Leptin enhances the efficacy of glucantime to modulate macrophage polarization toward the M1 phenotype in Leishmania tropica-infected macrophages

Parasit Vectors. 2025 Aug 25;18(1):360. doi: 10.1186/s13071-025-07004-6.

Abstract

Background: Macrophages are essential immune cells during Leishmania infection, as their polarization toward M1/M2 phenotypes determines disease outcome. This study aimed to investigate the modulatory effects of leptin, alone and in combination with glucantime, on macrophage polarization in Leishmania tropica infection.

Methods: Human THP-1-derived macrophages infected with L. tropica were treated with leptin (5 or 10 ng/ml), glucantime (100 or 200 μg/ml), or their combinations. The cytotoxic effects, parasite survival, reactive oxygen species (ROS), nitric oxide (NO) generation, and expression of M1/M2 acrophage-related parameters were evaluated using standard methods.

Results: Both leptin doses significantly increased the expression of M1-associated markers (CD86, iNOS, SOCS3, miR-155) and pro-inflammatory cytokines (TNF-α, IL-12, IFN-γ) while decreasing M2-associated markers (CD206, ARG1, SOCS1, miR-146a) and anti-inflammatory cytokines (IL-4, IL-10, TGF-β). The leptin-glucantime combinations showed synergistic effects, shifting macrophage polarization toward the M1 phenotype more than either treatment alone. In particular, the combination of 10 ng/ml leptin with 100 μg/ml glucantime completely eliminated intracellular amastigotes and showed a superior selectivity index (17.66) compared to mono-treatment (leptin: 7.88; glucantime: 6.87).

Conclusions: The findings indicate that leptin enhances the efficacy of glucantime against L. tropica by promoting M1 macrophage polarization. This presents a potential therapeutic approach that may lower conventional drug doses and associated toxicity while preserving or even improving treatment outcomes.

Keywords: Leishmania tropica; Glucantime; Leishmaniasis; Leptin; M1/M2 macrophages; Macrophages.

MeSH terms

  • Antiprotozoal Agents* / pharmacology
  • Cytokines / metabolism
  • Drug Synergism
  • Humans
  • Leishmania tropica* / drug effects
  • Leptin* / pharmacology
  • Macrophages* / drug effects
  • Macrophages* / immunology
  • Macrophages* / parasitology
  • Meglumine Antimoniate* / pharmacology
  • Nitric Oxide / metabolism
  • Phenotype
  • Reactive Oxygen Species / metabolism
  • THP-1 Cells

Substances

  • Meglumine Antimoniate
  • Leptin
  • Cytokines
  • Nitric Oxide
  • Reactive Oxygen Species
  • Antiprotozoal Agents