A natural cell-penetrating nanopeptide combined with pentavalent antimonial as experimental therapy against cutaneous leishmaniasis

Exp Parasitol. 2020 Oct:217:107934. doi: 10.1016/j.exppara.2020.107934. Epub 2020 Jul 19.

Abstract

The inadequacy of available treatments for leishmaniasis has presented up to 40% therapeutic failure. This fact suggests an urgency in the discovery of new drugs or alternative approaches for treating this disease. The objective of this study was to evaluate the antileishmanial activity of combined therapy between crotamine (CTA) from Crotalus durissus terrificus and the pentavalent antimonial Glucantime® (GLU). The assays were in vitro performed measuring the inhibition of Leishmania amazonensis amastigotes, followed by the evaluation of cellular production of cytokines and nitrites. After that, analytical methods were performed in order to characterize the molecules involved in the study by Mass Spectrometry, molecular affinity through an in silico assay and Surface Plasmon Resonance. In vivo experiments with BALB/c mice were performed by analyzing parasitemia, lesion size and immunological mediators. In the in vitro experiments, the pharmacological association improved the inhibition of the amastigotes, modulated the production of cytokines and nitric oxide. The therapy improved the effectiveness of the GLU, demonstrating a decreased parasitemia in the infected tissues. Altogether, the results suggest that the combined approach with CTA and GLU may be a promising alternative for the treatment of cutaneous leishmaniasis.

Keywords: Combined therapy; Crotamine; Cutaneous leishmaniasis; Pentavalent antimonial.

MeSH terms

  • Animals
  • Antiprotozoal Agents / pharmacology
  • Antiprotozoal Agents / therapeutic use*
  • Crotalid Venoms / pharmacology
  • Crotalid Venoms / therapeutic use*
  • Crotalus*
  • Drug Combinations
  • Interleukin-12 / blood
  • Interleukin-12 / metabolism
  • Leishmania mexicana / drug effects*
  • Leishmania mexicana / isolation & purification
  • Leishmaniasis, Cutaneous / drug therapy*
  • Lymph Nodes / parasitology
  • Macrophages, Peritoneal
  • Mass Spectrometry
  • Meglumine Antimoniate / pharmacology
  • Meglumine Antimoniate / therapeutic use*
  • Mice
  • Mice, Inbred BALB C
  • Molecular Docking Simulation
  • Nitric Oxide / metabolism
  • Nitrites / analysis
  • Tumor Necrosis Factor-alpha / blood
  • Tumor Necrosis Factor-alpha / metabolism

Substances

  • Antiprotozoal Agents
  • Crotalid Venoms
  • Drug Combinations
  • Nitrites
  • Tumor Necrosis Factor-alpha
  • Interleukin-12
  • Nitric Oxide
  • Meglumine Antimoniate
  • crotamine