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Novel application of embelin or embelin compound in bacterium inhibition

A technology for inhibiting bacteria and compounds, applied in the direction of antibacterial drugs, active ingredients of esters, and resistance to vector-borne diseases, etc., can solve the problem that NDM-1 does not have any inhibitory activity

Active Publication Date: 2015-12-16
MICROBE EPIDEMIC DISEASE INST OF PLA MILITARY MEDICAL ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, current in vitro experiments show that the three existing β-lactamase inhibitors do not have any inhibitory activity against NDM-1

Method used

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  • Novel application of embelin or embelin compound in bacterium inhibition
  • Novel application of embelin or embelin compound in bacterium inhibition
  • Novel application of embelin or embelin compound in bacterium inhibition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0074] Embodiment 1, the preparation of albumen

[0075] 1. Preparation of NDM-1 protein

[0076] 1, with the genomic DNA of Klebsiella pneumoniae BAA-2146 as template, carry out PCR amplification with the primer pair that P1 and P2 form, obtain PCR amplified product (the sequence 2 that has sequence listing in the PCR amplified product is from 5' The NDM-1 gene shown in the 1st to 810th nucleotides of the terminal encodes the NDM-1 protein shown in Sequence 1 of the sequence listing).

[0077] P1: 5'- catatg gaattgcccaatattatg-3';

[0078] P2: 5'- ctcgag gcgcagcttgtcggccat-3'.

[0079] PCR conditions: 95°C for 3min; 30 cycles of 94°C for 30s, 60°C for 30s, and 72°C for 1min; 72°C for 5min.

[0080] PCR reaction system (50 μl): template 2 μl, upstream and downstream primers 2 μl, dNTP 4 μl, EasyTaqpolymerase 0.5 μl, 10×buffer 5 μl, add H 2 0 to 50 μl.

[0081] The agarose gel electrophoresis of the PCR amplification product is shown in figure 2 , M is Marker (2000bp...

Embodiment 2

[0124] Embodiment 2, the inhibitory activity of anthrabeline to various β-lactamases

[0125] Embelin is the compound shown in Formula 4.

[0126] 1. Inhibitory activity of anthrabecin on NDM-1 protein

[0127] 1. The NDM-1 protein solution prepared in Example 1, biapenem and 50 μM ZnCl 2 10 mM HEPES buffer (pH 7.5) was mixed so that the concentration of NDM-1 protein was 0.5 μg / ml and the concentration of biapenem was 0.5 mM.

[0128] 2. Divide the system in step 1 into several groups, add different amounts of anthracene respectively, react at 30°C for 10 minutes, and detect the absorption value at 235nm (the specific absorption peak of antibiotics) (A 235nm value).

[0129] The relative enzymatic activity of NDM-1 protein in the system=(A 235nm -A at the end moment 235nm value) / (the A 235nm -A at the end moment 235nm value) × 100%.

[0130] The half inhibitory concentration IC of anthrabexine on NDM-1 enzyme activity 50 =Concentration (μM) of compound I when the rel...

Embodiment 3

[0150] Embodiment 3, the reversal of the drug resistance of the compound to drug-resistant bacteria

[0151] Antibiotic refers to ampicillin, cephradine, ceftazidime, cefepime, meropenem or biapenem.

[0152] Inhibitors refer to compounds provided in the present invention (compounds shown in formula 1-1, compounds shown in formula 1-2, compounds shown in formula 1-3, compounds shown in formula 1-4, compounds shown in formula 1-5 Compounds, compounds represented by formula 1-6 and compounds represented by formula 1-7, compounds represented by formula 2-1, compounds represented by formula 3-1, compounds represented by formula 3-2, compounds represented by formula 4, compounds represented by formula 5 Compounds shown in -1, compounds shown in formula 5-2, compounds shown in formula 5-3, compounds shown in formula 5-4, compounds shown in formula 5-5, compounds shown in formula 5-6, compounds shown in formula 5-7 The compound shown, the compound shown in formula 5-8, the compound ...

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Abstract

The invention discloses a novel application of an embelin or embelin compound in bacterium inhibition. According to the novel application, the embelin or embelin compound has an effect of inhibiting enzyme activity of beta-lactamase, especially a prominent effect of inhibiting the wide anti-biological hydrolytic activity of New Delhi metallo-beta-lactamase-1, can be used for remarkably improving the sensitivity of drug-resistance bacteria on antibiotics, remarkably reducing the minimal inhibitory concentration of multiple antibiotics on superbug, reversing the drug resistance of drug-resistance bacteria and reducing clinical hazard of serious drug-resistance bacteria, and has certain bacteriostatic activity. A high-concentration embelin or embelin compound has remarkable bacteriostatic activity on staphylococcus aureus, pseudomonas aeruginosa, salmonella typhimurium, shigella sonnei, shigella flexneri, klebsiella pneumoniae, escherichia coli and other pathogenic bacteria, and even can be used for completely inhibiting bacterium growth.

Description

technical field [0001] The invention relates to a new application of anthracene or anthracene compound in inhibiting bacteria. Background technique [0002] Since the clinical use of penicillin in 1940, antibiotics have played an important role in the control and treatment of diseases. β-lactam antibiotics, including penicillin, are a class of antibacterial and microbial drugs that are widely used clinically and used in large quantities. With its widespread use, many bacteria that cause human diseases have developed drug resistance, and in recent years, drug-resistant bacteria that can resist a variety of antibiotics have repeatedly appeared. The report on the detection of bacterial drug resistance in my country published in 2010 shows that the bacteria are obviously resistant to β-lactam antibiotics such as penicillin and cephalosporins, among which E. Spectrum β-lactamase, the enzyme production rate is as high as 68%. In 2010, the spread of a drug-resistant bacteria prod...

Claims

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Application Information

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IPC IPC(8): A61K31/122A61K31/22A61K31/175A61K31/136A61K31/133A61K31/166A61K31/63A61K31/343A61K31/25A61K31/473A61K31/765A61P31/04
CPCY02A50/30
Inventor 王慧李涛陈芳红刘坤
Owner MICROBE EPIDEMIC DISEASE INST OF PLA MILITARY MEDICAL ACAD OF SCI
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