title: Harnessing the anti-inflammatory potential of palmitoylethanolamide.
abstract: Palmitoylethanolamide (PEA) is a peroxisome proliferator-activated receptor alpha (PPAR-α) ligand that exerts anti-inflammatory, analgesic and neuroprotective actions. PEA is synthetized from phospholipids through the sequential actions of N-acyltransferase and N-acylphosphatidylethanolamine-preferring phospholipase D (NAPE-PLD), and its actions are terminated by its hydrolysis by two enzymes, fatty acid amide hydrolase (FAAH) and N-acylethanolamine-hydrolysing acid amidase (NAAA). Here, we review the impact of PEA administration in inflammatory and neurodegenerative settings and the differential role of FAAH and NAAA in controlling PEA levels. Recent studies with NAAA inhibitors put forth this enzyme as capable of increasing PEA levels in vivo in inflammatory processes, and identified it as an interesting target for drug discovery research. Thus, PEA hydrolysis inhibitors could constitute potential therapeutic alternatives in chronic inflammatory and neurodegenerative diseases.
authors: Bioanalysis and Pharmacology of Bioactive Lipids Research Group, Louvain Drug Research Institute, Université catholique de Louvain, Av. E. Mounier 72, B1.72.01, B-1200 Bruxelles, Belgium.
authors: Mireille
authors: M
authors: Alhouayek
authors: Bioanalysis and Pharmacology of Bioactive Lipids Research Group, Louvain Drug Research Institute, Université catholique de Louvain, Av. E. Mounier 72, B1.72.01, B-1200 Bruxelles, Belgium. Electronic address: giulio.muccioli@uclouvain.be.
authors: Giulio G
authors: GG
authors: Muccioli
mesh_terms: D000577:Amides; D000581:Amidohydrolases / Q000378:metabolism; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D004983:Ethanolamines / Q000494:pharmacology*; D006801:Humans; D007249:Inflammation / Q000378:metabolism; D010169:Palmitic Acids / Q000494:pharmacology*; D000099252:Fatty Acid Amide Hydrolases
chemical_list: D000577:Amides; D000581:Amidohydrolases; D000894:Anti-Inflammatory Agents, Non-Steroidal; D004983:Ethanolamines; D010169:Palmitic Acids; D000099252:Fatty Acid Amide Hydrolases; C005958:palmidrol; C523108:NAAA protein, human