脱乙酰基利福喷丁抗结核杆菌生长活性的研究

目的　探讨和研究脱乙酰基利福喷丁体内及体外抗结核杆菌生长活性的作用。方法　测定脱乙酰基利福喷丁抗人型、牛型、草型结核杆菌的最低抑菌浓度 (MIC10 0 )及小鼠半数动物存活时间 (ST50 )。并以利福喷丁作为对照药物。结果　脱乙酰基利福喷丁抗人型、牛型、草型结核杆菌的最低抑菌浓度 (MIC10 0 )分别为 2mg/L ,2mg/L及 0 .2 5mg/L(利福喷丁的MIC10 0 分别为 2mg/L ,2mg/L及 0 .5mg/L)。 10～ 4 0mg/kg剂量的利福喷丁组及脱乙酰基利福喷丁组小鼠的ST50 均超过 2 8d ;2 .5mg/kg剂量和 5 .0mg/kg剂量的脱乙酰基利福喷丁组小鼠的ST50 分别为 16d和 2 7d(而同剂量的利福喷丁组的小鼠ST50 分别为 18d和 18d) ;感染对照组小鼠的ST50 为 13d。结论　脱乙酰基利福喷丁与利福喷丁比较 ,具有相似及良好的体内外抗结核杆菌生长活性的作用。

Study of 25-O-desacetylrifapentine against tubercle bacillus growth activity

Objective It is to discuss and study the effect of 25-O-desacetylrifapentine against tubercle bacillus growth activity in vivo and in vitro.Methods The MIC100 values of 25-O-desacetylrifapentine against M.tuberculosis, M.bovis and M.phlie, and the values of half survival time (ST50) for the mice were detected. Rifapentine was applied as a control durg.Results The MIC100 values of 25-O-desacetylrifapentine against M.tuberculosis, M.bovis and M.phlie were 2 mg/L, 2 mg/L and 0.25 mg/L respectively (the MIC100 values of Rifapeentine were 2 mg/L, 2 mg/L and 0.5 mg/L respectively). The ST50 for the mice in Rifapentine groups and 25-O-desacetylrifapentine groups with 10 to 40 mg/kg dosages were both over 28 days. The ST50 for the mice in 25-O-desacetylrifapentine groups with 2.5 mg/kg and 5.0 mg/kg dosages were 16 days and 27 days respectively (the ST50 for the mice in Rifapentine groups with the same dosages were 18 days and 18 days). The ST50 for the mice in infective control group was 13 days.Conclusion The effects of 25-O-desacetylrifapentine and Rifapentine against tubercle bacillus growth activities in vivo and in vitro are similar and nicer.