Novel quaternized polysulfones (PSFs) with two ionic chlorine contents were investigated, namely, their morphology and antimicrobial activity. Atomic force microscopy (AFM) studies on their membranes showed ordered domains, in which pores and nodules of different sizes and intensities were distributed. The charge density of the quaternized PSFs and the history of the membranes formed from solutions in solvent/nonsolvent mixtures influenced the different aspects of the surface images. The adhesion of Escherichia coli ATCC 10536 and Staphylococcus aureus ATCCC 6538 microorganisms to solutions of the modified PSFs is discussed in correlation with the hydrophobic/hydrophilic properties of the studied polymers and microorganisms.

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We report here the design, synthesis, experimental and in silico evaluation of the antibacterial and antifungal activity of some new benzo[f]quinoline derivatives. Two classes of benzo[f]quinolinium derivatives—(benzo[f]quinolinium salts (BQS) and pyrrolobenzo[f]quinolinium cycloadducts (PBQC)—were designed and obtained in two steps via a direct and facile procedure: quaternization followed by a cycloaddition reaction. The synthesized compounds were characterized by elemental and spectral analysis (FT-IR, 1H-NMR, 13C-NMR). The antimicrobial assay reveals that the BQS salts have an excellent quasi-nonselective antifungal activity against the fungus Candida albicans (some of them higher that the control drug nystatin) and very good antibacterial activity against the Gram positive bacterium Staphylococcus aureus. The PBQC compounds are inactive. Analysis of the biological data reveals interesting SAR correlations in the benzo[f]quinolinium series of compounds. The in silico studies furnished important data concerning the pharmacodynamics, pharmacokinetics and ADMET parameters of the BQS salts. Studies of the interaction of each BQS salt 3a–o with ATP synthase in the formed complex, reveal that salts 3j, 3i, and 3n have the best fit in a complex with ATP synthase. Study of the interaction of each BQS salt 3a-o with TOPO II in the formed complex reveals that salts 3j and 3n have the best-fit in complex with TOPO II. The in silico ADMET studies reveal that the BQS salts have excellent drug-like properties, including a low toxicity profile. Overall, the experimental and in silico studies indicate that compounds 3e and 3f (from the aliphatic series), respectively, and 3i, 3j and 3n (from the aromatic series), are promising leading drug candidates.

Combination of antibiotics with natural products is a promising strategy for potentiating antibiotic activity and overcoming antibiotic resistance. The purpose of the present study was to investigate whether morusin and kuwanon G, prenylated phenolics in Morus species, have the ability to enhance antibiotic activity and reverse antibiotic resistance in Staphylococcus aureus and Staphylococcus epidermidis . Commonly used antibiotics (oxacillin, erythromycin, gentamicin, ciprofloxacin, tetracycline, clindamycin) were selected for the combination studies. Checkerboard and time-kill assays were used to investigate potential bacteriostatic and bactericidal synergistic interactions, respectively between morusin or kuwanon G and antibiotics. According to both fractional inhibitory concentration index and response surface models, twenty combinations (14 morusin-antibiotic combinations, six kuwanon G-antibiotic combinations) displaying bacteriostatic synergy were identified, with 4–512-fold reduction in the minimum inhibitory concentration values of antibiotics in combination. Both morusin and kuwanon G reversed oxacillin resistance of methicillin-resistant Staphylococcus aureus. In addition, morusin reversed tetracycline resistance of Staphylococcus epidermidis . At half of the minimum inhibitory concentrations, combinations of morusin with oxacillin or gentamicin showed bactericidal synergy against methicillin-resistant Staphylococcus aureus. Fluorescence and differential interference contrast microscopy and scanning electron microscopy showed an increase in the membrane permeability and massive leakage of cellular content in methicillin-resistant Staphylococcus aureus exposed to morusin or kuwanon G . Overall, our findings strongly indicate that both prenylated compounds are good candidates for the development of novel antibacterial combination therapies.

Quaternized polysulfones with different ionic chlorine content tested for biomedical applications were obtained by quaternization reaction of chloromethylated polysulfones with N,N‐dimethylethanolamine. The relationship between the different physical and chemical characteristics of these polymers and their biocompatible and antimicrobial properties was established for maximizing the selectivity and performance of these materials for biomedical applications. Therefore, topographic reorganization of the polysulfonic films induced by the type of nonsolvent in casting solutions of polymer significantly influences films morphology, depending on the charge density of polyelectrolytes, the hydrophilic/hydrophobic characteristics, as well as on the history of the formed films. Furthermore, the study of the adhesion of red blood cells and cohesion of platelets on the surface of quaternized polysulfone films, as well as analysis of antibacterial activity, using Pseudomonas aeruginosa ATCC 27853 and Staphylococcus aureus ATCC 25923 microorganisms, contribute to extending the possible applications of quaternized polysulfones as semipermeable membranes in biomedical domains. POLYM. ENG. SCI., 55:2184–2194, 2015. © 2015 Society of Plastics Engineers

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In the present study, we report enhanced antimicrobial properties of 29 and 23 nm silver nanoparticles (Ag NPs) obtained by electrochemical synthesis in poly(amide-hydroxyurethane) media. Antibacterial activity assessed by disk diffusion method indicates that silver nanoparticles produced inhibition zones for both Escherichia coli and Staphylococcus aureus depending on silver concentration. The bacterial growth curve performed in the presence of silver nanoparticles showed a stronger antibacterial effect at lower concentrations than those described in the earlier reports. The effect was both dose and size dependent and was more pronounced against Gram negative bacteria than Gram positive one. The smallest Ag NPs used had a bactericidal effect resulting in killing E. coli cells. Scanning electron microscopy analysis indicated major damage and morphology changes of the silver nanoparticles treated bacterial cells. The major mechanism responsible for the antibacterial effect probably consists in clusters formation and nanoparticles anchorage to the bacterial cell surface.

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