Compound with antibacterial effect and application of compound in preparing antibacterial agent

A compound and drug technology, applied in the preparation of antibacterial drugs, in the field of compounds with antibacterial effects, can solve the problems of poor water solubility, unstable chemical sites, and low bioavailability of andrographolide, and achieve the improvement of antibiotic antibacterial / Bacteriostatic effect, significant antibacterial/bacteriostatic activity, high bioavailability effect

Active Publication Date: 2019-02-22
ZHUZHOU QIANJIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, further studies have found that andrographolide has poor water solubility, multiple unstable chemical sites, less absorption and low bioavailability in the body, which greatly limits its application.
Moreover, the composition of diterpene lactones in Andrographis paniculata is complex, about 40 kinds have been found so far, and the subtle differences in the structure of different compounds will also make their efficacy vary greatly
[0004] At present, the active mechanism of diterpene lactones in Andrographis paniculata has not yet had definite research results. At the same time, there is an urgent need for new, high-efficiency, plant-derived antibacterial agents or antibiotic synergists in this field to avoid and treat infections targeting existing microbial sources. Drug-resistant bacterial infections caused by overuse of antibiotics

Method used

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  • Compound with antibacterial effect and application of compound in preparing antibacterial agent
  • Compound with antibacterial effect and application of compound in preparing antibacterial agent
  • Compound with antibacterial effect and application of compound in preparing antibacterial agent

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] The present embodiment provides a kind of preparation method of the compound shown in formula (I), comprises the following steps:

[0039] S1. According to the method under the Fuke Qianjin Capsule in the Pharmacopoeia of the People's Republic of China [1]Extract from Zhuzhou Qianjin Pharmaceutical Co., Ltd. and prepare 1.5kg of Fuke Qianjin Prescription Extract Dry Cream (FKQJ). This dry paste was extracted 8 times with 3 times the volume of EtOAc to obtain an EtOAc extract (FKQJE, 156g);

[0040] S2. Take the EtOAc extract (FKQJE, 142.2g) and mix the sample with silica gel, then go through silica gel (1kg, 200-300 mesh) column chromatography, cyclohexane-EtOAc (9:1, 8:2, 7:3, 6:4 , 5:5, v / v) gradient elution, TLC detection and merging of similar fractions, a total of 10 fractions were obtained, respectively named: Fr.1, Fr.2, Fr.3, Fr.4, Fr. 5. Fr.6, Fr.7, Fr.8, Fr.9, Fr.10, spare;

[0041] S3. the fraction Fr.5 (11g) collected in step S2 is removed pigment (MeOH:H...

Embodiment 2

[0051] Use Escherichia coli (ATCC25922), Staphylococcus aureus (ATCC29213), Enterococcus faecalis (ATCC29212), Pseudomonas aeruginosa (ATCC27853) and Acinetobacter baumannii (ATCC19606) as test bacteria, refer to CLSI microplate The antibacterial / bacteriostatic activity of the compounds were detected and verified by the method.

[0052] 1. Experimental method

[0053] 1) Bacterial culture: Cultivate the experimental bacteria with Mueller-Hinton (MH) broth medium, and when it grows for 8-12 hours to about 0.5 Mcfarland concentration (1×10 8 CFU) for backup. A sample solution and a positive control solution with a certain concentration were prepared, and the positive control was ampicillin (Amp) and kanamycin (Kan) two (water soluble).

[0054] 2) Prepare samples and dilute bacteria solution. The samples (drug Fr.5-1 and control compound 1, 2, 3 or 4) were prepared at 2000 μg / mL, and all were dissolved in DMSO. Dilute the bacterial solution reasonably to ensure that the fina...

Embodiment 3

[0070] Escherichia coli (ATCC25922), Staphylococcus aureus (ATCC29213) and Enterococcus faecalis (ATCC29212) were used as test bacteria to test the stability of the drug Fr.5-1 with reference to the microplate method of CLSI.

[0071] 1. Experimental method

[0072] The drug Fr.5-1 together with the reference compounds 1 to 4 in Example 2, ampicillin (Amp) and kanamycin (Kan) are all made into a 1g / mL mother solution with dmso, stored at room temperature for half a year, and detected Its MIC values ​​for Escherichia coli (ATCC25922), Staphylococcus aureus (ATCC29213) and Enterococcus faecalis (ATCC29212).

[0073] Concrete detection method is as embodiment 2.

[0074] 2. Experimental results

[0075] The experimental results are shown in Table 2.

[0076] Table 2 MIC values ​​(μg / mL) of 5 strains of test bacteria:

[0077]

[0078] The results show that the drug Fr.5-1 has better stability than the control compounds 1 to 4, long-term storage at room temperature h...

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PUM

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Abstract

The invention discloses a compound with an antibacterial effect and an application of the compound in preparing an antibacterial agent. A structural formula of the compound is defined as the formula (I) in the description. The compound has good antibacterial/bacteriostatic effects, can improve the antibacterial/bacteriostatic effects of antibiotics, has no toxic or side effects and has good safety. The compound is prepared by secondary development of traditional Chinese medicine by utilizing a modern technical means and extraction, separation and purification of the traditional Chinese medicine gynecological qianjin tablets or gynecological qianjin capsules. The compound is simple in structure, high in purity, good in stability, high in bioavailability, simple in extraction and separationmethod and easy to synthesize, can adapt to the industrial application of new drugs, provides a new direction for the development of antibacterial/bacteriostatic agent, and has broad application prospects.

Description

technical field [0001] The present invention relates to the field of efficacy of compounds, more specifically, relates to a compound with antibacterial effect and its application in the preparation of antibacterial drugs. Background technique [0002] Bacterial infection is an acute systemic infection caused by pathogenic bacteria or opportunistic pathogenic bacteria invading the blood circulation to grow and reproduce, producing toxins and other metabolites. Clinically, it is characterized by chills, high fever, rash, arthralgia, and hepatosplenomegaly. Some may have septic shock and migratory lesions. Before the advent of antibiotics, one-third of the world's people died of pneumonia, tuberculosis, enteritis and diarrhea caused by bacterial infections at the beginning of the last century. The emergence of antibiotics is an important achievement in the field of human public health. But now humans have come to the other extreme: the abuse of antibiotics has led to the emer...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61P31/04
CPCA61K31/365A61P31/04Y02A50/30
Inventor 李伏君龚云王康华杨秀伟凌勇根白璐郑元青付卡利赵毅
Owner ZHUZHOU QIANJIN PHARMA
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