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Application of a kind of multi-armed AIE molecule in the preparation of antibacterial drugs and antibacterial drugs

An antibacterial drug and a multi-arm technology, applied in the field of antibacterial, can solve the problems of high toxicity of antibacterial polymers, low antibacterial ability, low bactericidal concentration and bactericidal concentration, achieve good bacteriostatic and bactericidal activities, promote wound healing, The effect of good treatment

Active Publication Date: 2022-05-24
SOUTH UNIVERSITY OF SCIENCE AND TECHNOLOGY OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Among them, natural antibacterial substances have been fully explored by people, so the screening rate of natural antibacterial substances is slow and the yield is low; the derivatives of antibiotics are designed and synthesized according to the structure of traditional antibiotics, and they are the same or similar to the antibacterial mechanism of traditional antibiotics, so it is easy to Cross-resistance occurs; antibacterial polymers are highly toxic and poorly soluble, and cannot be directly used for in vivo treatment of infectious diseases; the stability, toxicity, and in vivo drug metabolism of antibacterial nanoparticles need to be further studied
[0005] CN 104224776A discloses the use of tetraphenylethylene derivatives in the preparation of antibacterial drugs, and CN104224775A discloses a pharmaceutical composition containing tetraphenylethylene derivatives, but the minimum inhibitory concentration and minimum The minimum bactericidal concentration is 0.08μg / mL, and the antibacterial ability is low

Method used

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  • Application of a kind of multi-armed AIE molecule in the preparation of antibacterial drugs and antibacterial drugs
  • Application of a kind of multi-armed AIE molecule in the preparation of antibacterial drugs and antibacterial drugs
  • Application of a kind of multi-armed AIE molecule in the preparation of antibacterial drugs and antibacterial drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Minimum inhibitory concentration (MIC) determination of multi-arm AIE molecules:

[0056] The multi-arm AIE molecule is added to the DMSO (concentration is 4096 μg / mL), sonicates so that the molecule is sufficiently dissolved, and then the DMSO solution of the resulting multi-arm AIE molecule is rapidly diluted to 8 μg / mL with ultrapure water, for later use. Replace different multi-arm AIE molecules to obtain different multi-arm AIE molecular solutions.

[0057] Seven different gram-positive bacteria S.aureus, MRSA, S. epidermidis, MRSE, B. subtilis, E.faecium and MDR E.faecium and seven different gram-negative bacteria E.coli, P.aeruginosa, K.peneumoniae, A.baumani, MDR E.coli, MDR P.aeruginosa, MDRK.peneumoniae for the assay. Add 100 μL of bacterial medium to each well of the 96-well plate, then add 100 μL, 8 μg / mL of multi-arm AIE molecular solution to the first well of each row, mix well and take 100 μL and add it to the second well, and dilute it gradient to the 11th w...

Embodiment 2

[0064] Bacteriostatic activity testing of multi-armed AIE molecules:

[0065] Molecules 8, 9, 15, 21 and 25 were selected for testing. Set the concentration to 10 4 MrsA bacteria cfu / mL were cultured in LB medium (polygynical AIE molecules with a final concentration of 0.25 μg / mL) and ordinary LB medium (control group) added to the multi-arm AIE molecule, and the absorbance (OD) of the bacterial liquid at 600 nm was determined with a UV spectrophotometer at different time points (4, 8, 12, 16, 20 and 24 h). 600 The greater the absorbance, the greater the number of bacteria. Draw the OD 600 Curves that change over time, as a bacterial growth curve, result as in Figure 1 as shown.

[0066] The results showed that the OD of the bacterial fluid with the addition of multi-arm AIE molecules 600 The values did not change after 24 h, compared with the OD of the control group 600 The value is significantly higher, indicating that the multi-arm AIE molecule can effectively inhibit bacterial...

Embodiment 3

[0068] Bactericidal activity test of multi-arm AIE molecules:

[0069] Molecules 8, 9, 15, 21 and 25 were selected for testing. Dilute MRSA bacteria with LB medium to a concentration of 10 6 Cfu / mL or so, and then add multi-arm AIE molecular solution (final concentration of 2 μg / mL, without adding drug group as a control group) to the bacterial liquid, culture in a shaking chamber at 37 °C, respectively, at 4, 8, 12, 16 and 24 h, take part of the bacterial solution on the solid medium, incubate at 37 °C for 24 h, and record the number of colonies. Calculate the bacterial concentration change according to the number of colonies, and plot the change curve of bacterial concentration over time as a sterilization curve, as a result Figure 2 as shown.

[0070] composed Figure 2It can be seen that the number of bacteria in the control group increased with time and remained basically unchanged after 12h, while the number of bacteria in the bacterial liquid with the addition of multi-arm A...

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Abstract

The invention provides the use of a multi-arm AIE molecule in the preparation of antibacterial drugs and the antibacterial drugs. The multi-arm AIE molecule refers to a multi-arm AIE molecule having a core structure and at least two conjugated rigid arm structures connected to the core structure. The antibacterial drug includes at least one of the above-mentioned multi-armed AIE molecules and a dispersion medium. The present invention found that AIE molecules with multiple conjugated rigid arm structures can insert their conjugated rigid arm structures into the cell wall of bacteria, and affect the synthesis of bacterial cell walls by hindering the process of transglycosylation and transpeptidation, thereby inhibiting or killing bacteria . Antibacterial drugs prepared from this multi-armed AIE molecule have broad-spectrum antibacterial functions, can effectively inhibit bacterial growth, kill high-concentration bacteria, and can remove bacteria in mature biofilms to treat in vivo infections caused by multidrug-resistant bacteria.

Description

Technical field [0001] The present invention belongs to the field of antibacterial technology, specifically relates to the use of a multi-armed AIE molecule in the preparation of antibacterial drugs and antibacterial drugs. Background [0002] Pathogenic bacteria are important factors in causing nosocomial infections and community infections, causing a variety of diseases such as skin and soft tissue infections, osteomyelitis, endocarditis, pneumonia, bacteremia, and even sepsis. Existing drugs for the treatment of bacterial infections include β-lactams, macrolyclides, tetracyclines, peptides, and quinolones. But with the widespread use of these drugs, bacteria have developed severe resistance, threatening clinical anti-infective treatments. Therefore, the search for and development of new antimicrobial drugs is an urgent and important need to address bacterial resistance and ensure the health of human health. [0003] At present, people develop new antibacterial drugs mainly thr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/194A61K31/4192A61K31/136A61K31/444A61K31/185A61K31/505A61K31/53A61K31/196A61K31/385A61K31/409A61K31/14A61P31/04A61P17/02A61P11/00A01N37/10A01N37/40A01N43/647A01N33/06A01N43/40A01N41/04A01N33/12A01N43/54A01N43/66A01N37/44A01N43/28A01N43/90A01P1/00A61K8/368A61K8/41A61K8/44A61K8/46A61K8/49A61Q19/00
CPCA61K31/194A61K31/4192A61K31/136A61K31/444A61K31/185A61K31/505A61K31/53A61K31/196A61K31/385A61K31/409A61K31/14A61P31/04A61P17/02A61P11/00A01N37/10A01N37/40A01N43/647A01N33/06A01N43/40A01N41/04A01N33/12A01N43/54A01N43/66A01N37/44A01N43/28A01N43/90A61K8/368A61K8/496A61K8/411A61K8/4926A61K8/466A61K8/416A61K8/4953A61K8/4966A61K8/445A61K8/4986A61K8/494A61Q19/00A61K2800/524A61K2800/10
Inventor 蒋兴宇贾跃晓唐荣冰
Owner SOUTH UNIVERSITY OF SCIENCE AND TECHNOLOGY OF CHINA
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