Autor(es):
Ferreira, Maria do Perpétuo Socorro Borges Carriço ; Cardoso, M. F.C. ; Silva, F. C. da ; Ferreira, V?tor Francisco ; Lima, Emerson Silva ; Souza, João Vicente Braga de
Data: 2020
Origem: Oasisbr
Assunto(s): Ergosterol; Naphthoquinone; Perchloric Acid; Sorbitol; (naphtho[2,3 D]furan 5,10 Dione) Dione; 1,4 Naphthoquinone Derivative; 2,2 Dimethyl 2,3 Dihydronaphtho[1,2 B]furan 4,5 Dione; 2,2 Dimethyl 2,3 Dihydronaphtho[2,3 B]furan 4,9 Dione; 3a,10b Dihydro 1h Cyclopenta; 7,9a Dihydro 6bh Cyclopenta; Amphotericin B; Antifungal Agent; Naphtho[2,1 D]furan 5,6 Dione; Perchloric Acid; Unclassified Drug; Anti-fungal Activity; Arthroderma Gypseum; Aspergillus; Atomic Absorption; Broth Dilution; Candida Albicans; Candida Parapsilosis; Cell Membrane Permeability; Controlled Study; Cryptococcus; Cryptococcus Gattii; Cryptococcus Neoformans; Dermatophyte; Filamentous Fungus; Fungal Cell Wall; Fungal Membrane; Fusarium; Microsporum Canis; Minimum Inhibitory Concentration; Nonhuman; Potassium Transport; Candida Albicans; Cytolysis Assay; Fungal Cell; Yeast; Antifungal Agents; Cell Membrane Permeability; Fungi; Humans; Microbial Sensitivity Tests; Mycoses; Naphthoquinones
Descrição
This study evaluated the antifungal activities of synthetic naphthoquinones against opportunistic and dermatophytic fungi and their preliminary mechanisms of action. The minimum inhibitory concentrations (MICs) of four synthetic naphthoquinones for 89 microorganisms, including opportunistic yeast agents, dermatophytes and opportunistic filamentous fungi, were determined. The compound that exhibited the best activity was assessed for its action against the cell wall (sorbitol test), for interference associated with ergosterol interaction, for osmotic balance (K+ efflux) and for membrane leakage of substances that absorb at the wavelength of 260 nm. All tested naphthoquinones exhibited antifungal activity, and compound IVS320 (3a,10b-dihydro-1H-cyclopenta [b] naphtho [2,3-d] furan-5,10-dione)-dione) demonstrated the lowest MICs across the tested species. The MIC of IVS320 was particularly low for dermatophytes (values ranging from 5-28 μg/mL) and Cryptococcus spp. (3-5 μg/mL). In preliminary mechanism-of-action tests, IVS320 did not alter the fungal cell wall but did cause problems in terms of cell membrane permeability (efflux of K+ and leakage of substances that absorb at 260 nm). This last effect was unrelated to ergosterol interactions with the membrane. © 2014 Ferreira et al.
