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Author: Hahn, Veronika Ɨ Start date: 2020 Ɨ DDC: 570 Ɨ Type: Text Ɨ Version: publishedVersion Ɨ Publisher: Basel : MDPI Ɨ WGL Institute: INP Ɨ

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    Laccaseā€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. Laccaseā€catalyzed reactions have been successfully applied to synthesize new Ī²ā€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 2,5ā€dihydroxyā€Nā€(2ā€hydroxyethyl)ā€benzamide. The products were isolated, structurally characterized and tested in vitro for antibacterial activity against various strains of Staphylococci, including multidrugā€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.
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    Laccase-catalyzed derivatization of antibiotics with sulfonamide or sulfone structures
    (Basel : MDPI, 2021) Mikolasch, Annett; Hahn, Veronika
    Trametes spec. laccase (EC 1.10.3.2.) mediates the oxidative coupling of antibiotics with sulfonamide or sulfone structures with 2,5-dihydroxybenzene derivatives to form new heterodimers and heterotrimers. These heteromolecular hybrid products are formed by nuclear amination of the p-hydroquinones with the primary amino group of the sulfonamide or sulfone antibiotics, and they inhibited in vitro the growth of Staphylococcus species, including multidrug-resistant strains.