Hiruma R, Otsuki M, Tashima M, Obana Y, Nishino T
Department of Microbiology, Kyoto Pharmaceutical University, Japan.
J Antimicrob Chemother. 1990 Dec;26(6):769-81. doi: 10.1093/jac/26.6.769.
E1040 is a new parenteral cephalosporin with a broad antibacterial spectrum and potent activity against Gram-negative bacteria including Pseudomonas aeruginosa. The in-vitro activities of E1040 against clinical isolates of Enterobacter cloacae, Ent. aerogenes, Providencia rettgeri, and Morganella morganii were superior to those of ceftazidime, cefoperazone, cefmenoxime, and cefuzonam. The activities of E1040 against Gram-positive cocci were comparable with those of ceftazidime, but it was less active than cefmenoxime, cefuzonam, and cefoperazone. Against Ps. aeruginosa, E1040 was more potent than the other compounds, with an MIC90 of 0.39 mg/l, 1/16 that of ceftazidime. The in-vitro activity of E1040 was well sustained in vivo as shown by results obtained in experimental infections in mice. In particular, E1040 was the most active drug against Ps. aeruginosa including gentamicin-resistant and beta-lactamase-overproducing strains. Morphological studies using a scanning electron microscope and a phase-contrast microscope showed that E1040 caused spheroplast and bulge formation in Ps. aeruginosa at low concentrations.
E1040是一种新型肠胃外头孢菌素，具有广谱抗菌活性，对包括铜绿假单胞菌在内的革兰氏阴性菌有强效活性。E1040对阴沟肠杆菌、产气肠杆菌、雷氏普罗威登斯菌和摩根摩根菌临床分离株的体外活性优于头孢他啶、头孢哌酮、头孢甲肟和头孢唑南。E1040对革兰氏阳性球菌的活性与头孢他啶相当，但低于头孢甲肟、头孢唑南和头孢哌酮。对于铜绿假单胞菌，E1040比其他化合物更有效，其MIC90为0.39mg/l，是头孢他啶的1/16。如在小鼠实验性感染中获得的结果所示，E1040的体外活性在体内能很好地维持。特别是，E1040是针对铜绿假单胞菌（包括耐庆大霉素和高产β-内酰胺酶菌株）最具活性的药物。使用扫描电子显微镜和相差显微镜进行的形态学研究表明，E1040在低浓度下会导致铜绿假单胞菌形成原生质球和凸起。
