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Application of compound in preparation of medicine for inhibiting bacterial quorum sensing system

A quorum sensing system and antibacterial technology, applied in the field of medicine, can solve the problems of changing the physiological and biochemical characteristics of bacteria, reducing the effect of antibiotics, and reducing the sensitivity of antibiotics to pathogenic bacteria, so as to reduce the pathogenicity and virulence of bacteria, Does not inhibit growth, slows down the effect of bacterial multidrug resistance

Active Publication Date: 2020-09-29
GUANGDONG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0002] With the widespread use of antibiotics in clinical practice, the resistance of bacteria has gradually increased, which not only reduces the sensitivity of antibiotics to pathogenic bacteria, but also may change the physiological and biochemical characteristics of bacteria, causing bacteria to have characteristics that they did not have originally. Such as drug permeability barriers, generation of drug-inactivating enzymes, formation of biofilms, etc., thereby reducing the effect of antibiotics

Method used

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  • Application of compound in preparation of medicine for inhibiting bacterial quorum sensing system
  • Application of compound in preparation of medicine for inhibiting bacterial quorum sensing system
  • Application of compound in preparation of medicine for inhibiting bacterial quorum sensing system

Examples

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Comparison scheme
Effect test

Embodiment 1

[0053] Example 1 Extraction of 2-(3',4'-dihydroxyphenyl)-1,3-piperonin-5-aldehyde

[0054] In this embodiment, the extraction of 2-(3',4'-dihydroxyphenyl)-1,3-piperonin-5-aldehyde includes the following steps:

[0055] (1) Soak 10kg lotus seed heart in 80% (v / v) ethanol for 12h, then heat and reflux for extraction 3 times, the extraction temperature is (specific value) ℃, each time for 2h, remove the insolubles by vacuum filtration while hot , and the filtrate was dried under reduced pressure to obtain the first extract. Wherein, the mass ratio of lotus seed heart and ethanol is 1:12.

[0056] (2) The first extract was sequentially extracted three times with equal volumes of petroleum ether, ethyl acetate and n-butanol, and the ethyl acetate extract was taken, dried under reduced pressure in vacuum to obtain 4.5 g of the ethyl acetate extract;

[0057] (3) The chemical components of the ethyl acetate extract were separated by repeated silica gel column chromatography, open O...

Embodiment 2

[0059] Example 2 Effect of 2-(3',4'-dihydroxyphenyl)-1,3-piperon-5-aldehyde on PAO1-lasB pathway

[0060] Test compound: the compound 2-(3',4'-dihydroxyphenyl)-1,3-piperonen-5-aldehyde was prepared into a 200mM stock solution with 100% DMSO, and was mixed with isothiocyanate The compound Iberin (10 μM) was used as a positive control, and 0.2% DMSO was used as a solvent control.

[0061] Experimental method: the compound of the present invention is mixed with ABTGC medium in a 96-well microtiter plate and mixed by a doubling dilution method to finally have 100 μL of drug-containing ABTGC medium in each well. The culture of PAO1-lasB-gfp strain grown in LB medium at 37°C and 200rpm for 12-16h was diluted in ABTGC medium to 600nm (OD 600 ) with a final optical density of 0.02 (2.5×10 8 CFU / mL). Next, 100 μL of bacterial suspension was added to each well of a 96-well microtiter plate, so that the final concentration of the compound of the present invention in each well was 200,...

Embodiment 3

[0064] Example 3: Effect of 2-(3',4'-dihydroxyphenyl)-1,3-piperonin-5-aldehyde on PAO1-pqsA pathway

[0065] Test compound: the compound 2-(3',4'-dihydroxyphenyl)-1,3-piperonen-5-aldehyde was prepared into a 200mM stock solution with 100% DMSO, and was mixed with isothiocyanate The compound Iberin was used as a positive control, and 0.2% DMSO was used as a solvent control.

[0066] Experimental method: Take the overnight cultured PAO1-pqsA-gfp green fluorescent protein reporter strain and repeat the steps of the experimental method in Example 2 to detect 2-(3',4'-dihydroxyphenyl)-1,3-piperonylcycline-5 -Effects of aldehydes on the pqsA signaling pathway of the quorum sensing system of Pseudomonas aeruginosa.

[0067] Experimental results: see Figure 5 , is the inhibitory effect of 2-(3',4'-dihydroxyphenyl)-1,3-piperonen-5-aldehyde on the expression of pqsA-gfp in Example 3 of the present invention. Figure 5 It shows that 2-(3',4'-dihydroxyphenyl)-1,3-piperonyl-5-aldehyde ...

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to application of a compound in preparation of a medicine for inhibiting a bacterial quorum sensing system. The invention provides application of a compound in preparation of a medicine for inhibiting a bacterial quorum sensing system. Experiment results show that the 2-(3', 4'-dihydroxyphenyl)-1, 3-piperidine-5-aldehyde can inhibit three signal paths of a Pseudomonas aeruginosa quorum sensing system pqsA, lasB and rhlA and inhibit the activity of the Pseudomonas aeruginosa quorum sensing system without inhibiting the growth of the Pseudomonas aeruginosa. Therefore, the pathogenicity and toxicity of the bacteria are reduced without inhibiting the growth of the bacteria, and the generation of multiple drug resistance of the bacteria is slowed down.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to the application of a compound in the preparation of medicines for inhibiting bacterial quorum sensing systems. Background technique [0002] With the widespread use of antibiotics in clinical practice, the resistance of bacteria has gradually increased, which not only reduces the sensitivity of antibiotics to pathogenic bacteria, but also may change the physiological and biochemical characteristics of bacteria, causing bacteria to have characteristics that they did not have originally. Such as drug permeability barriers, generation of drug-inactivating enzymes, formation of biofilms, etc., thereby reducing the effect of antibiotics. At present, antibiotic resistance has become a serious public health problem worldwide. [0003] In recent years, the bacterial quorum sensing (QS) system has become an important target for the research of new anti-drug-resistant bacteri...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/36A61P31/04A61K36/62
CPCA61K31/36A61K36/62A61P31/04
Inventor 郑俊霞黄智霖陈鸿庚孙平华苏亚伦黄家晋王立抗谢俊涛杨超田文月胡炎鹏朱展良
Owner GUANGDONG UNIV OF TECH
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