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Memórias do Instituto Oswaldo Cruz
Fundação Oswaldo Cruz, Fiocruz
ISSN: 1678-8060 EISSN: 1678-8060
Vol. 111, No. 11, 2016, pp. 707-711
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Bioline Code: oc16113
Full paper language: English
Document type: Short Communication
Document available free of charge
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Memórias do Instituto Oswaldo Cruz, Vol. 111, No. 11, 2016, pp. 707-711
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Up-regulation of ATP-binding cassette transporters in the THP-1 human macrophage cell line by the antichagasic benznidazole
Perdomo, Virginia G; Rigalli, Juan P; Luquita, Marcelo G; Pellegrino, José M; Ruiz, María Laura & Catania, Viviana A
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.
Keywords
ABC transporters; benznidazole; macrophage cells
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