Identification of N-benzylacetamide as a major component of human plasmatic metabolic profiling of benznidazole

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 ris...

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Autores principales: Marson, María Elena, Altcheh, Jaime, Moscatelli, Guillermo, Moroni, Samanta, Garcia-Bournissen, Facundo, Mastrantonio Garrido, Guido Enrique
Formato: Articulo
Lenguaje:Inglés
Publicado: 2015
Materias:
Ciencias Exactas
Biología
Nitrocompounds
Benznidazole
N-benzylacetamide
Chagas disease
Metabolite
UPLC/MS/MS
Plasma
Pediatric pharmacology
Acceso en línea:http://sedici.unlp.edu.ar/handle/10915/130827
Aporte de:
SEDICI (UNLP) de Universidad Nacional de La Plata
id I19-R120-10915-130827
record_format dspace
institution Universidad Nacional de La Plata
institution_str I-19
repository_str R-120
collection SEDICI (UNLP)
language Inglés
topic Ciencias Exactas
Biología
Nitrocompounds
Benznidazole
N-benzylacetamide
Chagas disease
Metabolite
UPLC/MS/MS
Plasma
Pediatric pharmacology
spellingShingle Ciencias Exactas
Biología
Nitrocompounds
Benznidazole
N-benzylacetamide
Chagas disease
Metabolite
UPLC/MS/MS
Plasma
Pediatric pharmacology
Marson, María Elena
Altcheh, Jaime
Moscatelli, Guillermo
Moroni, Samanta
Garcia-Bournissen, Facundo
Mastrantonio Garrido, Guido Enrique
Identification of N-benzylacetamide as a major component of human plasmatic metabolic profiling of benznidazole
topic_facet Ciencias Exactas
Biología
Nitrocompounds
Benznidazole
N-benzylacetamide
Chagas disease
Metabolite
UPLC/MS/MS
Plasma
Pediatric pharmacology
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.
format Articulo
Articulo
author Marson, María Elena
Altcheh, Jaime
Moscatelli, Guillermo
Moroni, Samanta
Garcia-Bournissen, Facundo
Mastrantonio Garrido, Guido Enrique
author_facet Marson, María Elena
Altcheh, Jaime
Moscatelli, Guillermo
Moroni, Samanta
Garcia-Bournissen, Facundo
Mastrantonio Garrido, Guido Enrique
author_sort Marson, María Elena
title Identification of N-benzylacetamide as a major component of human plasmatic metabolic profiling of benznidazole
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
publishDate 2015
url http://sedici.unlp.edu.ar/handle/10915/130827
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