Validation of in vitro methods for human cytochrome P450 enzyme induction: Outcome of a multi-laboratory study.
CYP induction
HepaRG
human hepatocytes
in vitro hepatic system
metabolism
validation
Journal
Toxicology in vitro : an international journal published in association with BIBRA
ISSN: 1879-3177
Titre abrégé: Toxicol In Vitro
Pays: England
ID NLM: 8712158
Informations de publication
Date de publication:
Oct 2019
Oct 2019
Historique:
received:
06
03
2019
accepted:
29
05
2019
pubmed:
4
6
2019
medline:
25
1
2020
entrez:
4
6
2019
Statut:
ppublish
Résumé
CYP enzyme induction is a sensitive biomarker for phenotypic metabolic competence of in vitro test systems; it is a key event associated with thyroid disruption, and a biomarker for toxicologically relevant nuclear receptor-mediated pathways. This paper summarises the results of a multi-laboratory validation study of two in vitro methods that assess the potential of chemicals to induce cytochrome P450 (CYP) enzyme activity, in particular CYP1A2, CYP2B6, and CYP3A4. The methods are based on the use of cryopreserved primary human hepatocytes (PHH) and human HepaRG cells. The validation study was coordinated by the European Union Reference Laboratory for Alternatives to Animal Testing of the European Commission's Joint Research Centre and involved a ring trial among six laboratories. The reproducibility was assessed within and between laboratories using a validation set of 13 selected chemicals (known human inducers and non-inducers) tested under blind conditions. The ability of the two methods to predict human CYP induction potential was assessed. Chemical space analysis confirmed that the selected chemicals are broadly representative of a diverse range of chemicals. The two methods were found to be reliable and relevant in vitro tools for the assessment of human CYP induction, with the HepaRG method being better suited for routine testing. Recommendations for the practical application of the two methods are proposed.
Identifiants
pubmed: 31158489
pii: S0887-2333(19)30010-4
doi: 10.1016/j.tiv.2019.05.019
pmc: PMC6718736
pii:
doi:
Substances chimiques
Cytochrome P-450 Enzyme Inducers
0
Cytochrome P-450 Enzyme System
9035-51-2
Types de publication
Journal Article
Validation Study
Langues
eng
Sous-ensembles de citation
IM
Pagination
212-228Informations de copyright
Copyright © 2019 European Commission. Published by Elsevier Ltd.. All rights reserved.
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