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氟罗沙星的比较抗菌活性:耐药突变体的选择频率和外膜蛋白

[Comparative antibacterial activity of fleroxacin: selection frequencies and outer membrane proteins of resistant mutants].

作者信息

Cullmann W, Dechène M, Stieglitz M

机构信息

Institut für Hygiene und Mikrobiologie der Ruhr-Universität Bochum.

出版信息

Immun Infekt. 1988 Aug;16(4):152-8.

PMID:3141267
Abstract

The antibacterial activity of fleroxacin was evaluated in 427 gram-positive and gram-negative strains, all isolated recently from clinical specimens and compared to that of ofloxacin, ciprofloxacin and co-trimoxazole. The activity of fleroxacin resembled to that of ofloxacin; its excellent activity against Haemophilus influenzae on the one hand and its lack of activity against beta-hemolytic streptococci on the other hand have to be mentioned. Selection frequencies for resistant clones were evaluated for clinical E. coli and Serratia marcescens isolates and the quinolones. With respect to clinical E. coli and Serratia marcescens isolates selection frequencies ranged from 10(-7) to 10(-9) in the presence of 2-fold or 8-fold the MIC. The outer membrane proteins of E. coli and Serratia marcescens wild-type strains were compared with those of their quinolone-resistant mutants. No discrepancies could be observed in E. coli, whereas some of the resistant Serratia marcescens mutants exhibited an increased expression of 31 kdal protein linked with a decrease of a 37 kdal major outer membrane protein. As these alterations could not be observed in each of the resistant mutants, it cannot be decided at present whether such alterations may provide an explanation for the resistance observed.

摘要

对427株革兰氏阳性和革兰氏阴性菌株(均为最近从临床标本中分离得到)的氟罗沙星抗菌活性进行了评估,并与氧氟沙星、环丙沙星和复方新诺明的抗菌活性进行了比较。氟罗沙星的活性与氧氟沙星相似;一方面,它对流感嗜血杆菌具有出色的活性,另一方面,它对β溶血性链球菌缺乏活性,这一点必须提及。对临床分离的大肠杆菌和粘质沙雷氏菌以及喹诺酮类药物的耐药克隆选择频率进行了评估。对于临床分离的大肠杆菌和粘质沙雷氏菌,在存在2倍或8倍最低抑菌浓度(MIC)的情况下,选择频率范围为10^(-7)至10^(-9)。将大肠杆菌和粘质沙雷氏菌野生型菌株的外膜蛋白与其喹诺酮耐药突变体的外膜蛋白进行了比较。在大肠杆菌中未观察到差异,而一些耐药的粘质沙雷氏菌突变体表现出31 kdal蛋白表达增加,同时37 kdal主要外膜蛋白减少。由于并非在每个耐药突变体中都能观察到这些变化,目前尚无法确定这些变化是否可以解释所观察到的耐药性。

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