Cytotoxicity of lapachol metabolites produced by probiotics

Author(s)

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]

Affiliation

^[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

• Document type: Journal article
• Source: Letters in Applied Microbiology; v. 59, n. 1, p. 108-114, JUL 2014.
• Web of Science Citations: 11

Abstract

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)

• FAPESP's process: 11/21700-5 - The use of bacteria from gastrointestinal tract and filamentous fungi for biotransformation studies of naphthoquinones
• Grantee: Niege Araçari Jacometti Cardoso Furtado
• Support Opportunities: Regular Research Grants
• FAPESP's process: 09/51812-0 - Development of a platform for the study of in vitro and in vivo metabolism of natural products, a need for pre-clinical testing system
• Grantee: Norberto Peporine Lopes
• Support Opportunities: BIOTA-FAPESP Program - Thematic Grants