Production of More Potent Anti-Candida Labdane Diterpenes by Biotransformation Using Cunninghamella elegans

Autor(es)

Sousa, Ingrid P. ; De Sousa Teixeira, Maria, V ; Freitas, Jolindo A. ; Ferreira, Antonio G. ; Pires, Loren M. ; Santos, Raquel A. ; Gomes Heleno, Vladimir Constantino ; Cardoso Furtado, Niege A. Jacometti

• Tipo de documento: Artigo Científico
• Fonte: CHEMISTRY & BIODIVERSITY; v. 19, n. 3, p. 9-pg., 2022-02-19.

Resumo

Candida species are responsible for causing invasive candidiasis with high mortality rate and their resistance to available antifungal drugs is a major clinical challenge. Biotransformation process of the labdane diterpene ent-labd-8(17)-en-15,18-dioic acid (1) carried out with Cunninghamella elegans afforded five new derivatives (compounds 2-6). Unusual regioselective hydroxylation of the methyl group at the C-20 position of labdane-type diterpene was achieved and all compounds were subjected to cytotoxicity and antifungal evaluations. Compound 1 and its derivatives were not cytotoxic to normal (MCF-10A) and tumor (MCF-7) cell lines. Compounds 2 and 3 exhibited fungistatic activity against all tested Candida strains at lower concentrations than fluconazole. Both compounds also showed the strongest fungicidal activity against C. albicans, which is the most prevalent fungal agent involved in candidemia. (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