Dimethyl fumarate and 4-octyl itaconate are anticoagulants that suppress Tissue Factor in macrophages via inhibition of Type I Interferon

Nat Commun. 2023 Jun 14;14(1):3513. doi: 10.1038/s41467-023-39174-1.

Abstract

Excessive inflammation-associated coagulation is a feature of infectious diseases, occurring in such conditions as bacterial sepsis and COVID-19. It can lead to disseminated intravascular coagulation, one of the leading causes of mortality worldwide. Recently, type I interferon (IFN) signaling has been shown to be required for tissue factor (TF; gene name F3) release from macrophages, a critical initiator of coagulation, providing an important mechanistic link between innate immunity and coagulation. The mechanism of release involves type I IFN-induced caspase-11 which promotes macrophage pyroptosis. Here we find that F3 is a type I IFN-stimulated gene. Furthermore, F3 induction by lipopolysaccharide (LPS) is inhibited by the anti-inflammatory agents dimethyl fumarate (DMF) and 4-octyl itaconate (4-OI). Mechanistically, inhibition of F3 by DMF and 4-OI involves suppression of Ifnb1 expression. Additionally, they block type I IFN- and caspase-11-mediated macrophage pyroptosis, and subsequent TF release. Thereby, DMF and 4-OI inhibit TF-dependent thrombin generation. In vivo, DMF and 4-OI suppress TF-dependent thrombin generation, pulmonary thromboinflammation, and lethality induced by LPS, E. coli, and S. aureus, with 4-OI additionally attenuating inflammation-associated coagulation in a model of SARS-CoV-2 infection. Our results identify the clinically approved drug DMF and the pre-clinical tool compound 4-OI as anticoagulants that inhibit TF-mediated coagulopathy via inhibition of the macrophage type I IFN-TF axis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anticoagulants
  • COVID-19*
  • Caspases
  • Dimethyl Fumarate / pharmacology
  • Dimethyl Fumarate / therapeutic use
  • Escherichia coli
  • Humans
  • Inflammation
  • Interferon Type I*
  • Lipopolysaccharides
  • Macrophages
  • SARS-CoV-2
  • Staphylococcus aureus
  • Thrombin
  • Thromboplastin
  • Thrombosis*

Substances

  • Anticoagulants
  • 4-octyl itaconate
  • Thromboplastin
  • Dimethyl Fumarate
  • Lipopolysaccharides
  • Thrombin
  • Caspases
  • Interferon Type I

Associated data

  • Dryad/10.5061/dryad.6wwpzgn28