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Linear antibacterial oligopeptide SLAP-S25 and application thereof

An oligopeptide and anti-bacterial technology, applied in the direction of anti-bacterial drugs, peptides, peptide/protein components, etc., can solve problems such as bacterial resistance, social panic, and human health threats

Active Publication Date: 2018-08-31
CHINA AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

If the problem of bacterial resistance is not properly controlled and resolved, it will pose a huge threat to human health and cause social panic

Method used

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  • Linear antibacterial oligopeptide SLAP-S25 and application thereof
  • Linear antibacterial oligopeptide SLAP-S25 and application thereof
  • Linear antibacterial oligopeptide SLAP-S25 and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1. Discovery and artificial synthesis of linear antimicrobial oligopeptide SLAP-S25

[0041] 1. Discovery of linear antimicrobial oligopeptide SLAP-S25

[0042]Through the bioinformatics analysis of a variety of linear antibacterial oligopeptide sequences, optimization of the peptide chain structure, and construction of a linear oligopeptide library, the antibacterial effects of the obtained linear oligopeptides and their combination with various antibacterial drugs (such as β-lactams, Synergistic antibacterial effect of tetracyclines, glycopeptides, quinolones, cyclic peptides and rifamycins), the inventors of the present invention obtained the linear oligolinear antibacterial oligopeptide SLAP-S25. The structural formula of the linear antimicrobial oligopeptide SLAP-S25 is shown in formula (I) (the nitrogen terminal 2,4-diaminobutyric acid is modified by acetylation, and the carbon terminal alanine is modified by amidation), and the molecular weight is 1229.10...

Embodiment 2

[0048] Embodiment 2, the mensuration of antibacterial activity of linear antibacterial oligopeptide SLAP-S25

[0049] See Table 1 for the strains to be tested.

[0050] Table 1

[0051]

[0052]

[0053] Note: a. Staphylococcus aureus ATCC No.29213, Bacillus subtilis ATCC No.6051, Escherichia coli ATCC No.25922, Salmonella enterica ATCC No.13076 and Pseudomonas aeruginosa (Pseudomonasaeruginosa) PAO1 ATCC No. 47085 is preserved in the American Type Culture Collection (abbreviated as ATCC, address: American Type Culture Collection (ATCC) 10801 University Boulevard Manassas, VA 20110 USA), and the public can obtain it from the American Type Culture Collection.

[0054] b. Staphylococcus aureus (Staphylococcusaureus) 215 (LZD R +cfr) carrying the drug resistance gene cfr and resistant to linezolid. Enterococcus faecalis (Enterococcus faecalis) VRE A4 is a vancomycin-resistant strain. Staphylococcus aureus (Staphylococcusaureus) MRSA T144 is methicillin-resistant Staphyl...

Embodiment 3

[0067] Embodiment 3, the synergistic effect of linear antimicrobial oligopeptide SLAP-S25 and antibacterial drugs

[0068]Tetracycline belongs to the tetracycline class of drugs. Vancomycin is a glycopeptide drug. Ofloxacin belongs to the quinolone class of drugs. Rifampicin belongs to the rifamycin class of drugs. Polymyxins belong to the class of cyclic peptide drugs. Ampicillin and imipenem are β-lactam drugs.

[0069] 1. The synergistic effect of linear antibacterial oligopeptide SLAP-S25 and antibacterial drugs

[0070] 1. Synergistic effect of linear antimicrobial oligopeptide SLAP-S25 and antibacterial drugs against Gram-negative bacteria

[0071] Antibiotics were tetracycline, vancomycin, ofloxacin, rifampin, polymyxin, or imipenem.

[0072] The checkerboard analysis method was used to detect the synergy between the linear antimicrobial oligopeptide SLAP-S25 and different antibacterial drugs. The test strain was Escherichia coli (Escherichia coli) B2 (NDM-5+mcr-1...

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Abstract

The invention discloses a linear antibacterial oligopeptide SLAP-S25 and an application thereof. The linear antibacterial oligopeptide SLAP-S25 is an oligopeptide obtained by acetylation modificationof a nitrogen terminal and amidation modification of a carbon terminal of the oligopeptide as shown in a sequence 1 in a sequence table which is described in the specification. Experiment results showthat the linear antibacterial oligopeptide SLAP-S25 has a certain bacteriostatic effect on a variety of gram-positive and gram-negative bacteria, has good synergistic effects with antibacterial drugs(like tetracycline, vancomycin, ofloxacin and rifampicin), can restore the sensitivity of polymyxin-resistant gram-negative bacteria to polymyxin, reinforces the sensitivity of klebsiella pneumoniaeto a variety of antibacterial drugs, is free of hemolysis, has good tissue compatibility, can effectively inhibit polymyxin drug-resistance bacteria, and can treat bacteremia. The linear antibacterialoligopeptide SLAP-S25 provided by the invention has the advantages of small molecular weight, simple structure, convenient large-scale synthesis and important application values.

Description

technical field [0001] The invention relates to the field of biotechnology, in particular to linear antibacterial oligopeptide SLAP-S25 and its application. Background technique [0002] Antibacterial drugs play a vital role in the treatment and control of microbial infection diseases, safeguarding the health of humans and animals. However, the problem of bacterial resistance caused by the large-scale and irregular use of antibacterial drugs is becoming more and more serious, resulting in the reduction or ineffectiveness of many antibacterial drugs against bacterial infections. In 2011, Gram-negative bacteria capable of producing NDM-1 and unreported pathogenic bacteria Shigella and Vibrio cholerae were found in South Asia; in the same year, community-associated methicillin-resistant Staphylococcus aureus (CA- MRSA); in 2015, plasmid-mediated polymyxin-resistant (MCR-1) Escherichia coli was discovered in China, and the "last line of defense" for the treatment of drug-resist...

Claims

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Application Information

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IPC IPC(8): C07K7/06A61K38/08A61P31/04
CPCA61K38/00A61P31/04C07K7/06
Inventor 朱奎沈建忠丁双阳刘源宋玫蓉
Owner CHINA AGRI UNIV
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