Presence of benznidazole conjugated metabolites in urine identified by β-glucuronidase treatment

Chagas disease is a serious public health problem in Latin America and, due to migration, in other nonendemic regions. Benznidazole (BNZ) is first choice drug in pediatric therapeutics. However, little is known regarding its metabolism in humans. The aim of the study was to isolate and identify prod...

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Detalles Bibliográficos
Autores principales:	Marson, María Elena, García Bournissen, Facundo, Altcheh, Jaime, Moscatelli, Guillermo, Moroni, Samantha, Mastrantonio Garrido, Guido Enrique
Formato:	Articulo
Lenguaje:	Español
Publicado:	2020
Materias:	Química Benznidazole metabolites Chagas Disease/drug therapy Glucuronidase/urine High Performance Liquid Chromatography HPLC/methods Mass Spectrometry/ methods Antiparasitic agents/pharmacology
Acceso en línea:	http://sedici.unlp.edu.ar/handle/10915/121849
Aporte de:	SEDICI (UNLP) de Universidad Nacional de La Plata

id	I19-R120-10915-121849
record_format	dspace
institution	Universidad Nacional de La Plata
institution_str	I-19
repository_str	R-120
collection	SEDICI (UNLP)
language	Español
topic	Química Benznidazole metabolites Chagas Disease/drug therapy Glucuronidase/urine High Performance Liquid Chromatography HPLC/methods Mass Spectrometry/ methods Antiparasitic agents/pharmacology
spellingShingle	Química Benznidazole metabolites Chagas Disease/drug therapy Glucuronidase/urine High Performance Liquid Chromatography HPLC/methods Mass Spectrometry/ methods Antiparasitic agents/pharmacology Marson, María Elena García Bournissen, Facundo Altcheh, Jaime Moscatelli, Guillermo Moroni, Samantha Mastrantonio Garrido, Guido Enrique Presence of benznidazole conjugated metabolites in urine identified by β-glucuronidase treatment
topic_facet	Química Benznidazole metabolites Chagas Disease/drug therapy Glucuronidase/urine High Performance Liquid Chromatography HPLC/methods Mass Spectrometry/ methods Antiparasitic agents/pharmacology
description	Chagas disease is a serious public health problem in Latin America and, due to migration, in other nonendemic regions. Benznidazole (BNZ) is first choice drug in pediatric therapeutics. However, little is known regarding its metabolism in humans. The aim of the study was to isolate and identify products of human BZN metabolism in urine samples obtained from a pediatric Chagas patient and a healthy adult volunteer both treated with BZN. Urine samples were collected after dose of BNZ. Urine was treated with β-glucuronidase followed by an extraction procedure under two different pH conditions and a HPLC/UV and MS/MS identification of BZN and its metabolites. BZN (m/z 260.09847) was identified in all urine extracts. Peaks from each extracted chromatograms were selected for MS and MS/MS identification. Three compounds structurally related to BZN were identified: BZN-Na+ (m/z 283.08009), N-amine-BZN (m/z 230.12307) and N-hydroxi-amine-BZN (m/z 246.11702). BNZ-Na+ was identified in all extracts, but N-amine-BZN and N-hydroxi-amine-BZN were only observed in those extracts treated with β-glucuronidase. This is the first experimental report showing elimination of BZN N-reduced metabolites in urine. As they were released after treatment with β-glucuronidase it can be suggested that glucuronization plays a role in BNZ metabolism and renal elimination.
format	Articulo Articulo
author	Marson, María Elena García Bournissen, Facundo Altcheh, Jaime Moscatelli, Guillermo Moroni, Samantha Mastrantonio Garrido, Guido Enrique
author_facet	Marson, María Elena García Bournissen, Facundo Altcheh, Jaime Moscatelli, Guillermo Moroni, Samantha Mastrantonio Garrido, Guido Enrique
author_sort	Marson, María Elena
title	Presence of benznidazole conjugated metabolites in urine identified by β-glucuronidase treatment
title_short	Presence of benznidazole conjugated metabolites in urine identified by β-glucuronidase treatment
title_full	Presence of benznidazole conjugated metabolites in urine identified by β-glucuronidase treatment
title_fullStr	Presence of benznidazole conjugated metabolites in urine identified by β-glucuronidase treatment
title_full_unstemmed	Presence of benznidazole conjugated metabolites in urine identified by β-glucuronidase treatment
title_sort	presence of benznidazole conjugated metabolites in urine identified by β-glucuronidase treatment
publishDate	2020
url	http://sedici.unlp.edu.ar/handle/10915/121849
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bdutipo_str	Repositorios
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Presence of benznidazole conjugated metabolites in urine identified by β-glucuronidase treatment

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