Anti- Candida albicans Activity of Thiazolylhydrazone Derivatives in Invertebrate and Murine Models.

Autor:	Cruz LIB; Departamento de Microbiologia, Instituto de Ciências Biológicas, Universidade Federal de Minas Gerais, Avenida Presidente Antônio Carlos, 6627, Pampulha, Belo Horizonte-Minas Gerais 31270-901, Brasil. lanabarretocruz@gmail.com., Lopes LFF; Departamento de Microbiologia, Instituto de Ciências Biológicas, Universidade Federal de Minas Gerais, Avenida Presidente Antônio Carlos, 6627, Pampulha, Belo Horizonte-Minas Gerais 31270-901, Brasil. lafinamore@gmail.com., de Camargo Ribeiro F; Departamento de Biociências e Diagnóstico Bucal, Instituto de Ciência e Tecnologia de São José dos Campos-UNESP, Av. Francisco José Longe, 777, Jardim São Dimas, São José dos Campos-São Paulo 12245-000, Brasil. felipe_c_ribeiro@hotmail.com., de Sá NP; Departamento de Microbiologia, Instituto de Ciências Biológicas, Universidade Federal de Minas Gerais, Avenida Presidente Antônio Carlos, 6627, Pampulha, Belo Horizonte-Minas Gerais 31270-901, Brasil. niveasap@gmail.com.; Department of Molecular Genetics and Microbiology, Division of Infectious Diseases, Stony Brook University, 150 Life Science Building, Stony Brook, NY 11794, USA. niveasap@gmail.com., Lino CI; Departamento de Produtos Farmacêuticos, Faculdade de Farmácia, Universidade Federal de Minas Gerais, Belo Horizonte-Minas Gerais 31270-901, Brasil. inaciol@hotmail.com., Tharmalingam N; Division of Infectious Diseases, Rhode Island Hospital, Alpert Medical School, and Brown University, Providence, RI 02903, USA. nagendran_tharmaligam@brown.edu., de Oliveira RB; Departamento de Produtos Farmacêuticos, Faculdade de Farmácia, Universidade Federal de Minas Gerais, Belo Horizonte-Minas Gerais 31270-901, Brasil. renatabo.ufmg@gmail.com., Rosa CA; Departamento de Microbiologia, Instituto de Ciências Biológicas, Universidade Federal de Minas Gerais, Avenida Presidente Antônio Carlos, 6627, Pampulha, Belo Horizonte-Minas Gerais 31270-901, Brasil. carlrosa@icb.ufmg.br., Mylonakis E; Division of Infectious Diseases, Rhode Island Hospital, Alpert Medical School, and Brown University, Providence, RI 02903, USA. emylonakis@lifespan.org., Fuchs BB; Division of Infectious Diseases, Rhode Island Hospital, Alpert Medical School, and Brown University, Providence, RI 02903, USA. helen_fuchs@brown.edu., Johann S; Departamento de Microbiologia, Instituto de Ciências Biológicas, Universidade Federal de Minas Gerais, Avenida Presidente Antônio Carlos, 6627, Pampulha, Belo Horizonte-Minas Gerais 31270-901, Brasil. sjohann@icb.ufmg.br.
Jazyk:	angličtina
Zdroj:	Journal of fungi (Basel, Switzerland) [J Fungi (Basel)] 2018 Dec 12; Vol. 4 (4). Date of Electronic Publication: 2018 Dec 12.
DOI:	10.3390/jof4040134
Abstrakt:	Candidiasis is an opportunistic fungal infection with Candida albicans being the most frequently isolated species. Treatment of these infections is challenging due to resistance that can develop during therapy, and the limited number of available antifungal compounds. Given this situation, the aim of this study was to evaluate the antifungal activity of four thiazolylhydrazone compounds against C. albicans . Thiazolylhydrazone compounds 1 , 2 , 3 , and 4 were found to exert antifungal activity, with MICs of 0.125⁻16.0 μg/mL against C . albicans . The toxicity of the compounds was evaluated using human erythrocytes and yielded LC 50 > 64 μg/mL. The compounds were further evaluated using the greater wax moth Galleria mellonella as an in vivo model. The compounds prolonged larval survival when tested between 5 and 15 mg/kg, performing as well as fluconazole. Compound 2 was evaluated in murine models of oral and systemic candidiasis. In the oral model, compound 2 reduced the fungal load on the mouse tongue; and in the systemic model it reduced the fungal burden found in the kidney when tested at 10 mg/kg. These results show that thiazolylhydrazones are an antifungal towards C. albicans with in vivo efficacy.
Databáze:	MEDLINE
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