Zileuton, a 5-Lypoxigenase Inhibitor, is Antiparasitic and Prevents Inflammation in the Chronic Stage of Heart Chagas Disease

ACS Infect Dis. 2024 Dec 13;10(12):4258-4270. doi: 10.1021/acsinfecdis.4c00623. Epub 2024 Nov 28.

Abstract

Chronic Chagas cardiomyopathy is associated with an unbalanced immune response and impaired heart function, and available drugs do not prevent its development. Zileuton (Zi), a 5-lypoxigenase inhibitor, affects inflammatory/pro-resolution mediators. Herein, Zi treatment in the early phase of infection reduced parasitemia associated mainly with the direct effect of Zi on the parasite, and the enzyme epoxide hydrolase was the potential molecular target behind the trypanocidal effect. In the intermediate acute phase of infection, Zi reduced the number of innate and adaptive inflammatory cells, increased the level of SOCS2 expression in the heart associated with lower inflammation, and improved cardiac function. Zi treatment initiated in the chronic stage increased the level of SOCS2 expression in the heart, reduced inflammation, and improved cardiac function. Our data suggest that Zi protects against Trypanosoma cruzi infection by acting directly on the parasite and reducing heart damage and is a promising option for the treatment of Chagas disease.

Keywords: Chagas disease; cardiomyopathy; epoxide hydrolase; immunoregulation; trypanocidal effect; zileuton.

MeSH terms

  • Animals
  • Antiparasitic Agents / pharmacology
  • Antiparasitic Agents / therapeutic use
  • Chagas Cardiomyopathy* / drug therapy
  • Chronic Disease
  • Hydroxyurea* / analogs & derivatives
  • Hydroxyurea* / pharmacology
  • Hydroxyurea* / therapeutic use
  • Inflammation / drug therapy
  • Male
  • Mice
  • Parasitemia / drug therapy
  • Trypanosoma cruzi* / drug effects

Substances

  • zileuton
  • Hydroxyurea
  • Antiparasitic Agents