RESUMO

Cryptococcosis is a fungal disease of global significance for which new effective treatments are needed. The conjugation of the synthetic antimicrobial peptide fragment UBI 31-38 to a coumarin derivative showed to be an effective approach for the design of a novel anticryptococcal agent. In addition to antifungal activity, the conjugate exhibited intense fluorescence, which could be valuable for mechanistic investigations of this molecule. In this work, we studied the photophysical properties of the conjugate and confocal scanning laser microscopy was used to inspect the distribution of the peptide-coumarin conjugate in Cryptococcus cell. The synergism of this compound with amphotericin B or fluconazole against C. gattii and C. neoformans strains was also investigated. The results indicated that the fluorescent conjugate alone as well as its combination with amphotericin B are promising tools against cryptococcosis.

Assuntos

Anfotericina B/farmacologia , Antifúngicos/farmacologia , Cumarínicos/farmacologia , Criptococose/tratamento farmacológico , Cryptococcus/efeitos dos fármacos , Fragmentos de Peptídeos/farmacologia , Anfotericina B/química , Antifúngicos/síntese química , Antifúngicos/química , Cumarínicos/química , Cryptococcus/citologia , Relação Dose-Resposta a Droga , Sinergismo Farmacológico , Humanos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Fragmentos de Peptídeos/síntese química , Fragmentos de Peptídeos/química , Processos Fotoquímicos , Relação Estrutura-Atividade