RESUMEN
The study presents unconventional, bifunctional, heterogeneous antimicrobial agents - Cu2O-loaded anion exchangers. The synergetic effect of a cuprous oxide deposit and polymeric support with trimethyl ammonium groups was studied against the reference strains of Enterococcus faecalis ATCC 29212 and Pseudomonas aeruginosa ATCC 27853. Biological testing (minimum bactericidal concentration, MBC), time- and dose-dependent bactericidal effect (under different conditions - medium composition and static/dynamic culture) demonstrated promising antimicrobial activity and confirmed its multimode character. The standard values of MBC, for all studied hybrid polymers and bacteria, were similar (64-128 mg/mL). However, depending on the medium conditions, due to the copper release into the bulk solution, bacteria were actively killed even at much lower doses of the hybrid polymer (25 mg/mL) and low Cu(II) concentrations in solution (0.01 mg/L). Simultaneously, confocal microscopic studies confirmed the effective inhibition of bacterial adhesion and biofilm formation on their surface. The studies conducted under different conditions showed also the influence of the structure and physical properties of studied materials on the biocidal efficacy and an antimicrobial action mechanism was proposed that could be significantly affected by electrostatic interactions and copper release to the solution. Although the antibacterial activity was also dependent on various strategies of bacterial cell resistance to heavy metals present in the aqueous medium, the studied hybrid polymers are versatile and efficient biocidal agents against bacteria of both types, Gram-positive and Gram-negative. Therefore, they can be a convenient alternative for point-of-use water disinfection systems providing water quality in medical devices such as dental units, spa equipment, and aesthetic devices used in the cosmetic sector.
Asunto(s)
Antiinfecciosos , Infecciones Bacterianas , Humanos , Cobre/farmacología , Bacterias , Antibacterianos/farmacología , Antibacterianos/química , Polímeros , Pruebas de Sensibilidad MicrobianaRESUMEN
Helicobacter pylori is one of the most frequent human pathogens and a leading etiological agent of various gastric diseases. As stringent response, coordinated by a SpoT protein, seems to be crucial for the survivability of H. pylori, the main goal of this article was to use in silico computational studies to find phytochemical compounds capable of binding to the active site of SpoT from H. pylori and confirm the ability of the most active candidates to interfere with the virulence of this bacterium through in vitro experiments. From 791 natural substances submitted for the virtual screening procedure, 10 were chosen and followed for further in vitro examinations. Among these, dioscin showed the most interesting parameters (the lowest MIC, the highest anti-biofilm activity in static conditions, and a relatively low stimulation of morphological transition into coccoids). Therefore, in the last part, we extended the research with a number of further experiments and observed the ability of dioscin to significantly reduce the formation of H. pylori biofilm under Bioflux-generated flow conditions and its capacity for additive enhancement of the antibacterial activity of all three commonly used antibiotics (clarithromycin, metronidazole, and levofloxacin). Based on these results, we suggest that dioscin may be an interesting candidate for new therapies targeting H. pylori survivability and virulence.