期刊
CHEMISTRY AND PHYSICS OF LIPIDS
卷 162, 期 1-2, 页码 53-61出版社
ELSEVIER IRELAND LTD
DOI: 10.1016/j.chemphyslip.2009.08.005
关键词
NAPE-PLD; Cannabinoid; Palmitoylethanolamide; Anandamide; Oleoylethanolamide; Diether phospholipid substrate
资金
- Lundbeck Foundation
- Novo Nordisk Foundation
- Danish Medical Research Council
N-Acylethanolamines (NAEs) constitute a family of endogenous bioactive lipids that includes arachidonoylethanolamide (anandamide), palmitoylethanolamide (PEA) and oleoylethanolamide (OEA). These lipids are formed from their respective N-acylated ethanolamine phospholipid (NAPE) precursor by the action of a phospholipase D enzyme (NAPE-PLD). Anandamide, OEA, and PEA are all bioactive lipids that may influence, amongst others: neuroinflammation, food intake, and oocyte implantation. Here we have synthesized a number of NAPE analogues with variation in the phosphoester structure. The NAPE analogues as well as selected phospholipids and beta-lactamase substrates were tested as potential modifiers of cloned human NAPE-PLD in an enzyme assay involving a C-14-labeled diether-NAPE substrate. One hit was identified, namely 1,2-dihexanoyl-glycero-N-(3-(tetradecanoylamino)propyl)phosphoramidate (AHP-71B) which showed inhibitory activity and may serve as template for further structure-activity developments. Furthermore, it was found that NAPE-PLD was activated by phosphatidylethanolamine and inhibited by the beta-lactamase substrate nitrocefin. (C) 2009 Elsevier Ireland Ltd. All rights reserved.
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