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Application of 20(S)-ginsenoside Rh2 in preparation of drugs enhancing antibacterial action of 4-quinolones

A ginsenoside and quinolone technology, applied in pharmaceutical formulations, antibacterial drugs, medical preparations containing active ingredients, etc., can solve the mutation of drug target enzymes, the inability of the body's immune system to recognize and kill bacteria, and hinder drugs and bacteria Target binding, etc.

Inactive Publication Date: 2013-12-25
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, with the expansion of the application scale of quinolones, the problem of bacterial resistance to them has become increasingly serious and has gradually become a worldwide problem.
The main mechanism of quinolone antibiotic resistance is divided into 1) the bacteria themselves change to produce drug resistance, that is, the high expression of efflux transporters on the surface of the bacterial wall membrane, which leads to increased active efflux of antibiotics and hinders the drug from interacting with the target in the bacterium Combination, or drug target enzyme mutation; ②Bacteria enter the host cell, making the immune system unable to recognize and kill the bacteria or the drug cannot directly contact with the bacteria to produce drug effect
The emergence of drug resistance has greatly limited the clinical use of antibiotics. Therefore, in the case of high cost and difficulty in the development of new drugs, finding non-toxic drugs that can synergistically increase the efficacy of antibiotics has become another way to overcome bacterial resistance

Method used

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  • Application of 20(S)-ginsenoside Rh2 in preparation of drugs enhancing antibacterial action of 4-quinolones
  • Application of 20(S)-ginsenoside Rh2 in preparation of drugs enhancing antibacterial action of 4-quinolones
  • Application of 20(S)-ginsenoside Rh2 in preparation of drugs enhancing antibacterial action of 4-quinolones

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] Example 1: Therapeutic effect of Rh2 combined with ciprofloxacin on mouse abdominal infection model

[0012] Experimental materials: clean-grade ICR mice (provided by the Comparative Medicine Center of Yangzhou University), Staphylococcus aureus ATCC29213 was preserved by the Department of Microbiology, China Pharmaceutical University, Rh2 (purity > 98%) was purchased from the Department of Organic Chemistry, School of Pharmacy, Jilin University, environmental Profloxacin injection (Guangzhou Nanxin Pharmaceutical Co., Ltd.). Both MH broth medium and MH agar medium were purchased from Beijing Sanyao Technology Development Company.

[0013] experimental method:

[0014] 1. Bacterial solution preparation: Take the slant of fresh MRSA strain, inoculate it into fresh sterile MH nutrient broth, set it on a constant temperature shaker at 35°C and determine the species with the analysis system VITEK. 20(S)-Ginsenoside-Rh2 (purity>98%) was purchased from the Department of Org...

Embodiment 2

[0031] Embodiment 2: Rh2 combined with ciprofloxacin on the impact of the number of colonies in the blood in the mouse abdominal cavity infection model

[0032] Experimental material: same as embodiment 2

[0033] 1. Bacterial solution preparation, animal grouping, dosing regimen and bacterial inoculation method are the same as in Example 1.

[0034] 2. After tail vein administration of ciprofloxacin for 24 hours, remove eyeballs from mice in a sterile environment to get blood, take 0.5ml and carry out doubling dilution with sterile normal saline, take 1ml of the diluted bacterial solution for plate counting (n =3).

[0035] Experimental results:

[0036] The result is as image 3 , 4 Shown, compared with single-use ciprosa, Rh2 (25, 50, 100mg / kg) gavage one day ( image 3 ) and seven days ( Figure 4 ) combined with ciprofloxacin can significantly reduce the number of colonies in the blood. Group because the survival rate of mice did not meet the statistical requiremen...

Embodiment 3

[0037] Example 3: Rh2 in vitro synergistic antibacterial efficacy research

[0038] Experimental Materials:

[0039] Staphylococcus aureus ATCC29213 and Pseudomonas aeruginosa ATCC27853 were preserved by the Department of Microbiology, China Pharmaceutical University.

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Abstract

The invention relates to application of 20(S)-ginsenoside Rh2 in preparation of drugs enhancing antibacterial action of 4-quinolones. The invention discloses that 20(S)-ginsenoside Rh2 can improve the therapeutic effect of ciprofloxacin on a mouse abdominal infection model, and can reduce the minimal inhibitory concentration (MIC) of ciprofloxacin in staphylococcus aureus ATCC 29213, 4 staphylococcus aureus clinical strains, and pseudomonas aeruginosa ATCC 27853. On a staphylococcus aureus invaded THP-1 macrophage model, 20(S)-ginsenoside Rh2 can enhance the intracellular antibacterial action of levofloxacin. Therefore, 20(S)-ginsenoside Rh2 is expected to be used for preparing a synergist of quinolone antibiotics, and can be developed into assistant drugs of anti-infective therapy.

Description

technical field [0001] The invention relates to the field of natural medicines, in particular to the application of 20(S)-ginsenoside Rh2 in the preparation of medicines for enhancing the antibacterial effect of quinolones. Background technique [0002] Quinolones (4-quinolones), also known as pyroxic acids or pyridoxic acids, are a relatively new class of synthetic antibacterial drugs. The target enzymes of quinolones are bacterial DNA gyrase (gyrase) and topoisomerase IV. For most Gram-negative bacteria, DNA gyrase is the main target enzyme of quinolones, while for most Gram-positive bacteria, quinolones mainly inhibit bacterial topoisomerase IV, which is responsible for melting Enzyme that releases coiled daughter chromosomes during DNA replication. Quinolones have a wide antibacterial spectrum, especially have a strong bactericidal effect on aerobic Gram-negative bacilli including Pseudomonas aeruginosa, and have good antibacterial effects on Staphylococcus aureus and ...

Claims

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Application Information

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IPC IPC(8): A61K31/704A61P31/04A61K31/496A61K31/5383
Inventor 王广基孙渊周芳王瑶瑶张经纬查伟斌汪辉郝刚罗丹
Owner CHINA PHARM UNIV
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