Application of flavone oxygen glycoside compounds in preparations of bacterial quorum sensing inhibitory drugs

A flavonoid oxoside and quorum sensing technology, applied in the field of biomedicine, can solve problems such as bacterial quorum sensing systems that have not yet been discovered, and achieve the effects of not easy bacterial resistance and great citation prospects.

Inactive Publication Date: 2019-06-04
GUANGDONG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But so far, most of its reports have focused on pharmacology, extraction, and analysis, and i

Method used

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  • Application of flavone oxygen glycoside compounds in preparations of bacterial quorum sensing inhibitory drugs
  • Application of flavone oxygen glycoside compounds in preparations of bacterial quorum sensing inhibitory drugs
  • Application of flavone oxygen glycoside compounds in preparations of bacterial quorum sensing inhibitory drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] The biofilm inhibition experiment of embodiment 1 flavonoid oxyglycosides

[0031] Test compound: with furanone compound (Z)-4-bromo-5-(bromomethylene)-2(5H)-furanone as positive control, DMSO as negative control, positive drug and compound 1 of the present invention ~3 flavonoid oxyglycosides were formulated to 32, 64, 128 μg / mL, respectively.

[0032] Test strains: Pseudomonas aeruginosa 9027 (ATCC 9027), Pseudomonas aeruginosa 27853 (ATCC 27853) and drug-resistant Pseudomonas aeruginosa (drug-resistant strain).

[0033] Experimental method: Add 100 μL of the prepared compound to be tested to the well plate, and inoculate 100 μL of bacterial solution. A blank control group (200 μL of LB medium) and a negative control group (100 μL of each of LB medium and bacterial solution) were set up. Incubated in a 37°C incubator. After 20 hours, absorb the bacterial liquid on the surface layer of the hole, wash with distilled water three times, and wash away the planktonic bac...

Embodiment 2

[0037] Embodiment 2 anti-pseudomonas aeruginosa granules

[0038] Compound 1 10mg;

[0039] Lactose 15mg;

[0040] 10% starch slurry 3mg;

[0041] The preparation steps of anti-pseudomonas aeruginosa granules are:

[0042] (1) Take 10 mg of compound 1 in Example 1, first mix it with lactose for 10-15 minutes;

[0043] (2) Add 10% starch slurry to make soft material, pass through a 14-mesh sieve, and dry after granulating;

[0044] (3) Pass through a 12-mesh sieve, granulate and then dry to obtain anti-Pseudomonas aeruginosa granules.

Embodiment 3

[0045] Embodiment 3 anti-pseudomonas aeruginosa capsules

[0046]

[0047]

[0048] The preparation steps of anti-pseudomonas aeruginosa capsules are:

[0049] (1) Take 10 mg of compound 2 in Example 1, first mix it with lactose for 10-15 minutes;

[0050] (2) Add microcrystalline cellulose and mix for 10-15 minutes;

[0051] (3) Add talcum powder and mix for 3-5 minutes;

[0052] (4) The mixture is packed into a gelatin capsule shell to obtain an anti-Pseudomonas aeruginosa capsule.

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Abstract

The present invention discloses an application of flavone oxygen glycoside compounds in preparations of bacterial quorum sensing inhibitory drugs. Structure of the compounds is as described in a formula I; wherein R1 is H, hydroxy or methoxy; R2 is hydroxy; R3 is H, hydroxy or galactoside; and R4 is hydroxy or galactoside. The present invention provides a novel use of the flavone oxygen glycosidein preparations of the bacterial quorum sensing inhibitory drugs. Experimental results show that the flavone oxygen glycoside can all inhibit biofilms of pseudomonas aeruginosa 9027, pseudomonas aeruginosa 27853 and drug resistance pseudomonas aeruginosa, show that the flavone oxygen glycoside compounds can inhibit the bacterial quorum sensing system to reduce bacterial virulence and pathogenicity, while bacterial growth is not inhabited and bacteria are not easy to produce the drug resistance of the bacteria, it is indicated that the flavone oxygen glycoside compounds can be prepared into a pseudomonas aeruginosa quorum sensing inhibitor.

Description

technical field [0001] The invention relates to the technical field of biomedicine, and more specifically, relates to the application of flavonoid oxyglycosides in the preparation of bacterial quorum sensing inhibitory drugs. Background technique [0002] With the widespread use of antibiotics, the resistance of microorganisms is getting higher and higher, and the resistance spectrum is getting wider and wider. The speed of drug resistance formation is proportional to the sterilization ability of antibiotics. Once resistance is established, it will persist. The continued use of antibiotics will only continue to provide selection pressure for highly drug-resistant strains, promoting their replication, organization, and sharing of drug-resistant genes, resulting in the accelerated formation of multi-drug resistant strains. At present, antibiotic resistance has become a serious public health problem worldwide. [0003] my country has extremely rich traditional Chinese medicin...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61P31/04
Inventor 郑俊霞杨超田文月王立抗黄家晋黄盈梁基铮赵肃清张焜李志明谢晓华张俊鑫冼志颖雷佩仪邝江林
Owner GUANGDONG UNIV OF TECH
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