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Application of 2,6-bis(2-benzimidazolyl) pyridine in preparation of carbapenem-resistant pseudomonas aeruginosa infection drug

A Pseudomonas aeruginosa, benzimidazole-based technology, applied in the field of medicine, can solve the problems of decreased drug concentration, bacteria cannot be effectively killed, etc., and achieves the effect of reducing bacteriostatic concentration, high purity of synthetic products and stable properties

Active Publication Date: 2020-09-15
HENAN UNIVERSITY OF TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The MexAB-OprM efflux pump system in Pseudomonas aeruginosa is the most important efflux pump system for carbapenem antibiotic resistance in Pseudomonas aeruginosa, and the MexA gene is a key regulatory gene in this efflux pump system , the corresponding protein expressed by this system will actively transport out the carbapenem drugs that have entered the bacteria, so that the concentration of the drug in the bacteria will decrease, making the bacteria unable to be effectively killed

Method used

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  • Application of 2,6-bis(2-benzimidazolyl) pyridine in preparation of carbapenem-resistant pseudomonas aeruginosa infection drug
  • Application of 2,6-bis(2-benzimidazolyl) pyridine in preparation of carbapenem-resistant pseudomonas aeruginosa infection drug
  • Application of 2,6-bis(2-benzimidazolyl) pyridine in preparation of carbapenem-resistant pseudomonas aeruginosa infection drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1: Verification that 2,6-bis(2-benzimidazolyl)pyridine induces the core sequence of MexA gene to form a G-quadruplex structure.

[0021] 1. Experimental equipment

[0022] The circular dichroism spectrometer was purchased from Applied Optical Physics, UK

[0023] 2. Experimental drugs and reagents

[0024] 2,6-bis(2-benzimidazolyl)pyridine was purchased from Alan (Shanghai) Huagong Technology Co., Ltd., the short-chain MexA core sequence was obtained from GeneBank (ID: 877855), and the DNA was purchased from Sangon Bioengineering (Shanghai) ) Co., Ltd., the sequence is 5'-GGCGGCGGTGGAGCAG-3', trimethylaminomethane (Tris) was purchased from Huamei Bioengineering Company, and the high-concentration stock solution of 2,6-bis(2-benzimidazolyl)pyridine was 20mM, dissolved in DMSO.

[0025] 3. Experimental method

[0026] System 1: Contains 10 μM MexA DNA and 10 mM Tris-HCl at a final concentration of 200 μL in total, and fill up the deficiency with distilled wate...

Embodiment 2

[0031] Example 2: Stability verification of the G-quadruplex structure formed by the core sequence of the MexA gene induced by 2,6-bis(2-benzimidazolyl)pyridine.

[0032] 1. Experimental equipment

[0033] The circular dichroism spectrometer was purchased from Applied Optical Physics, UK

[0034] 2. Experimental drugs and reagents

[0035] 2,6-bis(2-benzimidazolyl)pyridine was purchased from Alan (Shanghai) Huagong Technology Co., Ltd., the short-chain MexA core sequence was obtained from GeneBank (ID: 877855), and the DNA was purchased from Sangon Bioengineering (Shanghai) ) Co., Ltd., the sequence is 5'-GGCGGCGGTGGAGCAG-3', trimethylaminomethane (Tris) was purchased from Huamei Bioengineering Company, and the high-concentration stock solution of 2,6-bis(2-benzimidazolyl)pyridine was 20mM, dissolved in DMSO.

[0036] 3. Experimental method

[0037] System 1: Containing a final concentration of 20 μM MexA DNA and 10 mM Tris-HCl, the total volume is 200 μL, and the insuffic...

Embodiment 3

[0042] Example 3: Validation of 2,6-bis(2-benzimidazolyl)pyridine inhibiting MexA gene expression in carbapenem-resistant Pseudomonas aeruginosa.

[0043] 1. Experimental equipment

[0044] Fluorescent quantitative PCR instrument was purchased from Bio-Rad Company in the United States, Nanodrop2000 ultra-micro tube luminosity reagent was purchased from Thermo Fisher Corporation in the United States, and the water-proof constant temperature incubator was purchased from Shanghai Shuli Instrument Co., Ltd.

[0045] 2. Strains

[0046] Collect Pseudomonas aeruginosa strains isolated from a hospital microbiology laboratory from July to December 2018, and exclude repeated strains from the same patient. version) identified carbapenem-resistant Pseudomonas aeruginosa strains, and collected 11 carbapenem-resistant Pseudomonas aeruginosa strains. The quality control strain was Pseudomonas aeruginosa ATCC27853, which was purchased from Guangdong Huankai Microbial Technology Co., Ltd. ...

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Abstract

The invention discloses application of 2,6-bis(2-benzimidazolyl) pyridine in preparation of a carbapenem-resistant pseudomonas aeruginosa infection drug. Through circular dichroism, fluorescent real-time quantitative PCR and other methods, it is found that 2, 6-bis (2-benzimidazolyl) pyridine can form a G-quadruplex structure with a core sequence of a MexA gene in pseudomonas aeruginosa, thereby inhibiting expression of the MexA gene. A susceptibility testing verifies that 2, 6-bis (2-benzimidazolyl) pyridine can reduce the drug resistance of carbapenem-resistant pseudomonas aeruginosa to meropenem. When the usage amount of the 2, 6-bis (2-benzimidazolyl) pyridine is 5 <mu>M, the minimum inhibitory concentration of the carbapenem-resistant pseudomonas aeruginosa strain can be reduced to 2<mu> g / ml, and the effect of treating carbapenem-resistant pseudomonas aeruginosa infection by using meropenem is achieved.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the application of 2,6-bis(2-benzimidazolyl)pyridine in the preparation of carbapenem-resistant Pseudomonas aeruginosa infection drugs. Background technique [0002] Pseudomonas aeruginosa is a common opportunistic pathogen, and it is also one of the common pathogens of hospital infection in my country. The infection of Pseudomonas aeruginosa occurs mostly in the intensive care unit, and its infected patients are often accompanied by other complicated infections , treatment is very difficult. Pseudomonas aeruginosa is naturally resistant to a variety of antibiotics. In the past, third- and fourth-generation cephalosporins were often used clinically, but due to the extensive use of broad-spectrum antibiotics, more and more β-lactam-resistant antibiotics have emerged Pseudomonas aeruginosa species. Carbapenem antibiotics are currently the atypical β-lactam antibiotics with the br...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4439A61P31/04
CPCA61K31/4439A61P31/04
Inventor 苑立博杜蘅
Owner HENAN UNIVERSITY OF TECHNOLOGY
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