Novel penicillins synthesized by biotransformation using laccase from Trametes spec.
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.
Mikolasch
Annett
A
Institute of Microbiology, Ernst-Moritz-Arndt-University Greifswald, F.-L.-Jahn-Strasse 15, 17489 Greifswald, Germany. annett.mikolasch@gmx.de
Niedermeyer
Timo Horst Johannes
TH
Lalk
Michael
M
Witt
Sabine
S
Seefeldt
Simone
S
Hammer
Elke
E
Schauer
Frieder
F
Gesell
Manuela
M
Hessel
Susanne
S
Jülich
Wolf-Dieter
WD
Lindequist
Ulrike
U
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
D000903:Antibiotics, Antineoplastic; D007202:Indicators and Reagents; D010406:Penicillins; D065093:beta-Lactamase Inhibitors; D042845:Laccase; D001618:beta-Lactamases