Szabó I, Barabás J, Tar A, Kiss L, Filep M, Schmidt T, Marossy K, Tóth-Martinez B, Barabás G, Hernádi F
Institute of Biology, University Medical School, Debrecen, Hungary.
Antimicrob Agents Chemother. 1990 Feb;34(2):349-54. doi: 10.1128/AAC.34.2.349.
The antibacterial activity of BK-218 was similar to that of cefamandole when it was tested against several laboratory strains. The inhibiting effect of BK-218 was greater than that of cephalexin and cefoxitin on penicillin-binding proteins of Escherichia coli HB101. This result was in close correlation with the relative inhibition of radiolabeled glucosamine incorporation (greatest with BK-218) and with the lytic effect (most intensive with BK-218). BK-218 proved to be a good inhibitor for all five of the beta-lactamases that were investigated, although two enzymes (Enterobacter cloacae P99 and Pseudomonas aeruginosa Cilote) hydrolyzed it to some extent.
在针对几种实验室菌株进行测试时,BK - 218的抗菌活性与头孢孟多相似。BK - 218对大肠杆菌HB101青霉素结合蛋白的抑制作用大于头孢氨苄和头孢西丁。这一结果与放射性标记葡糖胺掺入的相对抑制作用(BK - 218的抑制作用最强)以及裂解作用(BK - 218的裂解作用最强烈)密切相关。尽管两种酶(阴沟肠杆菌P99和铜绿假单胞菌Cilote)会对BK - 218进行一定程度的水解,但BK - 218被证明是所研究的所有五种β - 内酰胺酶的良好抑制剂。