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
- Institución
- Consejo Nacional de Investigaciones Científicas y Técnicas
- OAI Identificador
- oai:ri.conicet.gov.ar:11336/13838
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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 Técnicas2025-09-29T10:42:06Zoai: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:34982025-09-29 10:42:06.435CONICET 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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1844614453564276736 |
score |
13.070432 |