Artículo

Frank, F.M.; Ciccarelli, A.B.; Bollini, M.; Bruno, A.M.; Batlle, A.; Lombardo, M.E. "Trypanocidal activity of thioamide-substituted imidazoquinolinone: Electrochemical properties and biological effects" (2013) Evidence-based Complementary and Alternative Medicine. 2013
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Abstract:

Three thioamide-substituted imidazoquinolinone, which possess a heterocyclic center similar to tryptanthrin and are named C1, C2, and C3, were studied regarding (a) their in vitro anti-Trypanosoma cruzi activity, (b) their cytotoxicity and electrochemical behaviour, and (c) their 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 M; IC50 amas=1.74 M; and IC50 try=34.89 M). The presence of an antioxidant compound such as ascorbic acid or dithiotreitol induced a threefold 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. © 2013 Fernanda M. Frank et al.

Registro:

Documento: Artículo
Título:Trypanocidal activity of thioamide-substituted imidazoquinolinone: Electrochemical properties and biological effects
Autor:Frank, F.M.; Ciccarelli, A.B.; Bollini, M.; Bruno, A.M.; Batlle, A.; Lombardo, M.E.
Filiación:Departamento de Microbiología, Facultad de Medicina, UBA, Paraguay 2155 P13, 1121 Buenos Aires, Argentina
Centro de Investigaciones Sobre Porfirinas y Porfirias, CIPYP (UBA-CONICET), Hospital de Clínicas José de San Martín, Córdoba 2351, 1120 Buenos Aires, Argentina
Departamento de Química Orgánica, Facultad de Farmacia y Bioquímica, UBA, Junín 956, 1113 Buenos Aires, Argentina
Departamento de Química Biológica, Facultad de Ciencias Exactas y Naturales, Int. Güiraldes 2160, 1428 Buenos Aires, Argentina
Palabras clave:antiparasitic agent; imidazoquinolinone derivative; thioamide; unclassified drug; animal cell; antitrypanosomal activity; apoptosis; article; biological activity; cell viability; controlled study; cytotoxicity; cytotoxicity test; drug activity; electrochemical analysis; epimastigote; IC 50; in vitro study; male; molecular weight; mouse; nonhuman; oxidation reduction state; oxidative stress; priority journal; Trypanosoma cruzi; trypomastigote
Año:2013
Volumen:2013
DOI: http://dx.doi.org/10.1155/2013/945953
Título revista:Evidence-based Complementary and Alternative Medicine
Título revista abreviado:Evid.-Based Complement. Altern. Med.
ISSN:1741427X
Registro:https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_1741427X_v2013_n_p_Frank

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Citas:

---------- APA ----------
Frank, F.M., Ciccarelli, A.B., Bollini, M., Bruno, A.M., Batlle, A. & Lombardo, M.E. (2013) . Trypanocidal activity of thioamide-substituted imidazoquinolinone: Electrochemical properties and biological effects. Evidence-based Complementary and Alternative Medicine, 2013.
http://dx.doi.org/10.1155/2013/945953
---------- CHICAGO ----------
Frank, F.M., Ciccarelli, A.B., Bollini, M., Bruno, A.M., Batlle, A., Lombardo, M.E. "Trypanocidal activity of thioamide-substituted imidazoquinolinone: Electrochemical properties and biological effects" . Evidence-based Complementary and Alternative Medicine 2013 (2013).
http://dx.doi.org/10.1155/2013/945953
---------- MLA ----------
Frank, F.M., Ciccarelli, A.B., Bollini, M., Bruno, A.M., Batlle, A., Lombardo, M.E. "Trypanocidal activity of thioamide-substituted imidazoquinolinone: Electrochemical properties and biological effects" . Evidence-based Complementary and Alternative Medicine, vol. 2013, 2013.
http://dx.doi.org/10.1155/2013/945953
---------- VANCOUVER ----------
Frank, F.M., Ciccarelli, A.B., Bollini, M., Bruno, A.M., Batlle, A., Lombardo, M.E. Trypanocidal activity of thioamide-substituted imidazoquinolinone: Electrochemical properties and biological effects. Evid.-Based Complement. Altern. Med. 2013;2013.
http://dx.doi.org/10.1155/2013/945953