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J Biomol Screen ; 12(2): 248-54, 2007 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-17259590

RESUMO

Cryopreserved, transiently transfected HepG2 cells were compared to freshly transfected HepG2 cells for use in a pregnane X receptor (PXR) transactivation assay. Assay performance was similar for both cell preparations; however, cryopreserved cells demonstrated less interassay variation. Validation with drugs of different PXR activation potencies and efficacies demonstrated an excellent correlation (r(2) > 0.95) between cryopreserved and fresh cells. Cryopreservation did not change the effect of known CYP3A4 inducers that have poor cell permeability, indicating that cryopreservation had little effect on membrane permeability. In addition, cryopreserved HepG2 cells did not exhibit enhanced susceptibility to cytotoxic compounds compared to transiently transfected control cells. The use of cryopreserved cells enables this assay to run with enhanced efficiency.


Assuntos
Bioensaio/métodos , Criopreservação/métodos , Preparações Farmacêuticas/metabolismo , Receptores de Esteroides/metabolismo , Ativação Transcricional , Células CACO-2 , Carcinoma Hepatocelular/patologia , Linhagem Celular Tumoral , Permeabilidade da Membrana Celular/efeitos dos fármacos , Efeitos Colaterais e Reações Adversas Relacionados a Medicamentos , Humanos , Neoplasias Hepáticas/patologia , Mifepristona/metabolismo , Mifepristona/farmacologia , Receptor de Pregnano X , Receptores de Esteroides/agonistas , Receptores de Esteroides/antagonistas & inibidores , Reprodutibilidade dos Testes , Rifampina/metabolismo , Rifampina/farmacologia , Sulfimpirazona/metabolismo , Sulfimpirazona/farmacologia , Transfecção
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