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Evaluation of hypoxia inducible factor targeting pharmacological drugs as antileishmanial agents. | LitMetric

Evaluation of hypoxia inducible factor targeting pharmacological drugs as antileishmanial agents.

Asian Pac J Trop Med

Department of Animal Biology, Biology Institute, Universidade Estadual de Campinas, Campinas, São Paulo, Brazil. Electronic address:

Published: July 2016

AI Article Synopsis

Article Abstract

Objective: To evaluate whether hypoxia inducible factor (HIF-1α) targeting pharmacological drugs, echinomycin, resveratrol and CdCl2 which inhibit HIF-1α stimulation, and mimosine, which enhances the stability of HIF-1α present antileishmanial properties.

Methods: The leishmanicidal effect of drugs was evaluated in mouse macrophages and Balb/c mouse model for cutaneous leishmaniosis.

Results: Resveratrol and CdCl2 reduced the parasite load [IC50, (27.3 ± 2.25) μM and (24.8 ± 0.95) μM, respectively]. The IC50 value of echinomycin was (22.7 ± 7.36) nM and mimosine did not alter the parasite load in primary macrophages. The macrophage viability IC50 values for resveratrol, echinomycin and CdCl2 and mimosine were >40 μM, >100 nM, >200 μM and>2000 μM, respectively. In vivo no differences between cutaneous lesions from control, resveratrol- and echinomycin-treated Balb/c mice were detected.

Conclusions: Resveratrol, echinomycin and CdCl2 reduce parasite survival in vitro. The HIF-1α targeting pharmacological drugs require further study to more fully determine their anti-Leishmania potential and their role in therapeutic strategies.

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Source
http://dx.doi.org/10.1016/j.apjtm.2016.05.018DOI Listing

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