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Comp Immunol Microbiol Infect Dis ; 84: 101797, 2022 May.
Artigo em Inglês | MEDLINE | ID: mdl-35325685

RESUMO

Treatment of leishmaniasis by conventional synthetic compounds has faced a serious challenge worldwide. This study was performed to evaluate the effect and modes of action of aromatic Turmerone on the Leishmania major intra-macrophage amastigotes, the causative agent of zoonotic cutaneous leishmaniasis in the Old World. In the findings, the mean numbers of L. major amastigotes in macrophages were significantly decreased in exposure to Turmerone plus meglumine antimoniate (Glucantime®; MA) than MA alone, especially at 50 µg/mL. In addition, Turmerone demonstrated no cytotoxicity as the selectivity index (SI) was 21.1; while it induced significant apoptosis in a dose-dependent manner on L. major promastigotes. In silico molecular docking analyses indicated an affinity of Turmerone to IL-12, with the MolDock score of - 96.8 kcal/mol; which may explain the increased levels of Th1 cytokines and decreased level of IL-10. The main mechanism of action is more likely associated with stimulating a powerful antioxidant and promoting the immunomodulatory roles in the killing of the target organism.


Assuntos
Antiprotozoários , Leishmania major , Leishmaniose Cutânea , Compostos Organometálicos , Animais , Antioxidantes/farmacologia , Antiprotozoários/farmacologia , Antiprotozoários/uso terapêutico , Leishmaniose Cutânea/tratamento farmacológico , Leishmaniose Cutânea/veterinária , Meglumina/farmacologia , Meglumina/uso terapêutico , Antimoniato de Meglumina/farmacologia , Simulação de Acoplamento Molecular , Compostos Organometálicos/farmacologia , Compostos Organometálicos/uso terapêutico
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