摘要
本文对呋苄青霉素等五种B—内酰胺类抗生素与绿脓杆菌K799/WT靶位蛋白—青霉素结合蛋白(PBPs)的亲和力进行了研究。结果表明呋苄青霉素对绿脓杆菌K799/WT的致死性PBPs具有强大的亲和力。对PBP-1a、PBP-1b、PBP-2、PBP-3的IC_(50)值分别为0.13、1.03、2.89、0.014 mg/L。羧节青霉素对PBP-1a、PBP-2、PBP-3的亲和力仅分别为呋苄青霉素的34％,<9.6％,与2.9％。呋苄青霉素对绿脓杆菌PBPS亲和力与苯咪唑青霉素相似,优于氧哌嗪青霉素与头孢哌酮。
The competition of furbenicillin (FBC) and other four beta-lactams with 14C-penicillin G for the peuicillinbinding proteins (PBPs) in Pseudomonas aeruginosa K 799/WT was investigated. FBC showed very high affinity to all three essential target proteins in the membrane of K799/WT. IC50 value (mg/ L) of FBC for the PBPs are as follows: PBP-la 0.13, PBP-lb 1.03, PBP-2 2.89, PBP 3 0.014. In contrast, for the corresponding PBPs, IC50 of carbenicillin (CBC) are 0.38, 1.16, >30, 0.49 respectively. So, the affinity of CBC to PBP-la, PBP-2, PBP-3 are 34%, <9.4%, 2.9% of thes of FBC.The affinity of azlocillin (AZL) to the essential PBPs is similar to FBC. Piperacillin (PIP) showed lower affinity than that of FBC and AZL to PBP-2, but higher affinity to PBP-lb than that of other bet-lactams tested.Although cefoperazone (CFP) showed high competing potency for PBP-la, its affinity to PBP-2 and PBP-3 were much lower than that of FBC and other ureidopenicillins.The molecular bases of the stronger activity of FBC than CBC against Pseudomonas aeruginosa was discussed.
出处
《北京医科大学学报》
CSCD
1989年第5期357-360,共4页
Journal of Peking University(Health Sciences)
关键词
呋苄青霉素
绿脓杆菌
结合蛋白
furbenicillin Ps. aeruginosa K799/WT Penicillin-binding proteins
