Filters

2018 - 201912020 - 20221

More filters

20232
Reset filters

Settings

Subject: Aminoglycoside antibiotics ×

Search Results

Now showing 1 - 2 of 2
  • Thumbnail Image
    Item
    Laccase‐Catalyzed Derivatization of Aminoglycoside Antibiotics and Glucosamine
    (Basel : MDPI, 2022) Mikolasch, Annett; Lindequist, Ulrike; Witt, Sabine; Hahn, Veronika
    The increasing demand for new and effective antibiotics requires intelligent strategies to obtain a wide range of potential candidates. Laccase‐catalyzed reactions have been successfully applied to synthesize new β‐lactam antibiotics and other antibiotics. In this work, laccases from three different origins were used to produce new aminoglycoside antibiotics. Kanamycin, tobramycin and gentamicin were coupled with the laccase substrate 2,5‐dihydroxy‐N‐(2‐hydroxyethyl)‐benzamide. The products were isolated, structurally characterized and tested in vitro for antibacterial activity against various strains of Staphylococci, including multidrug‐resistant strains. The cytotoxicity of these products was tested using FL cells. The coupling products showed comparable and, in some cases, better antibacterial activity than the parent antibiotics in the agar diffusion assay, and they were not cytotoxic. The products protected mice against infection with Staphylococcus aureus, which was lethal to the control animals. The results underline the great potential of laccases in obtaining new biologically active compounds, in this case new antibiotic candidates from the class of aminoglycosides.
  • Thumbnail Image
    Item
    Complex calcium carbonate/polymer microparticles as carriers for aminoglycoside antibiotics
    (London : RSC Publishing, 2018) Racovita, Stefania; Vasiliu, Ana-Lavinia; Bele, Adrian; Schwarz, Dana; Steinbach, Christine; Boldt, Regine; Schwarz, Simona; Mihai, Marcela
    Composite microparticles of CaCO3 and two pectin samples (which differ by the functional group ratio) or corresponding nonstoichiometric polyelectrolyte complexes with different molar ratios (0.5, 0.9 and 1.2) are obtained, characterized and tested for loading and release of streptomycin and kanamycin sulphate. The synthesized carriers were characterized before and after drug loading in terms of morphology (by SEM using secondary electron and energy selective backscattered electron detectors), porosity (by water sorption isotherms) and elemental composition (by elemental mapping using energy dispersive X-ray and FTIR spectroscopy). The kinetics of the release mechanism from the microparticles was investigated using Higuchi and Korsmeyer-Peppas mathematical models.