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(Referência obtida automaticamente do Web of Science, por meio da informação sobre o financiamento pela FAPESP e o número do processo correspondente, incluída na publicação pelos autores.)

Cytotoxicity of lapachol metabolites produced by probiotics

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Autor(es):
Oliveira Silva, E. [1] ; Cruz de Carvalho, T. [1] ; Parshikov, I. A. [2] ; Alves dos Santos, R. [3] ; Silva Emery, F. [1] ; Jacometti Cardoso Furtado, N. A. [1]
Número total de Autores: 6
Afiliação do(s) autor(es):
[1] Univ Sao Paulo, Fac Ciencias Farmaceut Ribeirao Preto, BR-14040903 Ribeirao Preto - Brazil
[2] Russian Acad Sci, Inst Appl Mech, Moscow - Russia
[3] Univ Franca, Nucleo Pesquisas Ciencias Exatas & Tecnol, Franca - Brazil
Número total de Afiliações: 3
Tipo de documento: Artigo Científico
Fonte: Letters in Applied Microbiology; v. 59, n. 1, p. 108-114, JUL 2014.
Citações Web of Science: 11
Resumo

Probiotics are currently added to a variety of functional foods to provide health benefits to the host and are commonly used by patients with gastrointestinal complaints or diseases. The therapeutic effects of lapachol continue to inspire studies to obtain derivatives with improved bioactivity and lower unwanted effects. Therefore, the general goal of this study was to show that probiotics are able to convert lapachol and are important to assess the effects of bacterial metabolism on drug performance and toxicity. The microbial transformations of lapachol were carried out by Bifidobacterium sp. and Lactobacillus acidophilus and different metabolites were produced in mixed and isolated cultures. The cytotoxic activities against breast cancer and normal fibroblast cell lines of the isolated metabolites (4-hydroxy-2,2-dimethyl-5-oxo-2,3,4,4,5,9-hexahydroindeno{[}1,2-]pyran-9 -carboxilic acid, a new metabolite produced by mixed culture and dehydro--lapachone produced by isolated cultures) were assessed and compared with those of lapachol. The new metabolite displayed a lower activity against a breast cancer cell line (IC50=532 center dot 7moll-1) than lapachol (IC50=72 center dot 3moll-1), while dehydro--lapachone (IC50=10 center dot 4moll-1) displayed a higher activity than lapachol. The present study is the first to demonstrate that probiotics are capable of converting lapachol into the most effective cytotoxic compound against a breast cancer cell line. (AU)

Processo FAPESP: 11/21700-5 - Utilização de bactérias do trato gastrointestinal e fungos filamentosos para estudos de biotransformação de naftoquinonas
Beneficiário:Niege Araçari Jacometti Cardoso Furtado
Linha de fomento: Auxílio à Pesquisa - Regular
Processo FAPESP: 09/51812-0 - Desenvolvimento de uma plataforma para o estudo do metabolismo in vivo e in vitro de produtos naturais, uma necessidade para o sistema de ensaios pré-clínicos
Beneficiário:Norberto Peporine Lopes
Linha de fomento: Auxílio à Pesquisa - Programa BIOTA - Temático