RESUMO
The antimicrobial and antiproliferative activities of vulpinic acids (1 a, b, c) have been assayed in vitro. Activity was demonstrated by vulpinic acids on Gram-positive bacteria only. The MIC values of these compounds were found to be ranging from 3.8-31.5 micrograms/ml. The significance of these results is discussed.
Assuntos
Antibacterianos/farmacologia , Antineoplásicos/farmacologia , Furanos/farmacologia , Fenilacetatos/farmacologia , Animais , Divisão Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Camundongos , Testes de Sensibilidade Microbiana , Células Tumorais CultivadasRESUMO
The synthesis of N-salicyloyl-N-benzyl-thiourea and 2,2-dimethyl-4-oxo-6-methoxy-benzo-1,3-dioxin are described. They were studied for their antiviral, antiproliferative and antimicrobial activities in vitro. N-salicyloyl-N-benzyl-thiourea exhibited significant activity against Gram-positive bacteria and against influenza viruses types A/Philippine/H3N2, A/Chilli/H1N1 and B/Paraha, as well as against K562 cell proliferation. By contrast, no such activity was demonstrated by 2,2-dimethyl-4-oxo-6-methoxy-benzo-1,3-dioxin.
Assuntos
Anti-Infecciosos/síntese química , Dioxinas/síntese química , Salicilatos/síntese química , Antibacterianos , Anti-Infecciosos/farmacologia , Antivirais/síntese química , Divisão Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Dioxinas/farmacologia , Bactérias Gram-Positivas/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Salicilatos/farmacologia , Espectrofotometria Infravermelho , Espectrofotometria Ultravioleta , Células Tumorais Cultivadas , Ensaio de Placa Viral , Vírus/efeitos dos fármacosRESUMO
Chlorhexidine (0.5-0.65 microM) and Triton X45 (30-40 microM) added to exponential phase Bacillus megaterium KM- cultures was growth inhibitory. The presence of KCl (0.05-0.35 M) in the medium did not significantly affect growth rate in the absence of drug, yet reduced the growth inhibitory activity of the chlorhexidine and enhanced that of Triton X45. These effects were maximal at KCl concentrations of 0.2 M and above, when complete protection towards chlorhexidine and lysis of the cultures in the presence of Triton X45 were observed. Time-survivor curves in the presence of chlorhexidine (0.7-1.0 microM) gave LT90 values of 1.5-2.0 h in the absence of KCl, yet its inclusion (0.35 M) totally inhibited this low level bactericidal activity. Drug absorption by whole cell and isolated cell wall preparations was determined in the presence and absence of KCl (0.35 M). Chlorhexidine uptake by intact cells was reduced by approximately 50% in the presence of salt whereas that of Triton X45 increased by a similar fraction. Uptake of chlorhexidine by the cell wall fraction accounted for approximately 50% of that for the whole cells and was relatively unaffected by the presence of KCl. Conversely, absorption of Triton X45 by the cell wall fraction accounted for most of the uptake by whole cells and increased markedly in the presence of salts.
