RESUMEN
BACKGROUND: Lubeluzole, a neuroprotective anti-ischemic drug, was tested for its ability to act as both antibiotic chemosensitizing and antipropulsive agent for the treatment of infectious diarrhea. METHODS: In the present report, the effect of lubeluzole against antidiarrheal target was tested. The antimicrobial activity towards Gram-positive and Gram-negative bacteria was investigated together with its ability to affect ileum and colon contractility. RESULTS: Concerning the antimicrobial activity, lubeluzole showed synergistic effects when used in combination with minocycline against four common Gram-positive and Gram-negative bacteria (Enterococcus faecalis ATCC 29212, Staphylococcus aureus ATCC 29213, Pseudomonas aeruginosa ATCC 27853, and Escherichia coli ATCC 25922), although relatively high doses of lubeluzole were required. In ex vivo experiments on sections of gut smooth muscles, lubeluzole reduced the intestinal contractility in a dose-dependent manner, with greater effects observed on colon than on ileum, and being more potent than reference compounds otilonium bromide and loperamide. CONCLUSION: All above results identify lubeluzole as a possible starting compound for the development of a novel class of antibacterial adjuvants endowed with spasmolytic activity.
Asunto(s)
Antidiarreicos/uso terapéutico , Diarrea/tratamiento farmacológico , Piperidinas/uso terapéutico , Tiazoles/uso terapéutico , Animales , Antibacterianos/farmacología , Bacterias/efectos de los fármacos , Colon/fisiopatología , Diarrea/microbiología , Diarrea/fisiopatología , Relación Dosis-Respuesta a Droga , Infecciones por Bacterias Gramnegativas/tratamiento farmacológico , Infecciones por Bacterias Gramnegativas/microbiología , Infecciones por Bacterias Grampositivas/tratamiento farmacológico , Infecciones por Bacterias Grampositivas/microbiología , Cobayas , Íleon/fisiopatología , Loperamida/uso terapéutico , Masculino , Pruebas de Sensibilidad Microbiana , Contracción Muscular/efectos de los fármacos , Fármacos Neuroprotectores/uso terapéutico , Compuestos de Amonio Cuaternario/uso terapéutico , Ratas , Ratas Sprague-DawleyRESUMEN
In this study we investigated a synergistic effect between the essential oils Origanum vulgare, Pelargonium graveolens and Melaleuca alternifolia and the antifungal compound Nystatin. Nystatin is considered a drug of choice in the treatment of fungal infections, but it can cause some considerable problems through its side effects, such as renal damage. Finding a new product that can reduce the Nystatin dose via combination is very important. Our findings showed an experimental occurrence of a synergistic interaction between two of these essential oils and Nystatin. The essential oil O. vulgare appeared to be the most effective, inhibiting all the Candida species evaluated in this study. Some combinations of Nystatin and P. graveolens essential oil did not have any synergistic interactions for some of the strains considered. Associations of Nystatin with M. alternifolia essential oil had only an additive effect.