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Sci Rep ; 8(1): 1150, 2018 01 18.
Artigo em Inglês | MEDLINE | ID: mdl-29348586

RESUMO

Disulfides from Allium stipitatum, commonly known as Persian shallot, were previously reported to possess antibacterial properties. Analogues of these compounds, produced by S-methylthiolation of appropriate thiols using S-methyl methanethiosulfonate, exhibited antimicrobial activity, with one compound inhibiting the growth of Mycobacterium tuberculosis at 17 µM (4 mg L-1) and other compounds inhibiting Escherichia coli and multi-drug-resistant (MDR) Staphylococcus aureus at concentrations ranging between 32-138 µM (8-32 mg L-1). These compounds also displayed moderate inhibitory effects on Klebsiella and Proteus species. Whole-cell phenotypic bioassays such as the spot-culture growth inhibition assay (SPOTi), drug efflux inhibition, biofilm inhibition and cytotoxicity assays were used to evaluate these compounds. Of particular note was their ability to inhibit mycobacterial drug efflux and biofilm formation, while maintaining a high selectivity towards M. tuberculosis H37Rv. These results suggest that methyl disulfides are novel scaffolds which could lead to the development of new drugs against tuberculosis (TB).


Assuntos
Allium/química , Antituberculosos/farmacologia , Biofilmes/efeitos dos fármacos , Dissulfetos/farmacologia , Genes MDR/efeitos dos fármacos , Mycobacterium tuberculosis/efeitos dos fármacos , Antituberculosos/química , Antituberculosos/isolamento & purificação , Biofilmes/crescimento & desenvolvimento , Dissulfetos/química , Dissulfetos/isolamento & purificação , Escherichia coli/efeitos dos fármacos , Escherichia coli/crescimento & desenvolvimento , Klebsiella/efeitos dos fármacos , Klebsiella/crescimento & desenvolvimento , Testes de Sensibilidade Microbiana , Mycobacterium tuberculosis/crescimento & desenvolvimento , Extratos Vegetais/química , Proteus/efeitos dos fármacos , Proteus/crescimento & desenvolvimento , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus aureus/crescimento & desenvolvimento
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