Imidazolium salts as innovative agents against Leishmania amazonensis.
作者： Raísha Costa Martins , Gilson Pires Dorneles , Vivian Oliveira Nunes Teixeira , Ana Maria Antonello , Júlia Lacerda Couto
DOI: 10.1016/J.INTIMP.2018.07.038
关键词: Amastigote 、 Leishmaniasis 、 Pharmacology 、 Parasite hosting 、 Peripheral blood mononuclear cell 、 Reactive oxygen species 、 Cytotoxicity 、 Nitric oxide 、 Chemistry 、 Chloride
摘要: Abstract The available chemotherapeutic drugs for the treatment of leishmaniasis present problems relating to efficacy, emergence parasite resistance, and adverse effects cost. Azole antifungal have been repurposed this proposition but clinical response has variable. In sense, study assessed leishmanicidal immunomodulatory activities azoles-derived imidazolium salts (IS), being ionic imidazole-derived equivalents: 1-n-butyl-3-methylimidazolium chloride (C4MImCl), 1-n-decyl-3-methylimidazolium (C10MImCl), 1-n-hexadecyl-3-methylimidazolium (C16MImCl), methanesulfonate (C16MImMeS), bis(trifluoromethanesulfonyl)imide (C16MImNTf2) 1-methyl-3-n-octadecylimidazolium (C18MImCl). Promastigotes Leishmania amazonensis were incubated with IS at concentrations ranging from 0.1 100 μM, survival was monitored. on reactive oxygen species (ROS) production mitochondrial membrane potential promastigotes, as well cytotoxicity against peripheral blood mononuclear cells (PBMC) human erythrocytes determined. Besides, amastigotes nitric oxide also evaluated. inhibited growth showed potent activity promastigotes L. amazonensis. addition, induced dysfunction ROS in parasites, presented low PBMC erythrocytes. Furthermore, very concentration (0.5 μM), C18MImCl, C16MImMeS, C16MImCl, C10MImCl C16MImNTf2 able kill intramacrophage parasites levels 91.3, 100, 94.4, 95.3 35.6%, respectively. These results indicate that are promising candidates development
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