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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Evaluation of the enantioselective in vitro metabolism of the chiral pesticide fipronil employing a human model: Risk assessment through in vitro-in vivo correlation and prediction of toxicokinetic parameters

Full text
Author(s):
Carrao, Daniel Blascke [1] ; dos Reis Gomes, Isabel Cristina [1] ; Barbosa Junior, Fernando [2] ; Moraes de Oliveira, Anderson Rodrigo [1]
Total Authors: 4
Affiliation:
[1] Univ Sao Paulo, Fac Filosofia Ciencias & Letras Ribeirao Preto, Dept Quim, Ave Bandeirantes 3900, BR-14040901 Ribeirao Preto, SP - Brazil
[2] Univ Sao Paulo, Fac Ciencias Farmaceut Ribeirao Preto, Lab Toxicol & Essencialidade Metais, Ave Bandeirantes 3900, BR-14049903 Ribeirao Preto, SP - Brazil
Total Affiliations: 2
Document type: Journal article
Source: Food and Chemical Toxicology; v. 123, p. 225-232, JAN 2019.
Web of Science Citations: 4
Abstract

The chiral pesticide fipronil is employed as a racemic mixture to control pests. Although there are no enantioselective differences in the fipronil enantiomer activities toward target organisms, fipronil enantiomers may exhibit enantioselective differences in their bioaccumulation, toxicity, and metabolism toward non-target organisms, including humans. The present work aims to provide significant reliable enantioselective information concerning fipronil risk assessment in humans. For that, the in vitro metabolism of rac-fipronil, S-fipronil, and R-fipronil by human liver microsomes was evaluated, the in vivo enantioselective toxicokinetic parameters were predicted and the main CYP450 isoforms involved in the enantioselective metabolism were determined. The obtained results demonstrated that fipronil may undergo a clearance by the liver and it is exclusively metabolized by the CYP3A4 isoform. Although no significative stereoselective differences were observed, the results provide reliable information on fipronil risk assessment for humans. (AU)

FAPESP's process: 16/07597-0 - Development of chromatographic/electrophoretic methods to be further used in in vitro enzymatic inhibition and drug interaction of chiral pesticides
Grantee:Anderson Rodrigo Moraes de Oliveira
Support type: Regular Research Grants
FAPESP's process: 14/50945-4 - INCT 2014: National Institute for Alternative Technologies of Detection, Toxicological Evaluation and Removal of Micropollutants and Radioactivies
Grantee:Maria Valnice Boldrin
Support type: Research Projects - Thematic Grants
FAPESP's process: 16/15680-5 - Enantioselective in vitro studies of metabolism, enzymatic inhibition and toxicity of the pesticide fipronil
Grantee:Daniel Blascke Carrão
Support type: Scholarships in Brazil - Doctorate
FAPESP's process: 18/07534-4 - Development of chromatographic / electrophoretic methods to be further applied in in vitro enzymatic inhibition studies and prediction of drug interactions of chiral pesticides - phase 2
Grantee:Anderson Rodrigo Moraes de Oliveira
Support type: Regular Research Grants