RESUMEN
To augment the functional attributes of pectin and expand its prospective utilization in food preservation, this research explored the enzymatic grafting of resorcinol and 4-hexylresorcinol onto pectin. Structural analysis verified the successful grafting of both resorcinol and 4-hexylresorcinol to pectin via esterification, with the 1-OH of resorcinol and 4-hexylresorcinol and the carboxyl group of pectin functioning as grafting sites. The grafting ratios of resorcinol-modified pectin (Re-Pe) and 4-hexylresorcinol-modified pectin (He-Pe) were 17.84 % and 10.98 %, respectively. This grafting modification notably enhanced the antioxidative and antibacterial properties of pectin. Specifically, DPPH clearance and the inhibition ratio in the ß-carotene bleaching assay increased from 11.38 % and 20.13 % (native pectin, Na-Pe) to 41.15 % and 36.67 % (Re-Pe), and 74.72 % and 53.40 % (He-Pe). Moreover, the inhibition zone diameter against Escherichia coli and Staphylococcus aureus rose from 10.12 and 10.08 mm (Na-Pe) to 12.36 and 11.52 mm (Re-Pe), and 16.78 and 14.87 mm (He-Pe). Additionally, the application of native and modified pectin coatings effectively impeded pork spoilage, with the modified pectins demonstrating a more potent effect. Among the two modified pectins, He-Pe exhibited the most significant enhancement in pork shelf life.
Asunto(s)
Hexilresorcinol , Pectinas , Pectinas/química , Hexilresorcinol/farmacología , Estudios Prospectivos , Conservación de Alimentos , Carne , Escherichia coliRESUMEN
High efficiency of a combined preparation including synergistic polymyxin B and 4-hexylresorcinol was shown for treatment of experimental sepsis caused by an antibiotic-resistant highly virulent hypermucoid Klebsiella pneumoniae strain KPM9Pmr in mice. Complex therapy with polymyxin B (1 mg/kg) and 4-hexylresorcinol (30 mg/kg) led to cure in 80%; in 20% of these mice, no bacterial cells were found. After treatment with polymyxin B alone, only 50% animals survived and all of them contained bacterial cells. Comparative analysis of the results of monotherapy and combined treatment indicates that 4-hexylresorcinol not only increases the efficiency of antibiotic, but also minimizes persistence of the infection agent and therefore, the risk of development of antibiotic resistance.
Asunto(s)
Antibacterianos/uso terapéutico , Farmacorresistencia Bacteriana Múltiple/efectos de los fármacos , Hexilresorcinol/farmacología , Klebsiella pneumoniae/efectos de los fármacos , Sepsis/tratamiento farmacológico , Animales , Animales no Consanguíneos , Antibacterianos/farmacología , Modelos Animales de Enfermedad , Sinergismo Farmacológico , Femenino , Infecciones por Klebsiella/complicaciones , Infecciones por Klebsiella/tratamiento farmacológico , Infecciones por Klebsiella/patología , Klebsiella pneumoniae/patogenicidad , Ratones , Pruebas de Sensibilidad Microbiana , Polimixina B/farmacología , Polimixina B/uso terapéutico , Polimixinas/análogos & derivados , Polimixinas/farmacología , Polimixinas/uso terapéutico , Sepsis/microbiologíaRESUMEN
DNA topoisomerases are highly exploited targets for antimicrobial drugs. The spread of antibiotic resistance represents a significant threat to public health and necessitates the discovery of inhibitors that target topoisomerases in novel ways. However, the traditional assays for topoisomerase activity are not suitable for the high-throughput approaches necessary for drug discovery. In this study we validate a novel assay for screening topoisomerase inhibitors. A library of 960 compounds was screened against Escherichia coli DNA gyrase and archaeal Methanosarcina mazei DNA topoisomerase VI. Several novel inhibitors were identified for both enzymes, and subsequently characterised in vitro and in vivo. Inhibitors from the M. mazei topoisomerase VI screen were tested for their ability to inhibit Arabidopsis topoisomerase VI in planta. The data from this work present new options for antibiotic drug discovery and provide insight into the mechanism of topoisomerase VI.
Asunto(s)
Proteínas Arqueales/antagonistas & inhibidores , Evaluación Preclínica de Medicamentos/métodos , Inhibidores de Topoisomerasa II , Inhibidores de Topoisomerasa/farmacología , Antraquinonas/farmacología , Arabidopsis/efectos de los fármacos , Arabidopsis/enzimología , Arabidopsis/crecimiento & desarrollo , ADN-Topoisomerasas de Tipo II , Evaluación Preclínica de Medicamentos/instrumentación , Escherichia coli/enzimología , Hexilresorcinol/farmacología , Methanosarcina/enzimología , Mitoxantrona/farmacología , Quinacrina/farmacología , Sulfolobus/enzimología , Suramina/farmacologíaRESUMEN
The anthelmintic activity of the drupe extracts of Melia azedarach L. (Meliaceae) growing in Argentina was tested against tapeworms, hookworms, nodular worms and earthworms, and was shown to be better than the standards piperazine phosphate and hexylresorcinol against tapeworms and hookworms, respectively.