Claudia Ta Pires1, Regiane Bl Scodro2, Diógenes Ag Cortez3,4, Mislaine A Brenzan3, Vera Ld Siqueira1, Katiany R Caleffi-Ferracioli1, Lucas Cc Vieira5, Júlia L Monteiro6, Arlene G Corrêa6, Rosilene F Cardoso1,2. 1. Programa de Pós-Graduação em Biociências e Fisiopatologia, Universidade Estadual de Maringá, 87020-900 Maringá, Paraná, 87020-900, Brazil. 2. Programa de Pós-Graduação em Ciências da Saúde, Universidade Estadual de Maringá, Maringá, Paraná, 87020-900, Brazil. 3. Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Estadual de Maringá, Maringá, Paraná, 87020-900, Brazil. 4. Programa de Pós-Graduação em Promoção da Saúde, Unicesumar - Centro Universitário, Maringá, Paraná, 87050-390, Brazil. 5. Instituto de Engenharia, Universidade Federal de Mato Grosso, Cuiabá, Mato Grosso, 78060-900, Brazil. 6. Laboratório de Síntese de Produtos Naturais - LSPN, Departamento de Química, Universidade Federal de São Carlos, São Carlos, São Paulo, 13565-905, Brazil.
Abstract
Aim: Eight coumarin derivatives (1a-h) obtained from natural (-)-mammea A/BB (1) and 13 synthetic coumarins (2-14) had their cytotoxicity and biological activity evaluated against Mycobacterium tuberculosis H37Rv reference strain and multidrug-resistant clinical isolates. Materials & methods: Anti-M. tuberculosis activity was evaluated by resazurin microtiter assay plate, and the cytotoxicity of natural and synthetic products using J774A.1 macrophages by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide. Results: Compounds 1g, 5, 6, 12 and 14 were more active against M. tuberculosis H37Rv and multidrug-resistant clinical isolates with MIC values ranging from 15.6 to 62.5 μg/ml. Conclusion: These results demonstrate that the coumarin derivatives were active against multidrug-resistant clinical isolates, becoming potential candidates to be used in the treatment of resistant tuberculosis.
Aim: Eight coumarin derivatives (1a-h) obtained from natural (-)-mammea A/BB (1) and 13 synthetic coumarins (2-14) had their cytotoxicity and biological activity evaluated against Mycobacterium tuberculosis H37Rv reference strain and multidrug-resistant clinical isolates. Materials & methods: Anti-M. tuberculosis activity was evaluated by resazurin microtiter assay plate, and the cytotoxicity of natural and synthetic products using J774A.1 macrophages by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide. Results: Compounds 1g, 5, 6, 12 and 14 were more active against M. tuberculosis H37Rv and multidrug-resistant clinical isolates with MIC values ranging from 15.6 to 62.5 μg/ml. Conclusion: These results demonstrate that the coumarin derivatives were active against multidrug-resistant clinical isolates, becoming potential candidates to be used in the treatment of resistant tuberculosis.
Entities:
Keywords:
Mycobacterium tuberculosis; SAR study; coumarin