چکیده (انگلیسی):

Objective: To evaluate whether hypoxia inducible factor (HIF-1a) targeting pharmacological
drugs, echinomycin, resveratrol and CdCl2 which inhibit HIF-1a stimulation,
and mimosine, which enhances the stability of HIF-1a 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) mM and
(24.8 ± 0.95) mM, 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 mM, >100 nM, >200 mM and>2 000 mM, 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-1a targeting pharmacological drugs require further study to more fully determine
their anti-Leishmania potential and their role in therapeutic strategies.