RESUMO
Gargantulide A (1), an extremely complex 52-membered macrolactone, was isolated from Streptomyces sp. A42983 and displayed moderate activity against MRSA. The planar structure of 1 was determined using 2D NMR, and its stereochemistry was partially established on the basis of NOESY correlations, J-based configuration analysis, and Kishi's universal NMR database.
Assuntos
Antibacterianos/isolamento & purificação , Antibacterianos/farmacologia , Macrolídeos/isolamento & purificação , Macrolídeos/farmacologia , Streptomyces/química , Antibacterianos/química , Candida albicans/efeitos dos fármacos , Clostridium/efeitos dos fármacos , Farmacorresistência Bacteriana/efeitos dos fármacos , Macrolídeos/química , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Saccharomyces cerevisiae/efeitos dos fármacos , Streptococcus pneumoniae/efeitos dos fármacos , Vancomicina/farmacologiaRESUMO
The root and stem bark extracts of a Nigerian sample of Leptonychia pubescens Keay (Sterculiaceae) were found to inhibit the serine protease tryptase, a potential therapeutic target for the treatment of asthma and chronic obstructive pulmonary disease (COPD). Bioassay-guided isolation led to the identification of 1-beta-ribofuranosylbrunfelsamidine as the active component with a tryptase IC (50) of 3 microM. Brunfelsamidine was also isolated, but was only weakly active.