Dipyridamole potentiated the trypanocidal effect of nifurtimox and improved the cardiac function in NMRI mice with acute chagasic myocarditis

Mem Inst Oswaldo Cruz. 2017 Sep;112(9):596-608. doi: 10.1590/0074-02760160499.

Abstract

Background: As chronic Chagas disease does not have a definitive treatment, the development of alternative therapeutic protocols is a priority. Dipyridamole (DPY) is an alternative to counteract the pathophysiological phenomena involved in Chagas cardiomyopathy.

Objective: To evaluate the therapeutic efficacy of DPY associated with nifurtimox (Nfx) in epimastigote axenic cultures and in mice with acute Chagas disease.

Methods: NMRI adult male mice were divided into nine groups: three healthy and six Trypanosoma cruzi-infected groups. Mice received vehicle, Nfx or DPY, alone or combined. The doses assayed were Nfx 10 and 40 mg/kg and DPY 30 mg/kg. The treatment efficacy was evaluated by clinical, electrocardiographic, parasitological, biochemical and histopathological methods.

Findings: In vitro, DPY and Nfx had a trypanocidal effect with IC50 values of 372 ± 52 and 21.53 ± 2.13 µM, respectively; DPY potentiated the Nfx effect. In vivo, Nfx (40 mg/kg) with or without DPY had a therapeutic effect, which was reflected in the 84-92% survival rate and elimination of parasitaemia and heart tissue amastigotes. Nfx (10 mg/kg) had a subtherapeutic effect with no survival and persistence of amastigotes, inflammation and fibrosis in heart tissue; adding DPY increased the survival rate to 85%, and all tested parameters were significantly improved.

Main conclusion: DPY has a trypanocidal effect in vitro and enhances the Nfx therapeutic effect in an in vivo murine model.

MeSH terms

  • Acute Disease
  • Animals
  • Chagas Cardiomyopathy / drug therapy*
  • Dipyridamole / therapeutic use*
  • Disease Models, Animal
  • Drug Synergism
  • Drug Therapy, Combination
  • Male
  • Mice
  • Nifurtimox / therapeutic use*
  • Trypanocidal Agents / therapeutic use*

Substances

  • Trypanocidal Agents
  • Dipyridamole
  • Nifurtimox