in agreement with the prostaglandin assay findings indicating a connection between them.Source
Bioorg Med Chem. 2007 May 15;15(10):3345-55. Epub 2007 Mar 13. Link to article on publisher's site
DOI
10.1016/j.bmc.2007.03.026Permanent Link to this Item
http://hdl.handle.net/20.500.14038/38377PubMed ID
17383881Related Resources
ae974a485f413a2113503eed53cd6c53
10.1016/j.bmc.2007.03.026