Omega-3-carboxylic acids provide efficacious anti-inflammatory activity in models of crystal-mediated inflammation

Sci Rep. 2018 Jan 19;8(1):1217. doi: 10.1038/s41598-018-19252-x.

Abstract

This study assesses the efficacy and exposure-response relationship of omega-3-carboxylic acids (OM-3 CA) in models of crystal-based inflammation. Human THP-1 macrophages and primary peripheral blood mononuclear cells exposed to multiple inflammatory crystal types were used to determine the anti-inflammatory potential of omega-3 (OM-3) fatty acids in vitro. Anti-inflammatory effects of OM-3 CA in vivo were tested in rat monosodium urate (MSU) crystal air pouch and rat knee intra-articular MSU injection models. Acute treatment with the OM-3 fatty acid docosahexaenoic acid suppressed MSU-, cholesterol crystal-, and calcium pyrophosphate crystal-mediated interleukin-1β (IL-1β) production in vitro. In vivo, OM-3 CA dose-dependently reduced crystal-mediated cell migration, exudate volume, and levels of IL-1β and prostaglandin E2. Following intra-articular injection of MSU, treatment with OM-3-CA (1 mL/kg) and indomethacin (1 mg/kg) resulted in similar mean reductions in pain (23% and 41%, respectively) and swelling (58% and 50%, respectively), compared with controls. Additionally, in complex formulations of OM-3 fatty acids, high levels of palmitic acid could reduce the in vivo effect on crystal-mediated IL-1β elevation. OM-3 CA has a broadly efficacious anti-inflammatory effect with a strong exposure-response relationship that could be beneficial in prevention and treatment of crystal arthritis, with potential applications in other IL-1β-mediated diseases.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / chemistry
  • Anti-Inflammatory Agents / pharmacology*
  • Arthritis, Gouty / drug therapy
  • Arthritis, Gouty / etiology*
  • Arthritis, Gouty / metabolism*
  • Arthritis, Gouty / pathology
  • Carboxylic Acids / chemistry
  • Carboxylic Acids / pharmacology*
  • Cell Movement / drug effects
  • Cytokines / metabolism
  • Dinoprostone / biosynthesis
  • Disease Models, Animal
  • Disease Progression
  • Exudates and Transudates / metabolism
  • Fatty Acids, Omega-3* / chemistry
  • Fatty Acids, Omega-3* / metabolism
  • Humans
  • Inflammation Mediators / metabolism
  • Interleukin-1beta / metabolism
  • Leukocytes / drug effects
  • Leukocytes / metabolism
  • Leukocytes / pathology
  • Macrophages / drug effects
  • Macrophages / metabolism
  • Macrophages / pathology
  • Palmitic Acid / pharmacology
  • Rats

Substances

  • Anti-Inflammatory Agents
  • Carboxylic Acids
  • Cytokines
  • Fatty Acids, Omega-3
  • Inflammation Mediators
  • Interleukin-1beta
  • Palmitic Acid
  • Dinoprostone