Application of phthalide compounds in the preparation of anti-drug-resistant bacteria drugs

A compound and phthalide technology, applied in the application field of phthalide compounds in the preparation of anti-drug-resistant bacteria, can solve the literature report that no phthalide-type compounds are found to resist drug-resistant bacteria and inhibit bacterial quorum sensing system and other issues to avoid the problem of antibiotic resistance

Active Publication Date: 2022-04-22
GUANGDONG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It was first recorded in "Shen Nong's Materia Medica" and listed as a Chinese product. Its unique medicinal effect has always been a treasure for doctors. It is known as "ten directions and nine returns". Angelica extract contains a variety of chemical components, such as phthalides Donggui phthalide, n-butylphthalide, butylenephthalide, cnidolide, etc. Systematic review of the literature on Angelica sinensis found that modern pharmacology and clinical research also show that Angelica sinensis has good antibacterial and anti-inflammatory effects, but no Bibliographical reports of phthalide compounds in Angelica sinensis extract against drug-resistant bacteria and inhibiting bacterial quorum sensing system

Method used

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  • Application of phthalide compounds in the preparation of anti-drug-resistant bacteria drugs
  • Application of phthalide compounds in the preparation of anti-drug-resistant bacteria drugs
  • Application of phthalide compounds in the preparation of anti-drug-resistant bacteria drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Embodiment 1: Biofilm inhibition experiment of phthalide compounds

[0019] Test compound: take furanone compound (Z)-4-bromo-5-(bromomethylene)-2(5H)-furanone as positive control, and DMSO as negative control, positive drug and formula I of the present invention - The phthalide compounds of the formula X were formulated at 32, 64, and 128 μg / mL, respectively.

[0020] 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 bacteria. After drying or drying in an oven, add 220ul of crystal violet with a concentration of 1%, leave it at room temperature for 30min, then carefully wash...

Embodiment 2

[0025] Embodiment 2 anti-pseudomonas aeruginosa capsules

[0026]

[0027] The preparation steps of anti-pseudomonas aeruginosa capsules are:

[0028] (1) The compound of formula I is first mixed with lactose for 10-15 minutes;

[0029] (2) Add microcrystalline cellulose and mix for 10-15 minutes;

[0030] (3) Add talcum powder and mix for 3-5 minutes;

[0031] (4) The mixture is packed into a gelatin capsule shell to obtain the anti-Pseudomonas aeruginosa capsule of the present invention.

Embodiment 3

[0032] Embodiment 3 anti-drug resistant Pseudomonas aeruginosa tablet

[0033]

[0034] The preparation steps of anti-drug-resistant Pseudomonas aeruginosa tablet are:

[0035] (1) The compound of formula III is first mixed with lactose for 10-15 minutes;

[0036] (2) Add 10% starch slurry to make soft material, pass through a 14-mesh sieve, dry after granulation, and pass through a 12-mesh sieve for granulation;

[0037] (3) Then add crospovidone and magnesium stearate, mix for 3-5 minutes;

[0038] (4) After mixing uniformly, tableting is obtained to obtain the anti-drug resistant Pseudomonas aeruginosa tablet of the present invention.

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Abstract

The present invention relates to the application of phthalide compounds against Pseudomonas aeruginosa and drug-resistant Pseudomonas aeruginosa, and the experimental results show that phthalides compounds have biofilm effects on Pseudomonas aeruginosa and drug-resistant Pseudomonas aeruginosa The inhibitory effect is similar to or even better than positive drugs, so as to exert its inhibitory effect on anti-Pseudomonas aeruginosa and drug-resistant Pseudomonas aeruginosa, which helps to avoid the problem of antibiotic resistance.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to the application of phthalide compounds in the preparation of drugs against drug-resistant bacteria. 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] In my country, the abuse of antibiotics leads to an increase of 80 billion yuan in ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/365A61P31/04
CPCA61K31/365
Inventor 郑俊霞郅慧王珊时伟朋黄鹏李鹏举徐怀双张焜赵肃清
Owner GUANGDONG UNIV OF TECH
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