Application of fluoroquinolone medicine used as polymyxin-type antibiotic sensitizer

A technology of fluoroquinolones and polymyxins, which is applied to medical preparations containing active ingredients, antibacterial drugs, pharmaceutical formulations, etc., and can solve problems such as high cost and long research and development cycle

Inactive Publication Date: 2019-11-15
EAST CHINA UNIV OF SCI & TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] There are two strategies to deal with the emergency of drug resistance. One is to study a new type of antibiotic with a new mode of action against resistant strains. However, this strategy has a long development cycle and high cost, and cannot alleviate clinical difficulties in a short period of time. situation

Method used

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  • Application of fluoroquinolone medicine used as polymyxin-type antibiotic sensitizer
  • Application of fluoroquinolone medicine used as polymyxin-type antibiotic sensitizer
  • Application of fluoroquinolone medicine used as polymyxin-type antibiotic sensitizer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Fluoroquinolone-sensitizing polymyxin B (Polymyxin B) produces a checkerboard experiment on the growth inhibition of DK2.

[0025] (1) Experimental materials and methods

[0026] DK2 was cultured overnight and diluted with fresh LB medium to an absorbance (OD600) of about 0.01. Add 100 μL of bacterial suspension to a 96-well plate, then add corresponding concentrations of fluoroquinolones and polymyxin B, and incubate the plate at 37°C for 18 hours. Fractional inhibitory concentration (FIC) was determined by checkerboard. The minimum inhibitory concentration (Minimum Inhibitory Concentration, abbreviated as "MIC") of each drug is the concentration of the drug when the sterile growth is visible to the naked eye. The FIC for each drug was calculated as (MIC of agents when used in combination) / (MIC of agents when used alone). The FIC index (FICI) is the sum of the FICs of fluoroquinolones and polymyxin B.

[0027] (2) Experimental results

[0028] The results are show...

Embodiment 2

[0042] Gemifloxacin sensitized polymyxin B inhibited DK2 growth in a concentration-dependent experiment.

[0043] (1) Experimental materials and methods: the same as "Example 1".

[0044] (2) Experimental results: See Table 3 for the results.

[0045] table 3

[0046]

[0047] a Refers to the MIC of polymyxin B for DK2 when combined with the corresponding concentration of gemifloxacin.

[0048] It can be seen from Table 3 that gemifloxacin can sensitize polymyxin B to DK2 in a concentration-dependent growth inhibitory effect, and the sensitization effect of gemifloxacin is 1 μg / mL is the best.

Embodiment 3

[0050] Gemifloxacin, enrofloxacin and sparfloxacin-sensitized colistin (Colistin) have growth inhibitory effects on DK2.

[0051] (1) Experimental materials and methods: the same as "Example 1". For DK2, when colistin was used alone, the MIC was >1024 μg / mL (indicating that DK2 was also severely resistant to colistin).

[0052] (2) Experimental results: the results are shown in Table 4.

[0053] Table 4

[0054]

[0055]

[0056] a Refers to the MIC of fluoroquinolones alone for DK2.

[0057] b Refers to the MIC of colistin for DK2 when combined with 1 μg / mL fluoroquinolone.

[0058] c The MIC sensitive point of colistin to aeruginosa was ≤2 μg / mL, and the drug-resistant point was ≥4 μg / mL.

[0059] It can be seen from Table 4 that gemifloxacin, enrofloxacin and sparfloxacin can sensitize the growth inhibitory effect of colistin on DK2. Among them, gemifloxacin and enrofloxacin can reduce the MIC of colistin to the range of clinical use.

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Abstract

The invention discloses novel application of a fluoroquinolone medicine and application of the fluoroquinolone medicine in preparation of a sensitizer of a pseudomonas aeruginosa (P.aeruginosa) inhibitor. The fluoroquinolone medicine is prepared from gemifloxacin, sparfloxacin, enrofloxacin, ciprofloxacin, sarafloxacin, moxifloxacin, pefloxacin, tosufloxacin, orbifloxacin, prulifloxacin, marbofloxacin, levofloxacin, flumequine or/and pazufloxacin; the pseudomonas aeruginosa is pseudomonas aeruginosa DK2 or PAO1; the pseudomonas aeruginosa inhibitor is polymyxin B or colistin.

Description

technical field [0001] The invention relates to a new application of fluoroquinolones; in particular, it relates to the application of fluoroquinolones in the preparation of sensitizers for Pseudomonas aeruginosa (P. aeruginosa) inhibitors. Background technique [0002] Pseudomonas aeruginosa (P. aeruginosa) is a serious human pathogen that can cause life-threatening infections. Multidrug-resistant (MDR) P. aeruginosa poses a serious threat to public health due to excessive intrinsic and acquired resistance mechanisms. In developed countries, P. aeruginosa is responsible for community- and hospital-acquired infections, including hospital-acquired pneumonia (HAP), ventilator-associated pneumonia (VAP), and bloodstream infection (BSI) (Imperi, Antimicrob.Agents.Chemother.2013, 57, 996-1005. Puzniak, Antimicrob Agents Chemother. 2019, 63, e02564. Nagarajan, Chin. Chem. Lett, 2014, 25, 419-422). In addition, P.aeruginosa is a common pathogen in patients with cystic fibrosis (C...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K31/4709A61K31/496A61K38/12A61P31/04
CPCA61K31/4709A61K31/496A61K38/12A61K45/00A61P31/04A61K2300/00
Inventor 李剑蓝乐夫郑新羽毛斐李晓康曹荞曹芹
Owner EAST CHINA UNIV OF SCI & TECH
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