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A novel naphthoquinone derivative shows selective antifungal activity against Sporothrix yeasts and biofilms.
Borba-Santos, Luana P; Nicoletti, Caroline Deckmann; Vila, Taissa; Ferreira, Patricia Garcia; Araújo-Lima, Carlos Fernando; Galvão, Bárbara Verena Dias; Felzenszwalb, Israel; de Souza, Wanderley; de Carvalho da Silva, Fernando; Ferreira, Vitor Francisco; Futuro, Debora Omena; Rozental, Sonia.
Affiliation
  • Borba-Santos LP; Laboratório de Biologia Celular de Fungos, Instituto de Biofísica Carlos Chagas Filho, Universidade Federal do Rio de Janeiro, RJ, Rio de Janeiro, Brazil. luanaborba@biof.ufrj.br.
  • Nicoletti CD; Departamento de Tecnologia Farmacêutica, Faculdade de Farmácia, Universidade Federal Fluminense, Niteroi, RJ, Brazil.
  • Vila T; Laboratório de Biologia Celular de Fungos, Instituto de Biofísica Carlos Chagas Filho, Universidade Federal do Rio de Janeiro, RJ, Rio de Janeiro, Brazil.
  • Ferreira PG; Departamento de Tecnologia Farmacêutica, Faculdade de Farmácia, Universidade Federal Fluminense, Niteroi, RJ, Brazil.
  • Araújo-Lima CF; Laboratório de Mutagênese Ambiental, Departamento de Biofísica e Biometria, Universidade Do Estado Do Rio de Janeiro, RJ, Rio de Janeiro, Brazil.
  • Galvão BVD; Laboratório de Mutagênese Ambiental, Departamento de Biofísica e Biometria, Universidade Do Estado Do Rio de Janeiro, RJ, Rio de Janeiro, Brazil.
  • Felzenszwalb I; Laboratório de Mutagênese Ambiental, Departamento de Biofísica e Biometria, Universidade Do Estado Do Rio de Janeiro, RJ, Rio de Janeiro, Brazil.
  • de Souza W; Laboratório de Ultraestrutura Celular Hertha Meyer, Instituto de Biofísica Carlos Chagas Filho, Universidade Federal do Rio de Janeiro, RJ, Rio de Janeiro, Brazil.
  • de Carvalho da Silva F; Departamento de Química Orgânica, Instituto de Química, Universidade Federal Fluminense, Niteroi, RJ, Brazil.
  • Ferreira VF; Departamento de Tecnologia Farmacêutica, Faculdade de Farmácia, Universidade Federal Fluminense, Niteroi, RJ, Brazil.
  • Futuro DO; Departamento de Tecnologia Farmacêutica, Faculdade de Farmácia, Universidade Federal Fluminense, Niteroi, RJ, Brazil.
  • Rozental S; Laboratório de Biologia Celular de Fungos, Instituto de Biofísica Carlos Chagas Filho, Universidade Federal do Rio de Janeiro, RJ, Rio de Janeiro, Brazil.
Braz J Microbiol ; 53(2): 749-758, 2022 Jun.
Article in En | MEDLINE | ID: mdl-35258797
ABSTRACT
Sporotrichosis is a subcutaneous mycosis that affects humans and animals, with few therapeutic options available in the pharmaceutical market. We screened the in vitro antifungal activity of fourteen 1,4-naphthoquinones derivative compounds against Sporothrix brasiliensis and Sporothrix schenckii, the main etiological agents of sporotrichosis in Latin America. The most active compound was selected for further studies exploring its antibiofilm activity, effects on yeast morphophysiology, interaction with itraconazole, and selectivity to fungal cells. Among the fourteen 1,4-naphthoquinones tested, naphthoquinone 5, a silver salt of lawsone, was the most active compound. Naphthoquinone 5 was able to inhibit Sporothrix biofilms and induced ROS accumulation, mitochondrial disturbances, and severe plasmatic membrane damage in fungal cells. Furthermore, naphthoquinone 5 was ten times more selective towards fungal cells than fibroblast, and the combination of itraconazole with naphthoquinone 5 improved the inhibitory activity of the azole. Combined, the data presented here indicate that the silver salt naphthoquinone 5 exerts promising in vitro activity against the two main agents of sporotrichosis with important antibiofilm activity and a good toxicity profile, suggesting it is a promising molecule for the development of a new family of antifungals.
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Full text: 1 Database: MEDLINE Main subject: Sporotrichosis / Sporothrix / Naphthoquinones Limits: Animals Language: En Year: 2022 Type: Article

Full text: 1 Database: MEDLINE Main subject: Sporotrichosis / Sporothrix / Naphthoquinones Limits: Animals Language: En Year: 2022 Type: Article