| Texto completo | |
| Autor(es): |
de Sousa, Ingrid Pontes
;
Ferreira, Antonio Gilberto
;
Miller Crotti, Antonio Eduardo
;
dos Santos, Raquel Alves
;
Kiermaier, Josef
;
Kraus, Birgit
;
Heilmann, Joerg
;
Jacometti Cardoso Furtado, Niege Aracari
Número total de Autores: 8
|
| Tipo de documento: | Artigo Científico |
| Fonte: | BIOORGANIC CHEMISTRY; v. 95, p. 8-pg., 2020-01-01. |
| Resumo | |
Candida glabrata, the most common non-albicans Candida species and one of the primary causes of candidemia, exhibits decreased susceptibility to azoles and more recently to echinocandins. Polyalthic acid 1, a furan diterpene, has been shown promising biological potential and in this study ent-polyalthic acid derivatives with antifungal activity against Candida glabrata were produced by microbial transformation. Incubation of 1 with Aspergillus brasiliensis afforded two known (compounds 5 and 10) and eight new derivatives (compounds 2-4, 6-9 and 11). The most common reaction was hydroxylation, but isomerization of the double bond and acetylation were also detected. None of the tested compounds showed cytotoxicity against HeLa, MCF-7 and MCF-10A cell lines showing IC50 values ranging from 62.6 mu M to > 500 mu M. Compounds 1, 5, 6, 8 and 11 showed fungistatic effects (ranging from 34.1 mu M to 39.5 mu M) on C. glabrata at lower concentrations than fluconazole (163.2 mu M). Compounds 1, 6 and 8 were more potent fungicides (ranging from 79.0 to 143.6 mu M) than fluconazole, which showed fungicidal effect at concentrations higher than 163.2 mu M. These results suggest that ent-polyalthic acid and some of its derivatives could be used as lead compounds to develop new antifungal agents. (AU) | |
| Processo FAPESP: | 11/13630-7 - Validação química e farmacológica de extratos e princípios ativos de espécies de Copaifera |
| Beneficiário: | Jairo Kenupp Bastos |
| Modalidade de apoio: | Auxílio à Pesquisa - Temático |
| Processo FAPESP: | 16/25201-7 - Estudos de bioacessibilidade, transporte intestinal e biotransformação in vitro dos ácidos ent-hardwickiico e ent-poliáltico das oleorresinas de Copaifera pubiflora e Copaifera duckei |
| Beneficiário: | Niege Araçari Jacometti Cardoso Furtado |
| Modalidade de apoio: | Auxílio à Pesquisa - Regular |