title: Novel penicillins synthesized by biotransformation using laccase from Trametes spec.
abstract: Eight novel penicillins were synthesized by heteromolecular reaction of ampicillin or amoxicillin with 2,5-dihydroxybenzoic acid derivatives using a laccase from Trametes spec. All products inhibited the growth of several gram positive bacterial strains in the agar diffusion assay, among them methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococci. The products protected mice against an infection with Staphylococcus aureus lethal to the untreated animals. Cytotoxicity and acute toxicity of the new compounds were neglectable. The results show the usefulness of laccase for the synthesis of potential new antibiotics. The biological activity of the new compounds stimulates intensified pharmacological tests.
authors.affiliation: Institute of Microbiology, Ernst-Moritz-Arndt-University Greifswald, F.-L.-Jahn-Strasse 15, 17489 Greifswald, Germany. annett.mikolasch@gmx.de
authors.forename: Annett
authors.initials: A
authors.lastname: Mikolasch
authors.forename: Timo Horst Johannes
authors.initials: TH
authors.lastname: Niedermeyer
authors.forename: Michael
authors.initials: M
authors.lastname: Lalk
authors.forename: Sabine
authors.initials: S
authors.lastname: Witt
authors.forename: Simone
authors.initials: S
authors.lastname: Seefeldt
authors.forename: Elke
authors.initials: E
authors.lastname: Hammer
authors.forename: Frieder
authors.initials: F
authors.lastname: Schauer
authors.forename: Manuela
authors.initials: M
authors.lastname: Gesell
authors.forename: Susanne
authors.initials: S
authors.lastname: Hessel
authors.forename: Wolf-Dieter
authors.initials: WD
authors.lastname: Jülich
authors.forename: Ulrike
authors.initials: U
authors.lastname: Lindequist
mesh_terms: D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects; D001487:Basidiomycota / Q000378:metabolism*; D045744:Cell Line, Tumor; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002851:Chromatography, High Pressure Liquid; D005260:Female; D007202:Indicators and Reagents; D042845:Laccase / Q000378:metabolism*; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D051379:Mice; D008807:Mice, Inbred BALB C; D008826:Microbial Sensitivity Tests; D010406:Penicillins / Q000096:biosynthesis* / Q000494:pharmacology; D013203:Staphylococcal Infections / Q000188:drug therapy / Q000382:microbiology; D065093:beta-Lactamase Inhibitors; D001618:beta-Lactamases / Q000378:metabolism
chemical_list: D000903:Antibiotics, Antineoplastic; D007202:Indicators and Reagents; D010406:Penicillins; D065093:beta-Lactamase Inhibitors; D042845:Laccase; D001618:beta-Lactamases