Epeleuton, a novel synthetic ω-3 fatty acid, reduces hypoxia/ reperfusion stress in a mouse model of sickle cell disease

Haematologica. 2024 Jun 1;109(6):1918-1932. doi: 10.3324/haematol.2023.284028.

Abstract

Inflammatory vasculopathy is critical in sickle cell disease (SCD)-associated organ damage. An imbalance between pro-inflammatory and pro-resolving mechanisms in response to different triggers such as hypoxia/reoxygenation or infections has been proposed to contribute to the progression of SCD. Administration of specialized pro-resolving lipid mediators may provide an effective therapeutic strategy to target inflammatory vasculopathy and to modulate inflammatory response. Epeleuton (15 hydroxy eicosapentaenoic acid ethyl ester) is a novel, orally administered, second-generation ω-3 fatty acid with a favorable clinical safety profile. In this study we show that epeleuton re-programs the lipidomic pattern of target organs for SCD towards a pro-resolving pattern. This protects against systemic and local inflammatory responses and improves red cell features, resulting in reduced hemolysis and sickling compared with that in vehicle-treated SCD mice. In addition, epeleuton prevents hypoxia/reoxygenation-induced activation of nuclear factor-κB with downregulation of the NLRP3 inflammasome in lung, kidney, and liver. This was associated with downregulation of markers of vascular activation in epeleuton-treated SCD mice when compared to vehicle-treated animals. Collectively our data support the potential therapeutic utility of epeleuton and provide the rationale for the design of clinical trials to evaluate the efficacy of epeleuton in patients with SCD.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anemia, Sickle Cell* / complications
  • Anemia, Sickle Cell* / drug therapy
  • Anemia, Sickle Cell* / metabolism
  • Anemia, Sickle Cell* / pathology
  • Animals
  • Disease Models, Animal*
  • Eicosapentaenoic Acid / analogs & derivatives
  • Eicosapentaenoic Acid / pharmacology
  • Fatty Acids, Omega-3 / pharmacology
  • Humans
  • Hypoxia / drug therapy
  • Hypoxia / metabolism
  • Male
  • Mice
  • Reperfusion Injury* / drug therapy
  • Reperfusion Injury* / metabolism
  • Reperfusion Injury* / pathology

Substances

  • Eicosapentaenoic Acid
  • eicosapentaenoic acid ethyl ester
  • Fatty Acids, Omega-3

Grants and funding

Funding: This study was supported by Afimmune Ltd. under a research collaborative grant to LDF.