A group of small peptides with anti-clinical multidrug-resistant bacteria and their derivatives and applications

A technology for multi-drug resistant bacteria and derivatives, applied in the field of small peptides and their derivatives and applications, can solve the problems of antimicrobial peptide hemolytic side effects, low antibacterial activity, hemolytic side effects, etc., achieve strong antibacterial effect and significant antibacterial effect effect, the effect of improving the survival rate

Active Publication Date: 2021-03-30
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are few attempts to directly use natural antimicrobial peptides as antibacterial drugs
The main reasons are: the antibacterial activity of many natural antimicrobial peptides is not high, and the yield is low; many antimicrobial peptides have strong hemolytic side effects
For example, melittin extracted from bee venom has strong antibacterial activity, but it also has hemolytic side effects, which limits the application of melittin as an antibacterial drug.

Method used

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  • A group of small peptides with anti-clinical multidrug-resistant bacteria and their derivatives and applications
  • A group of small peptides with anti-clinical multidrug-resistant bacteria and their derivatives and applications
  • A group of small peptides with anti-clinical multidrug-resistant bacteria and their derivatives and applications

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Solid Phase Synthesis of Antimicrobial Peptides and Their Derivatives

[0034] Antimicrobial peptides were synthesized by solid-phase synthesis using FMOC (9-fluorenylmethoxycarbonyl) as a protecting group. It was cleaved from the resin with 95% trifluoroacetic acid, 2.5% water and 2.5% triisopropylsilane (TIA). After repeated precipitation with diethyl ether, the polypeptide was purified by reverse-phase high-performance liquid chromatography. A C18 reverse-phase column was used in the purification: 0%-60% acetonitrile containing 0.05% trifluoroacetic acid was used as the mobile phase, and gradient elution was performed at a flow rate of 3 mL / min. Then the peptide was dissolved in oxidation buffer (100 mmol / L ammonium acetate, pH 8.5) at a concentration of 1 mg / mL, and stirred continuously at room temperature for 3 days to fully oxidize and fold to form disulfide bonds. Finally, it was purified to over 95% by reverse-phase HPLC and freeze-dried for use. C-terminally...

Embodiment 2

[0036] Determination of Antibacterial Activity

[0037] A polypeptide sample solution with a concentration of 6 mg / mL was prepared with sterilized physiological saline. The bacteria used in the test were inoculated in the nutrient broth, cultured at 37°C for 24 hours, diluted 1:105 times with sterile saline before use, and 12 bacterial culture tubes were taken and numbered, and nutrient meat was added to the first tube Add 1.8mL broth, and add 1.0mL broth to the remaining 11 tubes. Add 0.2mL of polypeptide solution to the first tube, mix well, take out 1.0mL and add it to the second tube, repeat this process, and dilute to the 12th tube in turn, add 0.2mL of bacterial solution to each tube, shake gently, place at 37 Cultivate for 24 hours. The lowest concentration of peptides for sterile growth is the minimum sample concentration (MIC) that inhibits bacterial growth. Table 1 shows the minimum inhibitory concentrations of antimicrobial peptide derivatives prepared in Example...

Embodiment 3

[0041] Determination of polypeptide hemolytic activity:

[0042]Human red blood cells were suspended in phosphate buffer (pH 7.4) to obtain red blood cell suspension (5% v / v). Dissolve the peptide in phosphate buffer to make about 5mg / mL stock solution, take 14 1.5mL centrifuge tubes, add 1mL peptide stock solution to the first centrifuge tube, add 0.5mL phosphate buffer to the other tubes solution, take 0.5mL peptide stock solution from the first tube and add it to the second tube, mix evenly with a micro mixer, then take 0.5mL solution from the second tube, add it to the third tube and mix evenly, and so on, That is, dilute to the 14th tube sequentially by doubling dilution method, discard 0.5mL, add 0.5mL prepared 5% red blood cell suspension to each tube until the final volume is 1.0mL, shake gently, and incubate in a 37°C incubator After 60 min, it was centrifuged at 4000 rpm for 10 minutes, and the supernatant was taken for colorimetry at 414 nm. Red blood cells suspend...

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Abstract

The invention relates to a small peptide with a function of resisting against clinic multiple resistant bacteria, a derivative and an application thereof. The small peptide comprises the sequence as shown in SEQ ID NO.1-6. The anti-bacterial peptide and the derivative thereof are degraded into amino acid so as to be absorbed and utilized by human body and no antibiotic remains. A solid-phase compounding method is adopted for preparing the anti-bacterial peptide and the derivative thereof with higher drug-fast bacteria resisting activity; the preparation method is simple; the compounding technology and the product quality are easily controlled; the peptide is suitable for large-scale industrial production; and meanwhile, the peptide is environment-friendly and is free from any harmful matters.

Description

technical field [0001] The present invention relates to a group of polypeptides and derivatives thereof, in particular to a group of small peptides with anti-clinical multidrug-resistant bacteria, derivatives and applications thereof. Background technique [0002] The discovery of antibiotics is of great significance in the history of human medicine. Its use has saved countless lives and increased human life expectancy by more than ten years. But with the widespread use of antibiotics, bacteria have gradually adapted and developed resistance to them. Although there are hundreds of antibiotics in clinical use at present, they are all small chemical molecules, and the newly developed antibiotics are generally structural modifications of them. It is difficult to solve the problem of bacterial resistance to antibiotics. With the emergence of drug-resistant bacteria, the development of new antibiotics against drug-resistant bacteria has become an international concern. [0003]...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K14/00A61K38/16A61P31/04A23K20/147A61K8/64A61Q19/00A23L33/18
CPCA23V2002/00A61K38/00A61K2800/10A23K20/147A23L33/18C07K14/00A23V2200/30A23V2250/55
Inventor 吴国球
Owner SOUTHEAST UNIV
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