Caco-2 cells cytotoxicity of nifuroxazide derivatives with potential activity against Methicillin-resistant Staphylococcus aureus (MRSA)

Autor(es)

Fernandes, Mariane B. ^[1] ; Goncalves, Jose E. ^[1] ; Scotti, Marcus T. ^[2] ; de Oliveira, Alex A. ^[3] ; Tavares, Leoberto C. ^[3] ; Storpirtis, Silvia ^[1]

Afiliação do(s) autor(es)

^[1] Univ Sao Paulo, Dept Pharm, Fac Pharmaceut Sci, BR-05508900 Sao Paulo - Brazil

^[2] Univ Fed Paraiba, Ctr Appl Sci & Educ, BR-58297000 Rio Tinto - Brazil

^[3] Univ Sao Paulo, Fac Pharmaceut Sci, Chem & Pharmaceut Technol Dept, BR-05508900 Sao Paulo - Brazil

• Tipo de documento: Artigo Científico
• Fonte: TOXICOLOGY IN VITRO; v. 26, n. 3, p. 535-540, APR 2012.
• Citações Web of Science: 7

Resumo

It is important to determine the toxicity of compounds and co-solvents that are used in cell monolayer permeability studies to increase confidence in the results obtained from these in vitro experiments. This study was designed to evaluate the cytotoxicity of new nifuroxazide derivatives with potential activity against Methicillin-resistant Staphylococcus aureus (MRSA) in Caco-2 cells to select analogues for further in vitro permeability analyses. In this study, nitrofurantoin and nifuroxazide, in addition to 6 furanic and 6 thiophenic nifuroxazide derivatives were tested at 2, 4, 6, 8 and 10 mu g/mL. In vitro cytotoxicity assays were performed according to the MTT (methyl tetrazolium) assay protocol described in ISO 10993-5. The viability of treated Caco-2 cells was greater than 83% for all tested nitrofurantoin concentrations, while those treated with nifuroxazide at 2, 4 and 6 mu g/mL had viabilities greater than 70%. Treatment with the nifuroxazide analogues resulted in viability values greater than 70% at 2 and 4 mu g/mL with the exception of the thiophenic methyl-substituted derivative, which resulted in cell viabilities below 70% at all tested concentrations. Caco-2 cells demonstrated reasonable viability for all nifuroxazide derivatives, except the thiophenic methyl-substituted compound. The former were selected for further permeability studies using Caco-2 cells. (C) 2012 Elsevier Ltd. All rights reserved. (AU)

• Processo FAPESP: 10/07188-7 - Permeabilidade e citotoxicidade in vitro de derivados da nifuroxazida com atividade frente a cepas multirresistentes de Staphylococcus aureus empregando células CACO-2
• Beneficiário: Silvia Storpirtis
• Modalidade de apoio: Auxílio à Pesquisa - Regular