Yamamoto T, Amitani R, Kuze F, Suzuki K
Department of Infection and Inflammation, First Clinic of Medicine, Kyoto, Japan.
Kekkaku. 1990 Dec;65(12):805-10.
The in vitro anti-M. tuberculosis and anti-M. avium complex activities of five new rifamycin derivatives, KRM1648, KRM1657, KRM1668, KRM1674 and KRM2312, provided by Kanegafuchi Chem. Ind. Co. Japan were evaluated and compared with those of rifampicin (RFP) and rifabutin (RBU). Antimycobacterial activity was tested by broth dilution method using Kirchner's liquid medium supplemented with 10% bovine serum. The MICs 90 (micrograms/ml) of all five KRMs and RBU for 20 clinical isolates of M. tuberculosis were 0.035-0.07, whereas that of RFP was 1.25. The new rifamycin derivatives showed 16 to 32 times lower MICs than those of RFP against M. tuberculosis. All five KRMs inhibited 100% of 20 clinical isolates of M. avium complex at a concentration of 1.25 micrograms/ml, while only 35% and 10% of the strains were inhibited by the same concentration of RBU and RFP, respectively. The MICs 90 (micrograms/ml) for the strains tested were 0.07-0.3 for all five KRMs, and 5 and 40-80 for RBU and RFP, respectively. The new rifamycin derivatives were 16 times more active than RBU, which was 8 times more active than RFP. The new rifamycin derivatives were far more effective against M. tuberculosis in vitro than RFP, and their superiority to RBU which showed the effect superior to RFP was notable in in vitro anti-M. avium complex activities.
对日本钟渊化学工业株式会社提供的5种新型利福霉素衍生物KRM1648、KRM1657、KRM1668、KRM1674和KRM2312的体外抗结核分枝杆菌和抗鸟分枝杆菌复合群活性进行了评估，并与利福平（RFP）和利福布汀（RBU）进行了比较。采用添加10%牛血清的基尔希纳液体培养基，通过肉汤稀释法检测抗分枝杆菌活性。5种KRM和RBU对20株结核分枝杆菌临床分离株的MIC90（微克/毫升）为0.035 - 0.07，而RFP的MIC90为1.25。新型利福霉素衍生物对结核分枝杆菌的MIC比RFP低16至32倍。5种KRM在浓度为1.25微克/毫升时对20株鸟分枝杆菌复合群临床分离株的抑制率均为100%，而相同浓度的RBU和RFP分别仅抑制35%和10%的菌株。5种KRM对所测试菌株的MIC90（微克/毫升）为0.07 - 0.3，RBU和RFP的MIC90分别为5和40 - 80。新型利福霉素衍生物的活性比RBU高16倍，RBU的活性比RFP高8倍。新型利福霉素衍生物在体外对结核分枝杆菌的效果远优于RFP，并且在体外抗鸟分枝杆菌复合群活性方面，它们相对于显示出比RFP更优效果的RBU的优势显著。
