Insights into Chagas treatment based on the potential of bacteriocin AS-48

Int J Parasitol Drugs Drug Resist. 2019 Aug:10:1-8. doi: 10.1016/j.ijpddr.2019.03.003. Epub 2019 Mar 29.

Abstract

Chagas disease caused by the protozoan parasite Trypanosoma cruzi represents a significant public health problem in Latin America, affecting around 8 million cases worldwide. Nowadays is urgent the identification of new antichagasic agents as the only therapeutic options available, Nifurtimox and Benznidazole, are in use for >40 years, and present high toxicity, limited efficacy and frequent treatment failures in the chronic phase of the disease. Recently, it has been described the antiparasitic effect of AS-48, a bacteriocin produced by Enterococcus faecalis, against Trypanosoma brucei and Leishmania spp. In this work, we have demonstrated the in vitro potential of the AS-48 bacteriocin against T. cruzi. Interesting, AS-48 was more effective against the three morphological forms of different T. cruzi strains, and displayed lower cytotoxicity than the reference drug Benznidazole. In addition, AS-48 combines the criteria established as a potential antichagasic agent, resulting in a promising therapeutic alternative. According to the action mechanism, AS-48 trypanocidal activity could be explained in a mitochondrion-dependent manner through a reactive oxygen species production and mitochondrial depolarization, causing a fast and severe bioenergetic collapse.

Keywords: AS-48; Antichagasic agent; Bacteriocin; Drug discovery; Trypanosoma cruzi.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Bacteriocins / metabolism
  • Bacteriocins / pharmacology*
  • Chagas Disease / drug therapy
  • Chagas Disease / parasitology*
  • Enterococcus faecalis / chemistry
  • Enterococcus faecalis / metabolism
  • Mitochondria / drug effects
  • Mitochondria / metabolism
  • Nitroimidazoles / pharmacology
  • Reactive Oxygen Species / metabolism
  • Trypanocidal Agents / metabolism
  • Trypanocidal Agents / pharmacology*
  • Trypanosoma cruzi / drug effects*
  • Trypanosoma cruzi / growth & development
  • Trypanosoma cruzi / metabolism

Substances

  • Bacteriocins
  • Nitroimidazoles
  • Reactive Oxygen Species
  • Trypanocidal Agents
  • benzonidazole