A proteomic analysis of the mechanism of action of naphthoimidazoles in Trypanosoma cruzi epimastigotes in vitro

J Proteomics. 2010 Nov 10;73(12):2306-15. doi: 10.1016/j.jprot.2010.07.002. Epub 2010 Jul 16.

Abstract

Chagas' disease, caused by the protozoan Trypanosoma cruzi, is endemic in Latin America, which current treatment presents variable efficacy and serious side effects. A previous screening of naphthoquinone derivatives pointed to the naphthoimidazoles N1, N2 and N3 as the most active compounds against T. cruzi. In this study, a proteomic approach was employed to identify proteins involved in the N1, N2 and N3 trypanocidal activity. In epimastigotes, the naphthoimidazoles are involved in multiple mechanisms: (a) redox metabolism; (b) energy production; (c) ergosterol biosynthesis; (d) cytoskeleton assembly; (e) protein metabolism and biosynthesis; and (f) chaperones modulation. They induce an imbalance in crucial pathways of the parasite, leading to the loss of metabolic homeostasis and T. cruzi death.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Chagas Disease / drug therapy*
  • Down-Regulation
  • Imidazoles / therapeutic use*
  • Naphthoquinones / therapeutic use*
  • Protozoan Proteins / biosynthesis
  • Trypanocidal Agents / therapeutic use*
  • Trypanosoma cruzi / drug effects*
  • Trypanosoma cruzi / metabolism

Substances

  • Imidazoles
  • Naphthoquinones
  • Protozoan Proteins
  • Trypanocidal Agents
  • naphthoimidazole N1