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dc.contributor.author
Ferreira de Almeida Fiuza, Ludmila
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dc.contributor.author
Batista, Denise G. J.
dc.contributor.author
Girão, Roberson D.
dc.contributor.author
Hulpia, Fabian
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Finamore-Araújo, Paula
dc.contributor.author
Aldfer, Mustafa M.
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Elmahallawy, Ehab Kotb
dc.contributor.author
De Koning, Harry P.
dc.contributor.author
Moreira, Otacílio
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Van Calenbergh, Serge
dc.contributor.author
Soeiro, Maria de Nazaré C.
dc.date.available
2023-09-29T17:18:02Z
dc.date.issued
2022-11
dc.identifier.citation
Ferreira de Almeida Fiuza, Ludmila; Batista, Denise G. J.; Girão, Roberson D.; Hulpia, Fabian; Finamore-Araújo, Paula; et al.; Phenotypic Evaluation of Nucleoside Analogues against Trypanosoma cruzi Infection: In Vitro and In Vivo Approaches; Molecular Diversity Preservation International; Molecules; 27; 22; 11-2022; 1-17
dc.identifier.issn
1420-3049
dc.identifier.uri
http://hdl.handle.net/11336/213632
dc.description.abstract
Chagas disease, caused by Trypanosoma cruzi (T. cruzi), is a serious public health problem. Current treatment is restricted to two drugs, benznidazole and nifurtimox, displaying serious efficacy and safety drawbacks. Nucleoside analogues represent a promising alternative as protozoans do not biosynthesize purines and rely on purine salvage from the hosts. Protozoan transporters often present different substrate specificities from mammalian transporters, justifying the exploration of nucleoside analogues as therapeutic agents. Previous reports identified nucleosides with potent trypanocidal activity; therefore, two 7-derivatized tubercidins (FH11706, FH10714) and a 3′-deoxytubercidin (FH8513) were assayed against T. cruzi. They were highly potent and selective, and the uptake of the tubercidin analogues appeared to be mediated by the nucleoside transporter TcrNT2. At 10 μM, the analogues reduced parasitemia >90% in 2D and 3D cardiac cultures. The washout assays showed that FH10714 sterilized the infected cultures. Given orally, the compounds did not induce noticeable mouse toxicity (50 mg/kg), suppressed the parasitemia of T. cruzi-infected Swiss mice (25 mg/kg, 5 days) and presented DNA amplification below the limit of detection. These findings justify further studies with longer treatment regimens, as well as evaluations in combination with nitro drugs, aiming to identify more effective and safer therapies for Chagas disease.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Molecular Diversity Preservation International
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dc.rights
info:eu-repo/semantics/openAccess
dc.rights.uri
https://creativecommons.org/licenses/by/2.5/ar/
dc.subject
CHAGAS DISEASE
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EXPERIMENTAL CHEMOTHERAPY
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NUCLEOSIDE DERIVATIVES
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THYMIDINE TRANSPORTER
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TRYPANOSOMA CRUZI
dc.subject.classification
Biología Celular, Microbiología
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dc.subject.classification
Ciencias Biológicas
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CIENCIAS NATURALES Y EXACTAS
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dc.title
Phenotypic Evaluation of Nucleoside Analogues against Trypanosoma cruzi Infection: In Vitro and In Vivo Approaches
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2023-07-07T22:59:29Z
dc.journal.volume
27
dc.journal.number
22
dc.journal.pagination
1-17
dc.journal.pais
Suiza
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dc.description.fil
Fil: Ferreira de Almeida Fiuza, Ludmila. Fundación Oswaldo Cruz; Brasil. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Química y Metabolismo del Fármaco. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Instituto de Química y Metabolismo del Fármaco; Argentina
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Fil: Batista, Denise G. J.. Fundación Oswaldo Cruz; Brasil
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Fil: Girão, Roberson D.. Fundación Oswaldo Cruz; Brasil
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Fil: Hulpia, Fabian. University of Ghent; Bélgica
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Fil: Finamore-Araújo, Paula. Fundación Oswaldo Cruz; Brasil
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Fil: Aldfer, Mustafa M.. University of Glasgow; Reino Unido
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Fil: Elmahallawy, Ehab Kotb. University of Glasgow; Reino Unido
dc.description.fil
Fil: De Koning, Harry P.. University of Glasgow; Reino Unido
dc.description.fil
Fil: Moreira, Otacílio. Fundación Oswaldo Cruz; Brasil
dc.description.fil
Fil: Van Calenbergh, Serge. University of Ghent; Bélgica
dc.description.fil
Fil: Soeiro, Maria de Nazaré C.. Fundación Oswaldo Cruz; Brasil
dc.journal.title
Molecules
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dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.3390/molecules27228087
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