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莫匹罗星(假单胞菌酸)——一种新型局部用抗生素的抗菌活性

Antibacterial activity of mupirocin (pseudomonic acid), a new antibiotic for topical use.

作者信息

Sutherland R, Boon R J, Griffin K E, Masters P J, Slocombe B, White A R

出版信息

Antimicrob Agents Chemother. 1985 Apr;27(4):495-8. doi: 10.1128/AAC.27.4.495.

Abstract

Mupirocin (pseudomonic acid A), an antibiotic produced by Pseudomonas fluorescens, showed a high level of activity against staphylococci and streptococci and against certain gram-negative bacteria, including Haemophilus influenzae and Neisseria gonorrhoeae, but was much less active against most gram-negative bacilli an anaerobes. Nearly all clinical isolates of Staphylococcus aureus and Staphylococcus epidermidis, including multiply resistant strains, were susceptible (mupirocin MIC, less than or equal to 0.5 microgram/ml). There was no cross-resistance between mupirocin and clinically available antibiotics, and the selection of resistant variants in vitro occurred at a low frequency. Mupirocin was highly bound (95% bound) to the protein of human serum, and activity was reduced 10- to 20-fold in the presence of human serum. The activity of mupirocin was not greatly influenced by inoculum size but was significantly enhanced in acid medium. In tests of bactericidal activity, MBCs were 8- to 32-fold higher than MICs and the antibiotic demonstrated a slow bactericidal action in time-kill tests, resulting in 90 to 99% killing after 24 h at 37 degrees C.

摘要

莫匹罗星(假单胞菌酸A)是由荧光假单胞菌产生的一种抗生素,对葡萄球菌、链球菌以及某些革兰氏阴性菌,包括流感嗜血杆菌和淋病奈瑟菌,表现出高度活性,但对大多数革兰氏阴性杆菌和厌氧菌的活性则低得多。几乎所有金黄色葡萄球菌和表皮葡萄球菌的临床分离株,包括多重耐药菌株,均敏感(莫匹罗星的最低抑菌浓度小于或等于0.5微克/毫升)。莫匹罗星与临床可用抗生素之间不存在交叉耐药性,并且体外耐药变异株的选择发生频率较低。莫匹罗星与人血清蛋白高度结合(结合率为95%),在人血清存在的情况下活性降低10至20倍。莫匹罗星的活性受接种量大小的影响不大,但在酸性培养基中活性显著增强。在杀菌活性测试中,最低杀菌浓度比最低抑菌浓度高8至32倍,并且该抗生素在时间杀菌试验中表现出缓慢的杀菌作用,在37℃下24小时后导致90%至99%的杀灭率。

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