Girolami R L, Stamm J M
Antimicrob Agents Chemother. 1980 Nov;18(5):766-72. doi: 10.1128/AAC.18.5.766.
The in vitro antimicrobial activity of O-demethylfortimicin A (ODMF), a derivative of fortimicin A, was compared with those of fortimicin A and gentamicin against a spectrum of 256 organisms. All three antibiotics were active in low concentrations against all strains of Enterobacteriaceae, Acinetobacter sp., and Staphylococcus aureus, with ODMF most active against Proteus mirabilis, indole-positive Proteus, and Providencia and gentamicin most active against other species. Activity of each of the antibiotics against group D streptococci was poor. The overall activity of ODMF was superior to that of fortimicin A for all groups of organisms examined and was most pronounced, approximately three-fold, against strains of Pseudomonas aeruginosa. Both ODMF and fortimicin A were resistant to the action of several aminoglycoside-inactivating enzymes, with the exception of 3-N-acetyltransferase-I. ODMF and fortimicin A showed similar rapid bactericidal effects at multiples of the minimum inhibitory concentration and equivalent synergistic activity against enterococci when combined with penicillin G. The combination of carbenicillin with ODMF, fortimicin A, or gentamicin was synergistic for approximately 80% of the P. aeruginosa strains tested. Inactivation of ODMF and fortimicin A when combined with carbenicillin in vitro was minimal or absent, whereas gentamicin was substantially inactivated under similar conditions. ODMF, fortimicin A, and gentamicin exhibited protective activity in mice infected with Escherichia coli, Klebsiella pneumoniae, Proteus vulgaris, S. aureus, or P. aeruginosa. Gentamicin was the most active, followed by ODMF and fortimicin A. The superior in vitro activity of ODMF compared with fortimicin A against P. aeruginosa was confirmed in vivo.
将福提霉素A的衍生物O - 去甲基福提霉素A（ODMF）的体外抗菌活性与福提霉素A和庆大霉素针对256种菌株的抗菌活性进行了比较。这三种抗生素在低浓度时对所有肠杆菌科菌株、不动杆菌属和金黄色葡萄球菌均有活性，其中ODMF对奇异变形杆菌、吲哚阳性变形杆菌和普罗威登斯菌活性最强，庆大霉素对其他菌种活性最强。每种抗生素对D组链球菌的活性都很差。在所检测的所有菌株组中，ODMF的总体活性均优于福提霉素A，对铜绿假单胞菌菌株的活性优势最为明显，约为其三倍。ODMF和福提霉素A均对几种氨基糖苷类失活酶的作用具有抗性，但3 - N - 乙酰转移酶 - I除外。ODMF和福提霉素A在最低抑菌浓度倍数下显示出相似的快速杀菌作用，与青霉素G联合使用时对肠球菌具有同等的协同活性。羧苄西林与ODMF、福提霉素A或庆大霉素联合使用时，对约80%的受试铜绿假单胞菌菌株具有协同作用。ODMF和福提霉素A与羧苄西林在体外联合使用时的失活作用极小或不存在，而庆大霉素在类似条件下会大量失活。ODMF、福提霉素A和庆大霉素在感染大肠杆菌、肺炎克雷伯菌、普通变形杆菌、金黄色葡萄球菌或铜绿假单胞菌的小鼠中均表现出保护活性。庆大霉素活性最强，其次是ODMF和福提霉素A。ODMF在体外对铜绿假单胞菌的活性优于福提霉素A，这一点在体内也得到了证实。
