Novel n-3 PUFA monoacylglycerides of pharmacological and medicinal interest: Anti-inflammatory and anti-proliferative effects

Eur J Pharmacol. 2016 Dec 5:792:70-77. doi: 10.1016/j.ejphar.2016.10.038. Epub 2016 Nov 3.

Abstract

Newly-synthesized, eicosapentaenoic acid monoacylglyceride (MAG-EPA), docosahexaenoic acid monoacylglyceride (MAG-DHA) and docosapentaenoic acid monoacylglyceride (MAG-DPA) have been demonstrated to display beneficial effects in several disorders including chronic airway inflammatory diseases, pulmonary hypertension, rheumatoid arthritis, and lung and colorectal adenocarcinoma. Recent evidence reveals that omega-3 polyunsaturated fatty acid (n-3 PUFA) precursors provide a window to explore the pathobiology of inflammatory disease as well as structural templates for the design of novel pro-resolving precursors that are well absorbed by the gastrointestinal (GI) tract and metabolized into bioactive metabolites. These metabolites are found in blood circulation and tissues thereby mediating numerous immuno-modulatory effects through the activation of specific receptors. Bioactive metabolites regulate cell membrane functions, lipid signaling and gene expressions encoding for enzymes responsible for lipid storage and fatty acid metabolism. This review highlights recent experimental findings regarding n-3 PUFA monoacylglyceride research, as well as the pharmacological and medicinal relevance of these stereospecific derivatives in the resolution of chronic inflammatory diseases.

Keywords: Asthma; Cancer; Inflammation; PUFA; Pulmonary hypertension; Rheumatoid arthritis.

Publication types

  • Review

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / chemistry*
  • Anti-Inflammatory Agents / pharmacology*
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Cell Proliferation / drug effects
  • Drug Discovery / methods*
  • Fatty Acids, Omega-3 / chemistry*
  • Fatty Acids, Omega-3 / pharmacology*
  • Humans
  • Monoglycerides / chemistry*

Substances

  • Anti-Inflammatory Agents
  • Antineoplastic Agents
  • Fatty Acids, Omega-3
  • Monoglycerides