Files
Document type
ArticleVersion
Published versionPublication date
Publication license
Please use this identifier to cite or link to this item: https://hdl.handle.net/2445/216109
Effect of the aggregated protein dye YAT2150 on Leishmania parasite viability
Journal Title
Director/Tutor
Journal ISSN
Volume Title
Related resource
Abstract
The problems associated with the drugs currently used to treat leishmaniasis, including resistance, toxicity, and the high cost of some formulations, call for the urgent identification of new therapeutic agents with novel modes of action. The aggregated protein dye YAT2150 has been found to be a potent antileishmanial compound, with a half-maximal inhibitory concentration (IC50) of approximately 0.5 µM against promastigote and amastigote stages of Leishmania infantum. The encapsulation in liposomes of YAT2150 significantly improved its in vitro IC50 to 0.37 and 0.19 µM in promastigotes and amastigotes, respectively, and increased the half-maximal cytotoxic concentration in human umbilical vein endothelial cells to >50 µM. YAT2150 became strongly fluorescent when binding intracellular protein deposits in Leishmania cells. This fluorescence pattern aligns with the proposed mode of action of this drug in the malaria parasite Plasmodium falciparum, the inhibition of protein aggregation. In Leishmania major, YAT2150 rapidly reduced ATP levels, suggesting an alternative antileishmanial mechanism. To the best of our knowledge, this first-in-class compound is the only one described so far having significant activity against both Plasmodium and Leishmania, thus being a potential drug for the treatment of co-infections of both parasites.
Subject
Subject (English)
Citation
Citation
MONTEIRO, Juan M., et al. Effect of the aggregated protein dye YAT2150 on Leishmania parasite viability. Antimicrobial Agents and Chemotherapy. 2024. Vol. 68, num. 3, pags. e0112723. ISSN 0066-4804. [consulted: 9 of June of 2026]. Available at: https://hdl.handle.net/2445/216109