Terasawa T, Watanabe M, Okubo T, Mitsuhashi S
Episome Institute, Seta-gun, Japan.
Antimicrob Agents Chemother. 1991 Jul;35(7):1370-5. doi: 10.1128/AAC.35.7.1370.
YM133, the 4"-O-(4-methoxyphenyl)acetyltylosin, is a new macrolide. The in vitro activity of YM133 was compared with those of erythromycin, josamycin, and rokitamycin by an agar dilution method. YM133 inhibited 90% of the tested isolates of Streptococcus pneumoniae, Legionella spp., and anaerobic bacteria at less than or equal to 1.56 micrograms/ml. The drug inhibited 90% of erythromycin-resistant staphylococci and Streptococcus pyogenes at less than or equal to 50 micrograms/ml. YM133 showed activity against erythromycin-, josamycin-, and rokitamycin-resistant (MIC greater than or equal to 100 micrograms/ml) strains of staphylococci, streptococci, Bacteroides spp., and Clostridium spp. Enterococci were less susceptible to other YM133-like macrolides. Unlike other macrolides, YM133 showed killing activity, and the MBC/MIC ratios of YM133 for several strains were 1:32, whereas those of erythromycin were 4:1,024. In a time-kill curve study, the reduction of viable cells started within 2 h after the addition of YM133.
YM133，即4”-O-(4-甲氧基苯基)乙酰泰乐菌素，是一种新型大环内酯类抗生素。采用琼脂稀释法比较了YM133与红霉素、交沙霉素和罗他霉素的体外活性。YM133对90%的肺炎链球菌、军团菌属和厌氧菌测试菌株的抑制浓度小于或等于1.56微克/毫升。该药物对90%的耐红霉素葡萄球菌和化脓性链球菌的抑制浓度小于或等于50微克/毫升。YM133对葡萄球菌、链球菌、拟杆菌属和梭菌属中耐红霉素、交沙霉素和罗他霉素（最低抑菌浓度大于或等于100微克/毫升）的菌株具有活性。肠球菌对其他类似YM133的大环内酯类抗生素不太敏感。与其他大环内酯类抗生素不同，YM133具有杀菌活性，YM133对几种菌株的最低杀菌浓度与最低抑菌浓度之比为1:32，而红霉素为4:1024。在时间-杀菌曲线研究中，加入YM133后2小时内活菌数开始减少。
