摘要
本文报道国产偶氮甲基利福霉素(FCE22250)对临床分离的357株革兰氏阳性、阴性菌体外抗菌活力及体内保护作用的研究。并与利福平、利福定和利福喷丁的抗菌活力进行比较。实验结果表明:偶氮甲基利福霉素对革兰氏阳性菌中的表葡球菌和金葡球菌的抑菌活力最强,在0.0005~0.125μg/ml浓度即可抑制73.96%的试验菌;对链球菌的抑菌活力不如金葡球菌好,MIC_(50)为2μg/ml;其次是粪链球菌和肠球菌。MIC_(50)均为8μg/ml。FCE22250对革兰氏阴性菌中的绿脓杆菌、大肠杆菌及肠杆菌属中的产气杆菌、阴沟杆菌亦均具有一定的抑菌活力,≤32μg/ml浓度即可抑制80%以上的试验菌,在0.25~16μg/ml浓度下可抑制所试的全部痢疾杆菌和伤寒杆菌。 偶氮甲基利福霉素体外抗金葡球菌的活力与利福喷丁一致,略低于利福平和利福定;对青霉素和甲氧西林耐药的金葡球菌敏感;在体内对金葡球菌感染具有很好的治疗活性。皮下与口服给药的ED_(50)分别为0.1和0.007mg/kg。体内抗金葡球菌的活力FCE22250不及福利平。
Results showed that FCE22250 had activityg aainst Gram-positive and Gram-negative bacteria in-vitro and in-vivo, especially Staphylococcus aureus. At a concentration of 0.005 to 0.125 μg/ml, FCE22250 inhibited 73.96% and 100% of the isolates of S. aureus and S. epidermidis respectively; and was active aainstg both Me-thicillin resistant and Penicillin resistant strains of S. aureus. At a concentration of 2 μg/ml and 5 μg/ml, it could inhibit 50% of Streptococcus spp. and Streptococcus faecalis tested.
At 32 μg/ml., 80% of Pseudomonas aeruginosa and all of Escherichia coli, E. aerogenes and E.cloeceai and at 0.25 -16μg/ml, 100% of Shigella sppiand Salmonella spp. could be inhibited.
In-vitro the activity of FCE22250 was similar to Rifapentine, and was less active than Rifampicin and Rifandin.
It showed excellent therapeutic activity in experimental mice infected by Staph. aureus when the animals were treated by oral or subcutaneous route, the ED50 of FCE 22250 was 0.1 and 0.07mg/kg respectively. The antibacterial activity of FCE 22250 in-vivo is slightly less than that of Rifampicin.
出处
《中国抗生素杂志》
CAS
CSCD
北大核心
1991年第1期52-57,共6页
Chinese Journal of Antibiotics
关键词
利福霉素
偶氮甲基
抗菌活力
FCE22250 Rifampicin 'Rifan diai Rifapentine In-vitro and in-vivo Antibacterial activity