Laber G, Schütze E
Zentralbl Bakteriol Orig A. 1977 Nov;239(3):403-8.
The minimal growth inhibiting concentration of tiamulin, a derivative of the diterpen antibiotic pleuromutilin, was evaluated in vitro against 11 different serogroups of leptospira interrogans by twofold serial dilution technique, in comparison to tetracyclin, dihydrostreptomycin and tylosin. The range of the MIC values of tiamulin is between 0.07 and 2.5 microgram/ml and thus comparable to the activities of the standard antibiotics tested (see table 1). The chemotherapeutic efficacy (ED50) of the compound was examined in two experimental leptospiral infections of the Syrian hamster, in comparison to tetracyclin. Both compounds were administered orally for 3 days. In the L. canicola infection, the ED50 values were 103.8 mg/kg and 306.3 mg/kg body-weight for tiamulin and tetracyclin, respectively. In the L. grippotyphosa infection, the ED50 values amounted to 35.16 and 277.5 mg/kg bodyweight for tiamulin and tetracyclin, respectively. Based on these values, tiamulin in comparison to tetracyclin showed 3-8 fold higher efficacy in vivo after oral administration.
通过两倍连续稀释技术，体外评估了二萜类抗生素截短侧耳素的衍生物泰妙菌素对11种不同血清群问号钩端螺旋体的最小生长抑制浓度，并与四环素、二氢链霉素和泰乐菌素进行了比较。泰妙菌素的最小抑菌浓度（MIC）值范围在0.07至2.5微克/毫升之间，因此与所测试的标准抗生素活性相当（见表1）。与四环素相比，在叙利亚仓鼠的两种实验性钩端螺旋体感染中检测了该化合物的化疗效果（ED50）。两种化合物均口服给药3天。在犬型钩端螺旋体感染中，泰妙菌素和四环素的ED50值分别为103.8毫克/千克和306.3毫克/千克体重。在黄疸出血型钩端螺旋体感染中，泰妙菌素和四环素的ED50值分别为35.16和277.5毫克/千克体重。基于这些值，与四环素相比，泰妙菌素口服给药后在体内显示出高3至8倍的疗效。
