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A new acridone with antifungal properties against Candida spp. and dermatophytes, and antibiofilm activity against C. albicans.
de Oliveira, D B C; Silva, L B; da Silva, B V; Borges, T C; Marques, B C; Dos Santos, M B; de Oliveira, L F; Bolzani, V S; Rodrigues, A R A; Regasini, L O; Andrade, A A.
Afiliación
  • de Oliveira DBC; Discipline of Microbiology, Institute of Biological and Natural Sciences, Federal University of Triângulo Mineiro (UFTM), Uberaba, Minas Gerais, Brazil.
  • Silva LB; Discipline of Microbiology, Institute of Biological and Natural Sciences, Federal University of Triângulo Mineiro (UFTM), Uberaba, Minas Gerais, Brazil.
  • da Silva BV; Discipline of Microbiology, Institute of Biological and Natural Sciences, Federal University of Triângulo Mineiro (UFTM), Uberaba, Minas Gerais, Brazil.
  • Borges TC; Discipline of Microbiology, Institute of Biological and Natural Sciences, Federal University of Triângulo Mineiro (UFTM), Uberaba, Minas Gerais, Brazil.
  • Marques BC; Laboratory of Green and Medicinal Chemistry, Department of Chemistry and Environmental Sciences, Institute of Biosciences, Humanities and Exact Sciences, São Paulo State University (UNESP), São José do Rio Preto, São Paulo, Brazil.
  • Dos Santos MB; Laboratory of Green and Medicinal Chemistry, Department of Chemistry and Environmental Sciences, Institute of Biosciences, Humanities and Exact Sciences, São Paulo State University (UNESP), São José do Rio Preto, São Paulo, Brazil.
  • de Oliveira LF; Discipline of Physiology, Institute of Biological and Natural Sciences, Federal University of Triângulo Mineiro (UFTM), Uberaba, Minas Gerais, Brazil.
  • Bolzani VS; Department of Organic Chemistry, Institute of Chemistry, São Paulo State University (UNESP), Araraquara, São Paulo, Brazil.
  • Rodrigues ARA; Discipline of Physiology, Institute of Biological and Natural Sciences, Federal University of Triângulo Mineiro (UFTM), Uberaba, Minas Gerais, Brazil.
  • Regasini LO; Laboratory of Green and Medicinal Chemistry, Department of Chemistry and Environmental Sciences, Institute of Biosciences, Humanities and Exact Sciences, São Paulo State University (UNESP), São José do Rio Preto, São Paulo, Brazil.
  • Andrade AA; Discipline of Microbiology, Institute of Biological and Natural Sciences, Federal University of Triângulo Mineiro (UFTM), Uberaba, Minas Gerais, Brazil.
J Appl Microbiol ; 127(5): 1362-1372, 2019 Nov.
Article en En | MEDLINE | ID: mdl-31297951
AIM: The increase in the number of fungal infections worldwide, coupled with the limitations of current antifungal chemotherapy, demand the development of safe and effective new antifungals. Here, we presented the synthesis of a novel acridone (M14) and its antifungal properties against Candida and dermatophytes species. METHODS AND RESULTS: A series of 17 acridones was designed, synthesized and tested for its antifungal activity. The minimum inhibitory concentration (MIC) was determined by the broth microdilution method. Only the acridone M14 showed growth-inhibitory activity against reference strains and clinical isolates of Candida and dermatophytes, with MIC range of 7·81-31·25 µg ml-1 . Moreover, M14 exhibited fungicidal activity and prevented biofilm formation by C. albicans as well as reduced the viability of preformed biofilms, even at sub-MICs. The confocal laser scanning microscopy analysis revealed that C. albicans hyphal growth was completely inhibited in the presence of M14. Similarly, there was a severe inhibition on hyphal growth of Trichophyton rubrum. We also found that M14 has relatively low toxicity to human fibroblasts. CONCLUSIONS: The new acridone M14 has antifungal properties against Candida spp. and dermatophytes, and antibiofilm activity against C. albicans. In addition, M14 is relatively selective to fungal cells compared to human normal cells. SIGNIFICANCE AND IMPACT OF THE STUDY: Because of its in vitro antifungal activity, anti-Candida biofilm effect and moderate cytotoxicity towards normal human cell, M14 may serve as a valuable lead compound to develop a new antifungal agent.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Candida / Biopelículas / Arthrodermataceae / Acridonas / Antifúngicos Límite: Humans Idioma: En Revista: J Appl Microbiol Asunto de la revista: MICROBIOLOGIA Año: 2019 Tipo del documento: Article País de afiliación: Brasil Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Candida / Biopelículas / Arthrodermataceae / Acridonas / Antifúngicos Límite: Humans Idioma: En Revista: J Appl Microbiol Asunto de la revista: MICROBIOLOGIA Año: 2019 Tipo del documento: Article País de afiliación: Brasil Pais de publicación: Reino Unido