Authors
Soumia Ftouh, Sandra Bourgeade-Delmas, Chloé Salis, Jean-Luc Stigliani, Clara Litot, Théo Villarubias, Anne-Dominique Terrisse, Jade Royo, Zhengcheng Liang, Nicolas Fabre, Marieke Vansteelandt, Xavier Iriart, Maëlle Carraz, Céline Deraeve, Catherine Hemmert, Karine Reybier, Alexis Valentin, Heinz Gornitzka
Published in
Chemistry (Weinheim an der Bergstrasse, Germany). Pages e71382. Jul 10, 2026. Epub Jul 10, 2026.
Abstract
A family of neutral gold(I) complexes involving N-heterocyclic carbene ligands bearing fluoro-aryl groups has been synthesized and characterized in order to evaluate its antileishmanial activity in vitro for all complexes and in vivo for the hit 34. Computational docking experiments on the potential target trypanothione reductase were performed for all complexes. Regarding complex 34, trypanothione reductase inhibition, ROS formation, as well as the impact on target genes by RT-qPCR have been addressed. Complex 34 showed almost identical activity in vitro, combined with higher selectivity than amphotericin B, the most effective drug currently used against leishmaniasis in clinical use. The high activity of this complex has been confirmed by in vivo experiments. Mechanistical studies reveal that gold complex 34 rapidly alters the expression of key genes involved in Leishmania infantum's redox homeostasis and mitochondrial function after treatment. The significant upregulation of genes in the trypanothione system suggests an early adaptive response to oxidative stress induced by this complex.
PMID:
42430206
Bibliographic data and abstract were imported from PubMed on 10 Jul 2026.
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