In vitro activity ofN-benzenesulfonylbenzotriazole on Trypanosoma cruzi epimastigote and trypomastigote forms

Autores
Becerra, María Cecilia; Guiñazú, N.; Hergert, Lisandro Yamil; Pellegrini, Andrea Vanina; Mazzieri, M. R.; Gea, Susana; Albesa, Inés
Año de publicación
2012
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
Chagas disease is still an important health problem in Central and South America. However, the only drugs currently available for specific treatment of this disease may induce toxic side effects in the host. The aim of this work was to determine the activity of N-benzenesulfonylbenzotriazole (BSBZT) against the protozoan parasite Trypanosoma cruzi. The effects of BSBZT and benzotriazole (BZT) were compared to those of benznidazole (BZL) on epimastigote and trypomastigote forms. BSBZT was found to have an in vitro growth inhibitory dose-dependent activity against epimastigotes, with flow cytometry analysis confirming that the treated parasites presented size reduction. BSBZT showed an IC50 of 21.56 μg/mL (81.07 μM) against epimastigotes at 72 h of incubation, whereas BZT did not affect the growth of this parasite form. Furthermore, the toxic effect of BSBZT, was stronger and appeared earlier (at 24 h) in trypomastigotes than in epimastigotes, with the LC50 of this compound being 28.40 μg/mL (106.79 μM) against trypomastigotes. The concentrations of BSBZT used in this study presented low hemolytic activity and cytotoxicity. Consequently, at concentrations near IC50 and LC50 (25 μg/mL), BSBZT caused only 2.4% hemolysis and 15% of RAW 264.7 cell cytotoxicity. These results reveal the potential of BSBZT as a prototype in drug design for developing new anti-T. cruzi compounds.
Fil: Becerra, María Cecilia. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Córdoba. Instituto Multidisciplinario de Biología Vegetal (p); Argentina. Universidad Nacional de Córdoba; Argentina
Fil: Guiñazú, N.. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Córdoba. Centro de Investigaciones en Bioquímica Clínica e Inmunología; Argentina
Fil: Hergert, Lisandro Yamil. Universidad Nacional de Córdoba; Argentina
Fil: Pellegrini, Andrea Vanina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Córdoba. Centro de Investigaciones En Bioquímica Clínica E Inmunología; Argentina
Fil: Mazzieri, M. R.. Universidad Nacional de Cordoba. Facultad de Ciencias Quimicas. Departamento de Farmacia; Argentina
Fil: Gea, Susana. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Córdoba. Centro de Investigaciones En Bioquímica Clínica E Inmunología; Argentina
Fil: Albesa, Inés. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Córdoba. Instituto Multidisciplinario de Biología Vegetal (p); Argentina. Universidad Nacional de Córdoba; Argentina
Materia
Benzenesulfonylbenzotriazole
Trypanocidal Activity
Prototype
Benzotriazole
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/13838
Acceder
id CONICETDig_f58c329d512926a6eed3869deb62b914
oai_identifier_str oai:ri.conicet.gov.ar:11336/13838
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling In vitro activity ofN-benzenesulfonylbenzotriazole on Trypanosoma cruzi epimastigote and trypomastigote formsBecerra, María CeciliaGuiñazú, N.Hergert, Lisandro YamilPellegrini, Andrea VaninaMazzieri, M. R.Gea, SusanaAlbesa, InésBenzenesulfonylbenzotriazoleTrypanocidal ActivityPrototypeBenzotriazolehttps://purl.org/becyt/ford/3.3https://purl.org/becyt/ford/3Chagas disease is still an important health problem in Central and South America. However, the only drugs currently available for specific treatment of this disease may induce toxic side effects in the host. The aim of this work was to determine the activity of N-benzenesulfonylbenzotriazole (BSBZT) against the protozoan parasite Trypanosoma cruzi. The effects of BSBZT and benzotriazole (BZT) were compared to those of benznidazole (BZL) on epimastigote and trypomastigote forms. BSBZT was found to have an in vitro growth inhibitory dose-dependent activity against epimastigotes, with flow cytometry analysis confirming that the treated parasites presented size reduction. BSBZT showed an IC50 of 21.56 μg/mL (81.07 μM) against epimastigotes at 72 h of incubation, whereas BZT did not affect the growth of this parasite form. Furthermore, the toxic effect of BSBZT, was stronger and appeared earlier (at 24 h) in trypomastigotes than in epimastigotes, with the LC50 of this compound being 28.40 μg/mL (106.79 μM) against trypomastigotes. The concentrations of BSBZT used in this study presented low hemolytic activity and cytotoxicity. Consequently, at concentrations near IC50 and LC50 (25 μg/mL), BSBZT caused only 2.4% hemolysis and 15% of RAW 264.7 cell cytotoxicity. These results reveal the potential of BSBZT as a prototype in drug design for developing new anti-T. cruzi compounds.Fil: Becerra, María Cecilia. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Córdoba. Instituto Multidisciplinario de Biología Vegetal (p); Argentina. Universidad Nacional de Córdoba; ArgentinaFil: Guiñazú, N.. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Córdoba. Centro de Investigaciones en Bioquímica Clínica e Inmunología; ArgentinaFil: Hergert, Lisandro Yamil. Universidad Nacional de Córdoba; ArgentinaFil: Pellegrini, Andrea Vanina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Córdoba. Centro de Investigaciones En Bioquímica Clínica E Inmunología; ArgentinaFil: Mazzieri, M. R.. Universidad Nacional de Cordoba. Facultad de Ciencias Quimicas. Departamento de Farmacia; ArgentinaFil: Gea, Susana. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Córdoba. Centro de Investigaciones En Bioquímica Clínica E Inmunología; ArgentinaFil: Albesa, Inés. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Córdoba. Instituto Multidisciplinario de Biología Vegetal (p); Argentina. Universidad Nacional de Córdoba; ArgentinaElsevier2012-03info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/13838Becerra, María Cecilia; Guiñazú, N.; Hergert, Lisandro Yamil; Pellegrini, Andrea Vanina; Mazzieri, M. R.; et al.; In vitro activity ofN-benzenesulfonylbenzotriazole on Trypanosoma cruzi epimastigote and trypomastigote forms; Elsevier; Experimental Parasitology; 131; 1; 3-2012; 57-620014-48941090-2449enginfo:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0014489412000823info:eu-repo/semantics/altIdentifier/doi/10.1016/j.exppara.2012.02.028info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-nd/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-10-15T15:40:04Zoai:ri.conicet.gov.ar:11336/13838instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982025-10-15 15:40:05.16CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv In vitro activity ofN-benzenesulfonylbenzotriazole on Trypanosoma cruzi epimastigote and trypomastigote forms
title In vitro activity ofN-benzenesulfonylbenzotriazole on Trypanosoma cruzi epimastigote and trypomastigote forms
spellingShingle In vitro activity ofN-benzenesulfonylbenzotriazole on Trypanosoma cruzi epimastigote and trypomastigote forms
Becerra, María Cecilia
Benzenesulfonylbenzotriazole
Trypanocidal Activity
Prototype
Benzotriazole
title_short In vitro activity ofN-benzenesulfonylbenzotriazole on Trypanosoma cruzi epimastigote and trypomastigote forms
title_full In vitro activity ofN-benzenesulfonylbenzotriazole on Trypanosoma cruzi epimastigote and trypomastigote forms
title_fullStr In vitro activity ofN-benzenesulfonylbenzotriazole on Trypanosoma cruzi epimastigote and trypomastigote forms
title_full_unstemmed In vitro activity ofN-benzenesulfonylbenzotriazole on Trypanosoma cruzi epimastigote and trypomastigote forms
title_sort In vitro activity ofN-benzenesulfonylbenzotriazole on Trypanosoma cruzi epimastigote and trypomastigote forms
dc.creator.none.fl_str_mv Becerra, María Cecilia
Guiñazú, N.
Hergert, Lisandro Yamil
Pellegrini, Andrea Vanina
Mazzieri, M. R.
Gea, Susana
Albesa, Inés
author Becerra, María Cecilia
author_facet Becerra, María Cecilia
Guiñazú, N.
Hergert, Lisandro Yamil
Pellegrini, Andrea Vanina
Mazzieri, M. R.
Gea, Susana
Albesa, Inés
author_role author
author2 Guiñazú, N.
Hergert, Lisandro Yamil
Pellegrini, Andrea Vanina
Mazzieri, M. R.
Gea, Susana
Albesa, Inés
author2_role author
author
author
author
author
author
dc.subject.none.fl_str_mv Benzenesulfonylbenzotriazole
Trypanocidal Activity
Prototype
Benzotriazole
topic Benzenesulfonylbenzotriazole
Trypanocidal Activity
Prototype
Benzotriazole
purl_subject.fl_str_mv https://purl.org/becyt/ford/3.3
https://purl.org/becyt/ford/3
dc.description.none.fl_txt_mv Chagas disease is still an important health problem in Central and South America. However, the only drugs currently available for specific treatment of this disease may induce toxic side effects in the host. The aim of this work was to determine the activity of N-benzenesulfonylbenzotriazole (BSBZT) against the protozoan parasite Trypanosoma cruzi. The effects of BSBZT and benzotriazole (BZT) were compared to those of benznidazole (BZL) on epimastigote and trypomastigote forms. BSBZT was found to have an in vitro growth inhibitory dose-dependent activity against epimastigotes, with flow cytometry analysis confirming that the treated parasites presented size reduction. BSBZT showed an IC50 of 21.56 μg/mL (81.07 μM) against epimastigotes at 72 h of incubation, whereas BZT did not affect the growth of this parasite form. Furthermore, the toxic effect of BSBZT, was stronger and appeared earlier (at 24 h) in trypomastigotes than in epimastigotes, with the LC50 of this compound being 28.40 μg/mL (106.79 μM) against trypomastigotes. The concentrations of BSBZT used in this study presented low hemolytic activity and cytotoxicity. Consequently, at concentrations near IC50 and LC50 (25 μg/mL), BSBZT caused only 2.4% hemolysis and 15% of RAW 264.7 cell cytotoxicity. These results reveal the potential of BSBZT as a prototype in drug design for developing new anti-T. cruzi compounds.
Fil: Becerra, María Cecilia. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Córdoba. Instituto Multidisciplinario de Biología Vegetal (p); Argentina. Universidad Nacional de Córdoba; Argentina
Fil: Guiñazú, N.. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Córdoba. Centro de Investigaciones en Bioquímica Clínica e Inmunología; Argentina
Fil: Hergert, Lisandro Yamil. Universidad Nacional de Córdoba; Argentina
Fil: Pellegrini, Andrea Vanina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Córdoba. Centro de Investigaciones En Bioquímica Clínica E Inmunología; Argentina
Fil: Mazzieri, M. R.. Universidad Nacional de Cordoba. Facultad de Ciencias Quimicas. Departamento de Farmacia; Argentina
Fil: Gea, Susana. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Córdoba. Centro de Investigaciones En Bioquímica Clínica E Inmunología; Argentina
Fil: Albesa, Inés. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Córdoba. Instituto Multidisciplinario de Biología Vegetal (p); Argentina. Universidad Nacional de Córdoba; Argentina
description Chagas disease is still an important health problem in Central and South America. However, the only drugs currently available for specific treatment of this disease may induce toxic side effects in the host. The aim of this work was to determine the activity of N-benzenesulfonylbenzotriazole (BSBZT) against the protozoan parasite Trypanosoma cruzi. The effects of BSBZT and benzotriazole (BZT) were compared to those of benznidazole (BZL) on epimastigote and trypomastigote forms. BSBZT was found to have an in vitro growth inhibitory dose-dependent activity against epimastigotes, with flow cytometry analysis confirming that the treated parasites presented size reduction. BSBZT showed an IC50 of 21.56 μg/mL (81.07 μM) against epimastigotes at 72 h of incubation, whereas BZT did not affect the growth of this parasite form. Furthermore, the toxic effect of BSBZT, was stronger and appeared earlier (at 24 h) in trypomastigotes than in epimastigotes, with the LC50 of this compound being 28.40 μg/mL (106.79 μM) against trypomastigotes. The concentrations of BSBZT used in this study presented low hemolytic activity and cytotoxicity. Consequently, at concentrations near IC50 and LC50 (25 μg/mL), BSBZT caused only 2.4% hemolysis and 15% of RAW 264.7 cell cytotoxicity. These results reveal the potential of BSBZT as a prototype in drug design for developing new anti-T. cruzi compounds.
publishDate 2012
dc.date.none.fl_str_mv 2012-03
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
http://purl.org/coar/resource_type/c_6501
info:ar-repo/semantics/articulo
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv http://hdl.handle.net/11336/13838
Becerra, María Cecilia; Guiñazú, N.; Hergert, Lisandro Yamil; Pellegrini, Andrea Vanina; Mazzieri, M. R.; et al.; In vitro activity ofN-benzenesulfonylbenzotriazole on Trypanosoma cruzi epimastigote and trypomastigote forms; Elsevier; Experimental Parasitology; 131; 1; 3-2012; 57-62
0014-4894
1090-2449
url http://hdl.handle.net/11336/13838
identifier_str_mv Becerra, María Cecilia; Guiñazú, N.; Hergert, Lisandro Yamil; Pellegrini, Andrea Vanina; Mazzieri, M. R.; et al.; In vitro activity ofN-benzenesulfonylbenzotriazole on Trypanosoma cruzi epimastigote and trypomastigote forms; Elsevier; Experimental Parasitology; 131; 1; 3-2012; 57-62
0014-4894
1090-2449
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0014489412000823
info:eu-repo/semantics/altIdentifier/doi/10.1016/j.exppara.2012.02.028
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
dc.format.none.fl_str_mv application/pdf
application/pdf
dc.publisher.none.fl_str_mv Elsevier
publisher.none.fl_str_mv Elsevier
dc.source.none.fl_str_mv reponame:CONICET Digital (CONICET)
instname:Consejo Nacional de Investigaciones Científicas y Técnicas
reponame_str CONICET Digital (CONICET)
collection CONICET Digital (CONICET)
instname_str Consejo Nacional de Investigaciones Científicas y Técnicas
repository.name.fl_str_mv CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicas
repository.mail.fl_str_mv dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar
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score 13.22299

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