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New application of using berberine as metal beta-lactamase inhibitor

A technology of lactamase and berberine, applied in the field of berberine, can solve the problem of no inhibitor

Active Publication Date: 2016-01-13
南京广方生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, the three types of enzymes A, C, and D rely on Ser in the active center to play a catalytic role, and can be inhibited by clinically used antibiotics such as clavulanic acid, tazobactam, and sulbactam; while type B enzymes need to rely on activity The Zn in the center plays a catalytic role in the enzyme, which is called metallo-β-lactamases (MBL), and there is no effective inhibitor of this type of enzyme clinically.

Method used

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  • New application of using berberine as metal beta-lactamase inhibitor
  • New application of using berberine as metal beta-lactamase inhibitor
  • New application of using berberine as metal beta-lactamase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Example 1 Detection of Berberine's Inhibitory Activity on Metallo-β-lactamases

[0018] Use 60 μM cefuroxime sodium as the substrate, and the buffer used is 50 mM HEPES (4-hydroxyethylpiperazineethanesulfonic acid), 200 mM NaCl, 100 μM ZnCl 2 , pH=7.2, the reaction temperature is 30°C, the final concentration of metallo-β-lactamase used is 10nM, and the detection wavelength is 260nm. The specific process is as follows:

[0019] 1. Firstly, the buffer solution for metallo-β-lactamase was configured into a solution with a concentration of 10nM, and incubated at 30°C for 10min, so that Zn 2+ Fully occupy the active center;

[0020] 2. Dissolve berberine in the buffer solution, prepare different concentrations, add it to the enzyme solution, and incubate at 30°C for 6 minutes to fully combine the inhibitor with the enzyme;

[0021] 3. Take 1ml of the above solution and add it to a quartz cuvette, add 3 μL of cefuroxime sodium (final concentration 60 μM) and shake well, me...

Embodiment 2

[0026] Example 2 The protective effect of berberine hydrochloride on β-lactam antibiotics

[0027] The MBLs-producing strain used in the test is the genetically engineered strain E.coliBL21(DE3) / pET28a-NDM-1, which can express NDM-1 type β-lactamase soluble in the cell, hydrolyze β-lactam antibiotics, and make Antibiotic inactivation. E.coliBL21(DE3) / pET28a strain was used as negative control. The protective effect of berberine on antibiotics was reflected by the protection index.

[0028] The protection index is defined as the ratio of the concentration of the antibiotic used when the protective agent is not added to the concentration of the antibiotic when the protective agent is added when the same activity effect (such as bacteriostasis) is achieved, as follows: when the value is greater than 1, it indicates that the addition of the protective agent After the dose, the amount of antibiotics that need to be used can be reduced, and the larger the value, the stronger the e...

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Abstract

The invention discloses new application of berberine. Berberine can be used as metal beta-lactamase inhibitor to be used for preventing compounds sensitive to metal beta-lactamase inhibitor from being hydrolyzed by enzymes, particularly hydrolysis of metal beta-lactamase for beta-lactam antibiotics, and antibiotics are protected.

Description

technical field [0001] The present invention relates to a new use of berberine as a metallo-beta-lactamase inhibitor for preventing enzymatic hydrolysis of compounds sensitive to metallo-beta-lactamases, preferably preventing metallo-beta-lactamase from affecting beta-lactamase The hydrolysis of lactam antibiotics has a protective effect on these antibiotics. By adding berberine to various preparations of β-lactam antibiotics such as penicillin, to inhibit the hydrolysis of β-lactam antibiotics by microorganisms producing metal β-lactamase, thereby improving the efficacy of β-lactam antibiotics Stability to maintain the efficacy of antibiotics. Or as preventive medicine, before using β-lactam antibiotics, use berberine to inhibit the activity of metallo-β-lactamases and improve the effect of β-lactam antibiotics. Background technique [0002] β-lactam antibiotics have good curative effect and low toxicity, and are currently important drugs for the treatment of infectious d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4375A61K31/546A61P31/04A61K31/407A61K31/431A61K31/43
Inventor 郑珩劳兴珍周丹丹余永柱
Owner 南京广方生物科技有限公司
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