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Laccase-Catalyzed Derivatization of Aminoglycoside Antibiotics and Glucosamine
- 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.
Author: | Annett Mikolasch, Ulrike Lindequist, Sabine Witt, Veronika Hahn |
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URN: | urn:nbn:de:gbv:9-opus-61276 |
DOI: | https://doi.org/10.3390/microorganisms10030626 |
ISSN: | 2076-2607 |
Parent Title (English): | Microorganisms |
Publisher: | MDPI |
Place of publication: | Basel |
Editor: | Mariam Gaid |
Document Type: | Article |
Language: | English |
Date of first Publication: | 2022/03/15 |
Release Date: | 2022/11/15 |
Tag: | aminoglycoside antibiotics; antimicrobial activity; antimicrobial resistance (AMR); biotransformation; cytotoxicity; laccase; methicillin-resistant; multidrug resistance (MDR); β-lactam antibiotics |
GND Keyword: | - |
Volume: | 10 |
Issue: | 3 |
Article Number: | 626 |
Page Number: | 13 |
Faculties: | Mathematisch-Naturwissenschaftliche Fakultät / Abteilung für Mikrobiologie und Molekularbiologie |
Licence (German): | Creative Commons - Namensnennung |