Somma S, Gastaldo L, Corti A
Antimicrob Agents Chemother. 1984 Dec;26(6):917-23. doi: 10.1128/AAC.26.6.917.
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.
替考拉宁是一种与万古霉素同属一类的新型糖肽类抗生素，它能抑制枯草芽孢杆菌细胞壁的合成；这种抑制作用伴随着UDP-N-乙酰胞壁酰五肽在细胞内的积累。嗜热脂肪芽孢杆菌的一种无细胞体系能够合成肽聚糖，在替考拉宁浓度为40微克/毫升时该体系受到50%的抑制，在100微克/毫升时受到100%的抑制；肽聚糖合成的抑制伴随着脂质中间体的平行积累。替考拉宁与细胞壁结合并与N，N'-二乙酰-L-赖氨酰-D-丙氨酰-D-丙氨酸形成复合物。通过分光光度滴定法计算，该复合物的缔合常数为2.56×10⁶升·摩尔⁻¹。文中将替考拉宁的作用机制与其他细胞壁生物合成抑制剂，即万古霉素、瑞斯托菌素和加迪米星的作用机制进行了比较。
