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Antibacterial pentapeptide derivatives and their applications

A peptide derivative and drug technology, applied in the direction of antibacterial drugs, peptides, peptide/protein components, etc., can solve the problems of poor enzyme resistance and stability, cytolytic toxicity, easy degradation, etc., and achieve low hemolytic toxicity and broad-spectrum killing activity. , the effect of strong antibacterial activity

Active Publication Date: 2020-09-04
CHONGQING UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, natural AMP still has problems such as long amino acid sequence, high production cost, poor enzyme resistance stability, easy degradation in vivo, and cytolytic toxicity, etc., which face serious difficulties in clinical application.

Method used

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  • Antibacterial pentapeptide derivatives and their applications
  • Antibacterial pentapeptide derivatives and their applications
  • Antibacterial pentapeptide derivatives and their applications

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Chemical synthesis of antimicrobial peptide a and antimicrobial peptide b and control antimicrobial peptide Lactoferricin B 4-9 .

[0018] Antimicrobial peptide a: RRWWR-NH 2 (Arg-Arg-Trp-Trp-Arg-NH 2 )

[0019] Antimicrobial peptide b: RRWWR-PEA (Arg-Arg-Trp-Trp-Arg-β-phenylethylamine)

[0020] 1. Antimicrobial peptide a (Arg-Arg-Trp-Trp-Arg-NH 2 ) preparation:

[0021] The preparation is carried out one by one from the C-terminal to the N-terminal, and is automatically controlled by the synthesizer.

[0022] First, weigh 0.01mol of the resin combined with the first amino acid, namely Arg (purchased from Applied Biosystems, USA), and pack it into a column; then protect it with 20% piperidine dimethylformamide solution, wash it with dimethylformamide, 9-Fat methoxycarbonyl (Fmoc)-protected free amino acids were dissolved in carbodiimide (DCC), hydroxybenzotriazole (HOBt) / diisopropylethylamine (DIPEA), and the dissolved solution was placed on the column Cycle the ...

Embodiment 2

[0034] Detection of Antibacterial Activity of Antimicrobial Peptides

[0035] The various standard strains used below were purchased from the Guangdong Provincial Microbial Culture Collection Center and the drug-resistant bacteria were provided by the Third Military Medical University.

[0036] The antibacterial activity of synthetic antimicrobial peptide b was detected by agar plate diffusion method, and the antibacterial activity of natural antimicrobial peptide LfcinB 4-9 And antimicrobial peptide a as contrast, to evaluate the bactericidal activity of antimicrobial peptide b in the present invention.

[0037] Measure the antibacterial activity of antimicrobial peptides according to the following steps:

[0038] a. Strain recovery: Pick appropriate amount of Escherichia coli, Staphylococcus aureus, Acinetobacter baumannii, Pseudomonas aeruginosa, Enterococcus faecalis, MRSA, single-drug resistant Acinetobacter baumannii (for Ceftazidime-resistant, the same below), and mul...

Embodiment 3

[0046] The bacteriostatic activity detection of embodiment 3 synthetic antimicrobial peptides

[0047] The various standard strains used below were purchased from the Guangdong Microbial Culture Collection Center, and the drug-resistant bacteria were provided by the Third Military Medical University.

[0048] The bactericidal activity of synthetic antimicrobial peptides was detected by 96-well plate method, and the natural antimicrobial peptide Lfcin B 4-9 As a control, to evaluate the antibacterial activity of antimicrobial peptides a and b.

[0049] Measure the antibacterial activity of antimicrobial peptides according to the following steps:

[0050] Experimental steps:

[0051] a. Escherichia coli, Staphylococcus aureus, Acinetobacter baumannii, Pseudomonas aeruginosa, Enterococcus faecalis, MRSA, single-drug-resistant Acinetobacter baumannii, and multidrug-resistant Acinetobacter baumannii were sterilized Cultivate overnight on the NA medium plate, pick a single colony...

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Abstract

The invention discloses an antibacterial pentapeptide derivative and application thereof. The sequence of the antibacterial pentapeptide derivative is Arg-Arg-Trp-Trp-Arg-beta-phenethylamine. The antibacterial pentapeptide derivative is applied to a medicament for treating or preventing bacterial infection. The bacterium is multi-drug resistant acinetobacter baumannii. The novel antibacterial pentapeptide derivative synthesized by artificial design, provided by the invention, can be conveniently obtained by a solid-phase synthesis method. The synthesized antibacterial peptide has wide spectrum killing activity for gram-positive bacteria and gram-negative bacteria, particularly shows higher antibacterial activity for the multi-drug resistant acinetobacter baumannii, is extremely-low in hemolytic toxicity, and can be applied to medicaments for treating or preventing diseases caused by the multi-drug resistant acinetobacter baumanni.

Description

technical field [0001] The invention relates to an antibacterial pentapeptide derivative and application thereof, belonging to the field of biotechnology. Background technique [0002] There are as many as 1.5 billion bacterial infections worldwide each year, including 4.6 million deaths, especially the high mortality rate caused by multi-drug resistant bacteria (MDRB) infections, which seriously threatens public health. Europe and the United States spend as much as 7 billion euros and 6.5 billion U.S. dollars on the prevention and treatment of bacterial infections each year, while developing countries need to bear a higher price for this. The rapid spread of MDRB infection in the world is closely related to the misuse of antibiotics and their research and development. That is, no new structural type of antibiotics was developed between 1962 and 2000; since 2000, only three new structural types of antibacterial drugs have entered the market. The Infectious Diseases Society ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K7/06A61K38/08A61P31/04
CPCA61K38/00C07K7/06
Inventor 王远强张玉萍唐光辉周朋朋高阳阳胡勇林治华
Owner CHONGQING UNIV OF TECH
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