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Earlier evidences showed that diglycosyl diselenides are active against the infective stage of African trypanosomes (top hits IC50 0.5 and 1.5 μM) but poorly selective (selectivity index <10). Here we extended the study to 33 new seleno-glycoconjugates with the aim to improve potency and selectivity. Three selenoglycosides and three glycosyl selenenylsulfides displayed IC50 against bloodstream Trypanosoma brucei in the sub-μM range (IC50 0.35-0.77 μM) and four of them showed an improved selectivity (selectivity index >38-folds vs. murine and human macrohages). For the glycosyl selenylsulfides, the anti-trypanosomal activity was not significantly influenced by the nature of the moiety attached to the sulfur atom. Except for a quinoline-, and to a minor extent a nitro-derivative, the most selective hits induced a rapid (within 60 min) and marked perturbation of the LMWT-redox homeostasis. The formation of selenenylsulfide glycoconjugates with free thiols has been identified as a potential mechanism involved in this process. Copyright © 2024 The Authors. Published by Elsevier Ltd.. All rights reserved.

Citation

Estefanía Dibello, Natalia Oddone, Jaime Franco, Tünde-Zita Illyés, Andrea Medeiros, Attila Kiss, Fanni Hőgye, Katalin E Kövér, László Szilágyi, Marcelo A Comini. Selenosugars targeting the infective stage of Trypanosoma brucei with high selectivity. International journal for parasitology. Drugs and drug resistance. 2024 Apr;24:100529

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PMID: 38461700

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