Teicoplanin, a new antibiotic from Actinoplanes teichomyceticus nov. sp.
Teicoplanin, a new glycopeptide antibiotic belonging to the same family as vancomycin, inhibits cell wall synthesis in Bacillus subtilis; the inhibition is accompanied by an intracellular accumulation of UDP-N-acetyl-muramyl-pentapeptide. A cell-free system from Bacillus stearothermophilus, capable of synthesizing peptidoglycan, is 50% inhibited by teicoplanin at 40 micrograms/ml and 100% inhibited at 100 micrograms/ml; suppression of peptidoglycan synthesis is accompanied by parallel accumulation of the lipid intermediate. Teicoplanin binds to cell walls and forms a complex with N,N'-diacetyl-L-lysyl-D-alanyl-D-alanine. The association constant of this complex is 2.56 X 10(6) liters mol-1, calculated by spectrophotometric titration. The mechanism of action of teicoplanin is discussed in comparison with those of other inhibitors of cell wall biosynthesis, namely, vancomycin, ristocetin, and gardimycin.
D000117:Acetylglucosamine / Q000378:metabolism; D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D001412:Bacillus subtilis / Q000187:drug effects / Q000378:metabolism; D001425:Bacterial Outer Membrane Proteins / Q000096:biosynthesis; D001433:Bacteriolysis / Q000187:drug effects; D001667:Binding, Competitive; D002473:Cell Wall / Q000378:metabolism; D002474:Cell-Free System; D004347:Drug Interactions; D006020:Glycopeptides / Q000378:metabolism / Q000494:pharmacology; D009113:Muramidase / Q000378:metabolism; D010457:Peptidoglycan / Q000096:biosynthesis; D011498:Protein Precursors / Q000096:biosynthesis; D017334:Teicoplanin
D000900:Anti-Bacterial Agents; D001425:Bacterial Outer Membrane Proteins; D006020:Glycopeptides; D010457:Peptidoglycan; D011498:Protein Precursors; D017334:Teicoplanin; D009113:Muramidase; D000117:Acetylglucosamine