Up-regulation of ATP-binding cassette transporters in the THP-1 human macrophage cell line by the antichagasic benznidazole.
Mem Inst Oswaldo Cruz
; 111(11): 707-711, 2016 Nov.
Article
em En
| MEDLINE
| ID: mdl-27783718
ABSTRACT
The effect of benznidazole (BZL) on the expression and activity of P-glycoprotein (P-gp, ABCB1) and multidrug resistance-associated protein 2 (MRP2, ABCC2), the two major transporters of endogenous and exogenous compounds, was evaluated in differentiated THP-1 cells. BZL induced P-gp and MRP2 proteins in a concentration-dependent manner. The increase in mRNA levels of both transporters suggests transcriptional regulation. P-gp and MRP2 activities correlated with increased protein levels. BZL intracellular accumulation was significantly lower in BZL-pre-treated cells than in control cells. PSC833 (a P-gp inhibitor) increased the intracellular BZL concentration in both pre-treated and control cells, confirming P-gp participation in BZL efflux.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Tripanossomicidas
/
Doença de Chagas
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Membro 1 da Subfamília B de Cassetes de Ligação de ATP
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Transportadores de Cassetes de Ligação de ATP
/
Macrófagos
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Nitroimidazóis
Limite:
Humans
Idioma:
En
Revista:
Mem Inst Oswaldo Cruz
Ano de publicação:
2016
Tipo de documento:
Article
País de afiliação:
Argentina