2018
DOI: 10.1590/0074-02760170345
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In vitro evaluation of the anti-leishmanial activity and toxicity of PK11195

Abstract: BACKGROUNDLeishmaniasis, one of the most neglected diseases, is a serious public health problem in many countries, including Brazil. Currently available treatments require long-term use and have serious side effects, necessitating the development of new therapeutic interventions. Because translocator protein (TSPO) levels are reduced in Leishmania amazonensis-infected cells and because this protein participates in apoptosis and immunomodulation, TSPO represents a potential target for Leishmania chemotherapy. T… Show more

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Cited by 7 publications
(5 citation statements)
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“…We found that this mitochondrial transmembrane protein exhibited a lower relative abundance of peptides in cells infected with L. amazonensis in comparison to L. major (Menezes et al, 2013 ). Modulating TSPO with one of its ligand, PK11195, caused the killing of amastigotes in vitro at dosages considered non-toxic to macrophages, indicating its potential as antileishmanial (Guedes et al, 2018 ). In sum, these findings strengthen the potentiality of global analysis of Leishmania -infected macrophages for the identification of biomarkers in host cells that probably participate in the pathogenesis of Leishmania infection and, subsequently, can function as targets for therapeutic intervention.…”
Section: Proteomic Contribution To Understanding the Macrophage Respomentioning
confidence: 99%
“…We found that this mitochondrial transmembrane protein exhibited a lower relative abundance of peptides in cells infected with L. amazonensis in comparison to L. major (Menezes et al, 2013 ). Modulating TSPO with one of its ligand, PK11195, caused the killing of amastigotes in vitro at dosages considered non-toxic to macrophages, indicating its potential as antileishmanial (Guedes et al, 2018 ). In sum, these findings strengthen the potentiality of global analysis of Leishmania -infected macrophages for the identification of biomarkers in host cells that probably participate in the pathogenesis of Leishmania infection and, subsequently, can function as targets for therapeutic intervention.…”
Section: Proteomic Contribution To Understanding the Macrophage Respomentioning
confidence: 99%
“…Before proceeding with in vitro experiments, we first assessed the potential cytotoxicity of PK11195 and D-DPA via cell viability measurements. BV2 murine microglia were exposed to PK11195 or D-DPA over a concentration range of 1–1000 μg/mL for 24 h. Consistent with previous in vitro studies, , PK11195 demonstrated significant dose-dependent toxicity, with the 1000 μg/mL dose reducing cell viability to ∼5% of controls (Figure S22). In contrast, D-DPA exhibited significantly less cytotoxicity ( p < 0.0001 PK11195 vs D-DPA), with the 1000 μg/mL dose exhibiting ∼60% cell viability.…”
Section: Resultsmentioning
confidence: 99%
“…Reading was performed in the spectrophotometer at wavelengths of 570 and 600 nm. The percentage of axenic culture inhibition was determined based on the untreated control (Guedes et al 2018).…”
Section: Antileishmanial Activitymentioning
confidence: 99%