Up-regulation of ATP-binding cassette transporters in the THP-1 human macrophage cell line by the antichagasic benznidazole
| Autor: | Virginia Gabriela Perdomo, Marcelo G. Luquita, María Laura Ruiz, Viviana A. Catania, José M. Pellegrino, Juan Pablo Rigalli |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
Microbiology (medical) lcsh:Arctic medicine. Tropical medicine macrophage cells ATP Binding Cassette Transporter Subfamily B lcsh:RC955-962 Short Communication 030106 microbiology lcsh:QR1-502 ATP-binding cassette transporter Endogeny Biology lcsh:Microbiology Cell Line 03 medical and health sciences medicine Humans THP1 cell line Chagas Disease ATP Binding Cassette Transporter Subfamily B Member 1 ATP Binding Cassette Transporter Subfamily B Member 2 benznidazole Multidrug resistance-associated protein 2 Macrophages Transporter Trypanocidal Agents Multidrug Resistance-Associated Protein 2 Cell biology Up-Regulation Biochemistry ABC transporters Benznidazole Nitroimidazoles ATP-Binding Cassette Transporters Efflux Multidrug Resistance-Associated Proteins Intracellular medicine.drug |
| Zdroj: | Memórias do Instituto Oswaldo Cruz Memórias do Instituto Oswaldo Cruz, Volume: 111, Issue: 11, Pages: 707-711, Published: 24 OCT 2016 Memórias do Instituto Oswaldo Cruz., Vol 111, Iss 11, Pp 707-711 |
| ISSN: | 1678-8060 0074-0276 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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