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dc.contributor.author
Frank, Fernanda Maria
dc.contributor.author
Ciccarelli, Allejandra Beatriz
dc.contributor.author
Bollini, Mariela
dc.contributor.author
Bruno, Ana M.
dc.contributor.author
Batlle, Alcira Maria del C.
dc.contributor.author
Lombardo, Maria Elisa
dc.date.available
2016-10-24T20:21:10Z
dc.date.issued
2013-07
dc.identifier.citation
Frank, Fernanda Maria; Ciccarelli, Allejandra Beatriz; Bollini, Mariela; Bruno, Ana M.; Batlle, Alcira Maria del C.; et al.; Trypanocidal activity of tioamide-sustituted imidazoisoquinolinones: Electrochemical properties and biological effects; Hindawi Publishing Corporation; Evidence-based Complementary And Alternative Medicine; 2013; 7-2013; 1-10
dc.identifier.issn
1741-427X
dc.identifier.uri
http://hdl.handle.net/11336/7791
dc.description.abstract
Three thioamide-substituted imidazoisoquinolinones, which possess an heterocyclic center similar to tryptanthrin and are named C1, C2 and C3, were studied regarding: a) its in vitro anti-Trypanosoma cruzi activity, b) its cytotoxicity and electrochemical behaviour and c) its effect on cell viability, redox state and mitochondrial function . The assayed compounds showed a significant activity against the proliferative forms, but only C1 showed activity on the trypomastigote form (for C1, IC50 epi = 1.49 µM; IC50 amas = 1.74 µM and IC50 try = 34.89 µM). The presence of an antioxidant compound such as ascorbic acid or dithiotreitol induced a three-fold increase in the antiparasitic activity, whereas glutathione had a dual effect depending on its concentration. Our results indicate that these compounds, which exhibited low toxicity to the host cells, can be reduced inside the parasite by means of the pool of low molecular weight thiols, causing oxidative stress and parasite death by apoptosis. The antiparasitic activity of the compounds studied could be explained by a loss of the capacity of the antioxidant defense system of the parasite to keep its intracellular redox state. C1 could be considered a good candidate for in vivo evaluation .
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Hindawi Publishing Corporation
dc.rights
info:eu-repo/semantics/openAccess
dc.rights.uri
https://creativecommons.org/licenses/by/2.5/ar/
dc.subject
Trypanosoma Cruzi
dc.subject
Chemotherapy
dc.subject
Imidazoizoquinolinones
dc.subject
Antioxidant Defense System
dc.subject.classification
Biología Celular, Microbiología
dc.subject.classification
Ciencias Biológicas
dc.subject.classification
CIENCIAS NATURALES Y EXACTAS
dc.title
Trypanocidal activity of tioamide-sustituted imidazoisoquinolinones: Electrochemical properties and biological effects
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2016-08-30T17:09:30Z
dc.identifier.eissn
1741-4288
dc.journal.volume
2013
dc.journal.pagination
1-10
dc.journal.pais
Reino Unido
dc.journal.ciudad
Oxford
dc.description.fil
Fil: Frank, Fernanda Maria. Consejo Nacional de Investigaciones Cienti­ficas y Tecnicas. Oficina de Coordinacion Administrativa Houssay. Instituto de Estudios de la Inmunidad Humoral "Profesor R. A. Margni"; Argentina
dc.description.fil
Fil: Ciccarelli, Allejandra Beatriz. Consejo Nacional de Investigaciones Cientificas y Tecnicas. Oficina de Coordinacion Administrativa Houssay. Centro de Investigacion Sobre Porfirinas y Porfirias; Argentina
dc.description.fil
Fil: Bollini, Mariela. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Química Orgánica; Argentina
dc.description.fil
Fil: Bruno, Ana M.. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Química Orgánica; Argentina
dc.description.fil
Fil: Batlle, Alcira Maria del C.. Consejo Nacional de Investigaciones Cientificas y Tecnicas. Oficina de Coordinacion Administrativa Houssay. Centro de Investigacion Sobre Porfirinas y Porfirias; Argentina
dc.description.fil
Fil: Lombardo, Maria Elisa. Consejo Nacional de Investigaciones Cientificas y Tecnicas. Oficina de Coordinacion Administrativa Houssay. Centro de Investigacion Sobre Porfirinas y Porfirias; Argentina. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Departamento de Química Biológica; Argentina
dc.journal.title
Evidence-based Complementary And Alternative Medicine
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/https://www.hindawi.com/journals/ecam/2013/945953/
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/http://dx.doi.org/10.1155/2013/945953


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