SARS-CoV2-mediated suppression of NRF2-signaling reveals potent antiviral and anti-inflammatory activity of 4-octyl-itaconate and dimethyl fumarate

Nat Commun. 2020 Oct 2;11(1):4938. doi: 10.1038/s41467-020-18764-3.

Abstract

Antiviral strategies to inhibit Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV2) and the pathogenic consequences of COVID-19 are urgently required. Here, we demonstrate that the NRF2 antioxidant gene expression pathway is suppressed in biopsies obtained from COVID-19 patients. Further, we uncover that NRF2 agonists 4-octyl-itaconate (4-OI) and the clinically approved dimethyl fumarate (DMF) induce a cellular antiviral program that potently inhibits replication of SARS-CoV2 across cell lines. The inhibitory effect of 4-OI and DMF extends to the replication of several other pathogenic viruses including Herpes Simplex Virus-1 and-2, Vaccinia virus, and Zika virus through a type I interferon (IFN)-independent mechanism. In addition, 4-OI and DMF limit host inflammatory responses to SARS-CoV2 infection associated with airway COVID-19 pathology. In conclusion, NRF2 agonists 4-OI and DMF induce a distinct IFN-independent antiviral program that is broadly effective in limiting virus replication and in suppressing the pro-inflammatory responses of human pathogenic viruses, including SARS-CoV2.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Anti-Inflammatory Agents / pharmacology*
  • Antioxidants / pharmacology
  • Antiviral Agents / pharmacology*
  • Betacoronavirus / drug effects*
  • Betacoronavirus / metabolism
  • COVID-19
  • Coronavirus Infections / drug therapy*
  • Coronavirus Infections / virology
  • Dimethyl Fumarate / agonists*
  • Dimethyl Fumarate / pharmacology
  • Female
  • Gene Expression
  • Gene Knockdown Techniques
  • Humans
  • Interferon Type I
  • Lung / pathology
  • Male
  • NF-E2-Related Factor 2 / genetics
  • NF-E2-Related Factor 2 / metabolism*
  • Pandemics
  • Pneumonia, Viral / drug therapy*
  • Pneumonia, Viral / virology
  • SARS-CoV-2
  • Signal Transduction / drug effects
  • Succinates / agonists*
  • Succinates / pharmacology
  • Virus Replication / drug effects

Substances

  • 4-octyl itaconate
  • Anti-Inflammatory Agents
  • Antioxidants
  • Antiviral Agents
  • Interferon Type I
  • NF-E2-Related Factor 2
  • Succinates
  • Dimethyl Fumarate