Eicosapentaenoic acid monoglyceride resolves inflammation in an ex vivo model of human peripheral blood mononuclear cell

Eur J Pharmacol. 2017 Jul 15:807:205-211. doi: 10.1016/j.ejphar.2017.05.018. Epub 2017 May 10.


Phosphorylation and activation of p38 MAPK and NFκB pathways, along with the resulting overproduction of interleukin IL-1β, IL-6, and tumor necrosis factor a (TNFα) is a hallmark of inflammatory disorders. Omega-3 polyunsaturated fatty acid (n-3 PUFA) supplementations are known to exert anti-inflammatory properties by reduction of keys cytokines and enzymes involved in inflammation. Here, we investigated the anti-inflammatory pathways and mediators modulated by eicosapentaenoic acid monoglyceride (MAG-EPA) on human peripheral blood mononuclear cells (PBMCs) from healthy donors and stimulated, ex vivo, with lipopolysaccharide (LPS). LPS stimulation increased p38 MAPK and NFκB phosphorylation, which was abolished by MAG-EPA treatments. Concomitantly, MAG-EPA also abolished LPS-induced inflammation in PBMCs by reducing IL-1β, IL-6, and TNFα cytokines at protein and transcript levels. Moreover, MAG-EPA decreased the levels of HIF1α in LPS-induced human PBMCs. Results also revealed a decreased of pro-inflammatory enzymes such as Cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX) in LPS-induced PBMCs. Altogether, the present data suggest that MAG-EPA, represents a new potential therapeutic strategy for resolving inflammation in inflammatory disorders including autoimmune diseases, allergies, asthma, arthritis and cancer.

Keywords: COX-2; EPA; Human PBMC; Inflammation; NFκB.

MeSH terms

  • Adult
  • Arachidonate 15-Lipoxygenase / metabolism
  • Arachidonate 5-Lipoxygenase / metabolism
  • Biomarkers / metabolism
  • Cell Proliferation / drug effects
  • Cytokines / genetics
  • Cytokines / metabolism
  • Enzyme Activation / drug effects
  • Gene Expression Regulation, Enzymologic / drug effects
  • Humans
  • Hypoxia-Inducible Factor 1, alpha Subunit / genetics
  • Hypoxia-Inducible Factor 1, alpha Subunit / metabolism
  • Inflammation / drug therapy
  • Inflammation / genetics
  • Inflammation / metabolism
  • Inflammation / pathology
  • Leukocytes, Mononuclear / cytology
  • Leukocytes, Mononuclear / drug effects*
  • Leukocytes, Mononuclear / metabolism
  • MAP Kinase Signaling System / drug effects
  • Mitogens / pharmacology
  • Monoglycerides / pharmacology*
  • Monoglycerides / therapeutic use
  • RNA, Messenger / genetics
  • RNA, Messenger / metabolism
  • Young Adult


  • 1-eicosapentaenoylglycerol
  • Biomarkers
  • Cytokines
  • HIF1A protein, human
  • Hypoxia-Inducible Factor 1, alpha Subunit
  • Mitogens
  • Monoglycerides
  • RNA, Messenger
  • Arachidonate 15-Lipoxygenase
  • Arachidonate 5-Lipoxygenase
  • ALOX5 protein, human