Identification of N-benzylacetamide as a major component of human plasmatic metabolic profiling of benznidazole
- Autores
- Marson, María Elena; Altcheh, Jaime; Moscatelli, Guillermo; Moroni, Samanta; Garcia-Bournissen, Facundo; Mastrantonio Garrido, Guido Enrique
- Año de publicación
- 2015
- Idioma
- inglés
- Tipo de recurso
- artículo
- Estado
- versión publicada
- Descripción
- Chagas disease is an endemic infection in Latin America with a high health impact. Caused by the parasite Trypanosoma cruzi, it has expanded to non-endemic regions such as North America and European countries via immigration of infected people. This infectious disease has been rising in the ranking of international health priorities due to the growing migration flows from endemic to non-endemic areas. Benznidazole (BZN), a nitroheterocyclic drug, is one of the two trypanocidal drugs currently in clinical use, associated with significant adverse drug reactions (ADRs). Mammalian metabolism of BNZ has been poorly studied, including the potential role of metabolites on both toxicity and anti-parasitic activity. High-resolution UPLC/MS/MS was used to analyze three plasma samples obtained from pediatric patients under BNZ treatment in steady state. Spectroscopic and structural criteria were applied to identify BNZ and accompanying substances from chromatographic signals. From all detected species, two can be undoubtedly associated with the BNZ and N-benzylacetamide molecules, the second one being a fragment of the parent drug (BZN). From the obtained results, two hypotheses could be formulated. The first one is to relate the presence of N-benzyl acetamide with the hepatic metabolism of BNZ. The second hypothesis has to do with the possible trypanocidal activity of this metabolite, as well as its role in the development of side effects, associated with the pharmacotherapy. Complementary studies should be carried out to determine the possible association of this metabolite with the BNZ treatment stages, patient's clinical features, ADRs, and trypanocidal effectiveness.
Facultad de Ciencias Exactas
Planta Piloto Multipropósito - Laboratorio de Servicios a la Industria y al Sistema Científico - Materia
-
Ciencias Exactas
Biología
Nitrocompounds
Benznidazole
N-benzylacetamide
Chagas disease
Metabolite
UPLC/MS/MS
Plasma
Pediatric pharmacology - Nivel de accesibilidad
- acceso abierto
- Condiciones de uso
- http://creativecommons.org/licenses/by-nc-sa/4.0/
- Repositorio
- Institución
- Universidad Nacional de La Plata
- OAI Identificador
- oai:sedici.unlp.edu.ar:10915/130827
Ver los metadatos del registro completo
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Identification of N-benzylacetamide as a major component of human plasmatic metabolic profiling of benznidazoleMarson, María ElenaAltcheh, JaimeMoscatelli, GuillermoMoroni, SamantaGarcia-Bournissen, FacundoMastrantonio Garrido, Guido EnriqueCiencias ExactasBiologíaNitrocompoundsBenznidazoleN-benzylacetamideChagas diseaseMetaboliteUPLC/MS/MSPlasmaPediatric pharmacologyChagas disease is an endemic infection in Latin America with a high health impact. Caused by the parasite <i>Trypanosoma cruzi</i>, it has expanded to non-endemic regions such as North America and European countries via immigration of infected people. This infectious disease has been rising in the ranking of international health priorities due to the growing migration flows from endemic to non-endemic areas. Benznidazole (BZN), a nitroheterocyclic drug, is one of the two trypanocidal drugs currently in clinical use, associated with significant adverse drug reactions (ADRs). Mammalian metabolism of BNZ has been poorly studied, including the potential role of metabolites on both toxicity and anti-parasitic activity. High-resolution UPLC/MS/MS was used to analyze three plasma samples obtained from pediatric patients under BNZ treatment in steady state. Spectroscopic and structural criteria were applied to identify BNZ and accompanying substances from chromatographic signals. From all detected species, two can be undoubtedly associated with the BNZ and N-benzylacetamide molecules, the second one being a fragment of the parent drug (BZN). From the obtained results, two hypotheses could be formulated. The first one is to relate the presence of N-benzyl acetamide with the hepatic metabolism of BNZ. The second hypothesis has to do with the possible trypanocidal activity of this metabolite, as well as its role in the development of side effects, associated with the pharmacotherapy. Complementary studies should be carried out to determine the possible association of this metabolite with the BNZ treatment stages, patient's clinical features, ADRs, and trypanocidal effectiveness.Facultad de Ciencias ExactasPlanta Piloto Multipropósito - Laboratorio de Servicios a la Industria y al Sistema Científico2015-06info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionArticulohttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdf209-217http://sedici.unlp.edu.ar/handle/10915/130827enginfo:eu-repo/semantics/altIdentifier/issn/0378-7966info:eu-repo/semantics/altIdentifier/issn/2107-0180info:eu-repo/semantics/altIdentifier/doi/10.1007/s13318-014-0195-8info:eu-repo/semantics/altIdentifier/pmid/24711214info:eu-repo/semantics/openAccesshttp://creativecommons.org/licenses/by-nc-sa/4.0/Creative Commons Attribution-NonCommercial-ShareAlike 4.0 International (CC BY-NC-SA 4.0)reponame:SEDICI (UNLP)instname:Universidad Nacional de La Platainstacron:UNLP2025-10-15T11:24:09Zoai:sedici.unlp.edu.ar:10915/130827Institucionalhttp://sedici.unlp.edu.ar/Universidad públicaNo correspondehttp://sedici.unlp.edu.ar/oai/snrdalira@sedici.unlp.edu.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:13292025-10-15 11:24:09.838SEDICI (UNLP) - Universidad Nacional de La Platafalse |
dc.title.none.fl_str_mv |
Identification of N-benzylacetamide as a major component of human plasmatic metabolic profiling of benznidazole |
title |
Identification of N-benzylacetamide as a major component of human plasmatic metabolic profiling of benznidazole |
spellingShingle |
Identification of N-benzylacetamide as a major component of human plasmatic metabolic profiling of benznidazole Marson, María Elena Ciencias Exactas Biología Nitrocompounds Benznidazole N-benzylacetamide Chagas disease Metabolite UPLC/MS/MS Plasma Pediatric pharmacology |
title_short |
Identification of N-benzylacetamide as a major component of human plasmatic metabolic profiling of benznidazole |
title_full |
Identification of N-benzylacetamide as a major component of human plasmatic metabolic profiling of benznidazole |
title_fullStr |
Identification of N-benzylacetamide as a major component of human plasmatic metabolic profiling of benznidazole |
title_full_unstemmed |
Identification of N-benzylacetamide as a major component of human plasmatic metabolic profiling of benznidazole |
title_sort |
Identification of N-benzylacetamide as a major component of human plasmatic metabolic profiling of benznidazole |
dc.creator.none.fl_str_mv |
Marson, María Elena Altcheh, Jaime Moscatelli, Guillermo Moroni, Samanta Garcia-Bournissen, Facundo Mastrantonio Garrido, Guido Enrique |
author |
Marson, María Elena |
author_facet |
Marson, María Elena Altcheh, Jaime Moscatelli, Guillermo Moroni, Samanta Garcia-Bournissen, Facundo Mastrantonio Garrido, Guido Enrique |
author_role |
author |
author2 |
Altcheh, Jaime Moscatelli, Guillermo Moroni, Samanta Garcia-Bournissen, Facundo Mastrantonio Garrido, Guido Enrique |
author2_role |
author author author author author |
dc.subject.none.fl_str_mv |
Ciencias Exactas Biología Nitrocompounds Benznidazole N-benzylacetamide Chagas disease Metabolite UPLC/MS/MS Plasma Pediatric pharmacology |
topic |
Ciencias Exactas Biología Nitrocompounds Benznidazole N-benzylacetamide Chagas disease Metabolite UPLC/MS/MS Plasma Pediatric pharmacology |
dc.description.none.fl_txt_mv |
Chagas disease is an endemic infection in Latin America with a high health impact. Caused by the parasite <i>Trypanosoma cruzi</i>, it has expanded to non-endemic regions such as North America and European countries via immigration of infected people. This infectious disease has been rising in the ranking of international health priorities due to the growing migration flows from endemic to non-endemic areas. Benznidazole (BZN), a nitroheterocyclic drug, is one of the two trypanocidal drugs currently in clinical use, associated with significant adverse drug reactions (ADRs). Mammalian metabolism of BNZ has been poorly studied, including the potential role of metabolites on both toxicity and anti-parasitic activity. High-resolution UPLC/MS/MS was used to analyze three plasma samples obtained from pediatric patients under BNZ treatment in steady state. Spectroscopic and structural criteria were applied to identify BNZ and accompanying substances from chromatographic signals. From all detected species, two can be undoubtedly associated with the BNZ and N-benzylacetamide molecules, the second one being a fragment of the parent drug (BZN). From the obtained results, two hypotheses could be formulated. The first one is to relate the presence of N-benzyl acetamide with the hepatic metabolism of BNZ. The second hypothesis has to do with the possible trypanocidal activity of this metabolite, as well as its role in the development of side effects, associated with the pharmacotherapy. Complementary studies should be carried out to determine the possible association of this metabolite with the BNZ treatment stages, patient's clinical features, ADRs, and trypanocidal effectiveness. Facultad de Ciencias Exactas Planta Piloto Multipropósito - Laboratorio de Servicios a la Industria y al Sistema Científico |
description |
Chagas disease is an endemic infection in Latin America with a high health impact. Caused by the parasite <i>Trypanosoma cruzi</i>, it has expanded to non-endemic regions such as North America and European countries via immigration of infected people. This infectious disease has been rising in the ranking of international health priorities due to the growing migration flows from endemic to non-endemic areas. Benznidazole (BZN), a nitroheterocyclic drug, is one of the two trypanocidal drugs currently in clinical use, associated with significant adverse drug reactions (ADRs). Mammalian metabolism of BNZ has been poorly studied, including the potential role of metabolites on both toxicity and anti-parasitic activity. High-resolution UPLC/MS/MS was used to analyze three plasma samples obtained from pediatric patients under BNZ treatment in steady state. Spectroscopic and structural criteria were applied to identify BNZ and accompanying substances from chromatographic signals. From all detected species, two can be undoubtedly associated with the BNZ and N-benzylacetamide molecules, the second one being a fragment of the parent drug (BZN). From the obtained results, two hypotheses could be formulated. The first one is to relate the presence of N-benzyl acetamide with the hepatic metabolism of BNZ. The second hypothesis has to do with the possible trypanocidal activity of this metabolite, as well as its role in the development of side effects, associated with the pharmacotherapy. Complementary studies should be carried out to determine the possible association of this metabolite with the BNZ treatment stages, patient's clinical features, ADRs, and trypanocidal effectiveness. |
publishDate |
2015 |
dc.date.none.fl_str_mv |
2015-06 |
dc.type.none.fl_str_mv |
info:eu-repo/semantics/article info:eu-repo/semantics/publishedVersion Articulo http://purl.org/coar/resource_type/c_6501 info:ar-repo/semantics/articulo |
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http://sedici.unlp.edu.ar/handle/10915/130827 |
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eng |
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