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光学活性氧氟沙星对DNA回旋酶的抑制作用。

Inhibition of DNA gyrase by optically active ofloxacin.

作者信息

Imamura M, Shibamura S, Hayakawa I, Osada Y

出版信息

Antimicrob Agents Chemother. 1987 Feb;31(2):325-7. doi: 10.1128/AAC.31.2.325.

DOI:10.1128/AAC.31.2.325
PMID:3032098
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC174716/
Abstract

Inhibition of DNA gyrase activity by optically active ofloxacins was studied and compared with the inhibition of norfloxacin and ciprofloxacin. The (-)-isomer of ofloxacin inhibited the supercoiling activity of gyrase from Micrococcus luteus more effectively than did the (+)-isomer. The 50% inhibitory concentrations of (-)-, (+/-)-, and (+)-ofloxacin; norfloxacin; and ciprofloxacin for gyrase from Escherichia coli were 0.78, 0.98, 7.24, 0.78, and 1.15 microgram/ml, respectively. These values correlated well with the antibacterial activity of each compound against intact bacterial cells.

摘要

研究了旋光性氧氟沙星对DNA促旋酶活性的抑制作用，并与诺氟沙星和环丙沙星的抑制作用进行了比较。氧氟沙星的（-）-异构体比（+）-异构体更有效地抑制了藤黄微球菌促旋酶的超螺旋活性。（-）-、（±）-和（+）-氧氟沙星；诺氟沙星；以及环丙沙星对大肠杆菌促旋酶的50%抑制浓度分别为0.78、0.98、7.24、0.78和1.15微克/毫升。这些值与每种化合物对完整细菌细胞的抗菌活性密切相关。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6fbe/174716/f3ed4fe7d23b/aac00093-0214-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6fbe/174716/f3ed4fe7d23b/aac00093-0214-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6fbe/174716/f3ed4fe7d23b/aac00093-0214-a.jpg

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本文引用的文献

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In vitro and in vivo activity of DL-8280, a new oxazine derivative.新型恶嗪衍生物DL-8280的体外和体内活性
Antimicrob Agents Chemother. 1982 Oct;22(4):548-53. doi: 10.1128/AAC.22.4.548.
2
DNA gyrase: affinity chromatography on novobiocin-Sepharose and catalytic properties.DNA 回旋酶：新生霉素 - 琼脂糖亲和层析及催化特性
Nucleic Acids Res. 1981 Aug 11;9(15):3589-603. doi: 10.1093/nar/9.15.3589.
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Replication of colicin E1 plasmid DNA in cell extracts.大肠杆菌素E1质粒DNA在细胞提取物中的复制
Clin Pharmacokinet. 1997 Feb;32(2):101-19. doi: 10.2165/00003088-199732020-00002.
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Spectrum of activity of levofloxacin against nontuberculous mycobacteria and its activity against the Mycobacterium avium complex in combination with ethambutol, rifampin, roxithromycin, amikacin, and clofazimine.左氧氟沙星对非结核分枝杆菌的活性谱及其与乙胺丁醇、利福平、罗红霉素、阿米卡星和氯法齐明联合对鸟分枝杆菌复合群的活性。
Antimicrob Agents Chemother. 1996 Nov;40(11):2483-7. doi: 10.1128/AAC.40.11.2483.
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Mechanism of differential activities of ofloxacin enantiomers.氧氟沙星对映体的差异活性机制。
Antimicrob Agents Chemother. 1996 Aug;40(8):1775-84. doi: 10.1128/AAC.40.8.1775.
6
Prevalence of resistance to three fluoroquinolones: assessment of levofloxacin disk test error rates and surrogate predictors of levofloxacin susceptibility. AST Surveillance Group.对三种氟喹诺酮类药物的耐药率：左氧氟沙星纸片扩散法检测错误率及左氧氟沙星敏感性替代预测指标的评估。AST监测组。
Antimicrob Agents Chemother. 1996 Jul;40(7):1633-9. doi: 10.1128/AAC.40.7.1633.
7
In vitro activities of levofloxacin used alone and in combination with first- and second-line antituberculous drugs against Mycobacterium tuberculosis.左氧氟沙星单独及与一线和二线抗结核药物联合使用对结核分枝杆菌的体外活性。
Antimicrob Agents Chemother. 1996 Jul;40(7):1610-6. doi: 10.1128/AAC.40.7.1610.
8
Novel 1-8-bridged chiral quinolones with activity against topoisomerase II: stereospecificity of the eukaryotic enzyme.具有拓扑异构酶II活性的新型1,8-桥连手性喹诺酮类：真核酶的立体特异性
Antimicrob Agents Chemother. 1993 Apr;37(4):646-51. doi: 10.1128/AAC.37.4.646.
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4
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6
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9
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