Efeito in vitro de complexo entre cetoconazol e ácido p-sulfônico calix[6]areno sobre Leishmania amazonensis e Leishmania infantum
Ano de defesa: | 2019 |
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Autor(a) principal: | |
Orientador(a): | |
Banca de defesa: | |
Tipo de documento: | Dissertação |
Tipo de acesso: | Acesso aberto |
Idioma: | por |
Instituição de defesa: |
Universidade Federal do Espírito Santo
BR Mestrado em Ciências Veterinárias Centro de Ciências Agrárias e Engenharias UFES Programa de Pós-Graduação em Ciências Veterinárias |
Programa de Pós-Graduação: |
Não Informado pela instituição
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Departamento: |
Não Informado pela instituição
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País: |
Não Informado pela instituição
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Palavras-chave em Português: | |
Link de acesso: | http://repositorio.ufes.br/handle/10/11217 |
Resumo: | Ketoconazole has been described as a leishmanicidal agent, however, the low aqueous solubility of the drug may limit its bioavailability and therapeutic efficacy. p-sulphonic acid calix[n]arene has been used to improve solubility and efficacy of drugs. The aim of this work was evaluate the in vitro effect of the ketoconazole/p-sulfonic acid calix[6]arene inclusion complex (CLX/CTZ) on promastigote forms of Leishmania amazonensis and Leishmania infantum, as well as their toxicity to DH82 macrophages. The leishmanicidal effect and toxicity of CLX/CTZ, pure ketoconazole (CTZ) and the physical mixture of the two compounds (PM) were evaluated by the resazurin method. The IC50 value of CLX/CTZ, CTZ and PM on the L. amazonensis promastigotes forms was 3.95, 14.35 and 13.87 µM; and in L. infantum was 6.74, 17.47 and 17.54 µM, respectively. The CLX/CTZ, CTZ and PM showed no toxicity to DH82 cells. CLX/CTZ has demonstrated higher leishmanicidal activity than CTZ and PM. CLX/CTZ also presented low toxicity to macrophages, representing a promising alternative for use in preclinical trials for leishmaniasis treatment. |