RESUMO
Soybean fermentation broth (SFB) exhibits potent antibacterial activity against different species of bacteria in in vitro assays and animal models. Four isoflavone compounds-daidzin, genistin, genistein, and daidzein-of SFB were analyzed and quantified by high-performance liquid chromatography. In the in vitro test, daidzin and daidzein had more potent antibacterial activity than genistin. The minimum inhibition concentration values for these bacteria of SFB ranged from 1.25% to 5%, and the minimum bactericidal concentration values of strains ranged from 2.5% to 10%, depending on the species or strain. Vancomycin-resistant Entercoccus faecalis (VRE) strains were also tested for susceptibility to SFB in two species of animal model: the Sprague-Dawley rat and the BALB/c mouse. SFB-fed Sprague-Dawley rats showed excellent elimination efficiency against VRE, close to 99% compared with the phosphate-buffered saline-fed control group. In the BALB/c mouse model, SFB antibacterial activity was 65-80% against VRE compared with the control. In conclusion, SFB contains natural antibacterial substances such as daidzin, genistin, and daidzein that inhibit bacterial growth.
Assuntos
Antibacterianos/uso terapêutico , Enterococcus faecalis/efeitos dos fármacos , Glycine max/química , Infecções por Bactérias Gram-Positivas/tratamento farmacológico , Isoflavonas/uso terapêutico , Leite de Soja/farmacologia , Resistência a Vancomicina/efeitos dos fármacos , Animais , Antibacterianos/farmacologia , Modelos Animais de Doenças , Fermentação , Infecções por Bactérias Gram-Positivas/microbiologia , Isoflavonas/análise , Isoflavonas/farmacologia , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Testes de Sensibilidade Microbiana , Ratos , Ratos Sprague-DawleyRESUMO
A series of bis-aziridinylnaphthoquinone derivatives has been prepared. The cytotoxic activities and DNA alkylation abilities of these synthetic bis-aziridinylnaphthoquinone derivatives were investigated. They displayed significant cytotoxicity against human carcinomna cell lines and weak cytotoxic activities against HL60 and skin fibroblast (SF). The bisaziridinylnaphthoquinone 1a was the most potent agent among those tested, with an LD50 value of 0.57 microM against the BC-M1 cell line. It exhibited the weakest activity against SF and HL60 with LD50 values of 5.67 and 20.1 microM, respectively, and it was able to alkylate DNA after chemical reduction in vitro. The analogues without aziridinyl moiety 2a and 3a lack DNA alkylation abilities.