Evaluation of hypoxia inducible factor targeting pharmacological drugs as antileishmanial agents
| Autor: | Myriam Janeth Salazar Terreros, Solange dos Santos Costa, Adriana Degrossoli, Marina Dal'Bó Pelegrini, Selma Giorgio, Juliana Biar Pereira |
|---|---|
| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
Stimulation Echinomycin Resveratrol Pharmacology Parasite load Hypoxia inducible factor 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Macrophage Mimosine Leishmaniosis Medicine(all) biology General Medicine Leishmania biology.organism_classification 030104 developmental biology chemistry Hypoxia-inducible factors CdCl2 030220 oncology & carcinogenesis |
| Zdroj: | Asian Pacific journal of tropical medicine. 9(7) |
| ISSN: | 2352-4146 |
| Popis: | Objective To evaluate whether hypoxia inducible factor (HIF-1α) targeting pharmacological drugs, echinomycin, resveratrol and CdCl 2 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 CdCl 2 reduced the parasite load [IC 50 , (27.3 ± 2.25) μM and (24.8 ± 0.95) μM, respectively]. The IC 50 value of echinomycin was (22.7 ± 7.36) nM and mimosine did not alter the parasite load in primary macrophages. The macrophage viability IC 50 values for resveratrol, echinomycin and CdCl 2 and mimosine were >40 μM, >100 nM, >200 μM and>2 000 μM, respectively. In vivo no differences between cutaneous lesions from control, resveratrol- and echinomycin-treated Balb/c mice were detected. Conclusions Resveratrol, echinomycin and CdCl 2 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|