Selenosugars targeting the infective stage of Trypanosoma brucei with high selectivity

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 38-folds vs. murine and human macrohages). For the glycosyl selenylsulfides, the anti-trypanosomal activity was n...

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Published in:International journal for parasitology -- drugs and drug resistance 2024-04, Vol.24, p.100529-100529, Article 100529
Main Authors: Dibello, Estefanía, Oddone, Natalia, Franco, Jaime, Illyés, Tünde-Zita, Medeiros, Andrea, Kiss, Attila, Hőgye, Fanni, Kövér, Katalin E., Szilágyi, László, Comini, Marcelo A.
Format: Article
Language:English
Subjects:
Bloodstream trypanosoma
Macrophage
Oxidative stress
Redox biosensor
Selenoglycosides
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Summary: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 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. [Display omitted]
ISSN:2211-3207
2211-3207
DOI:10.1016/j.ijpddr.2024.100529