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Antibacterial hexapeptides and their derivatives and applications

A technology of peptide derivatives and drugs, 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: 2020-10-13
湖南湃洵生物科技有限公司
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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 hexapeptides and their derivatives and applications
  • Antibacterial hexapeptides and their derivatives and applications
  • Antibacterial hexapeptides and their derivatives and applications

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Chemically synthesized antimicrobial peptide a and antimicrobial peptide b and control antimicrobial peptide Lactoferricin B4-9.

[0021] Antimicrobial Peptide a:RRWWRW(Arg-Arg-Trp-Trp-Arg-Trp)

[0022] Antimicrobial peptide b: RRWWRW-PEA (Arg-Arg-Trp-Trp-Arg-Trp-β-phenethylamine)

[0023] 1. Preparation of antimicrobial peptide b (Arg-Arg-Trp-Trp-Arg-Trp-β-phenethylamine):

[0024] a. After washing the resin with 4 times the amount of DMF and drying it completely, add 10 mL of 20% (piperidine: DMF, mass ratio) mixed solution of piperidine and DMF, shake for 1 min and dry, then add 10 mL of 20% (piperidine: DMF) , mass ratio) piperidine, DMF mixed solution shake for 30min; dry the reaction vessel and wash the resin with 4 times the amount of DMF to ensure that there is no piperidine residue, check the resin particles with ninhydrin should be blue.

[0025] b. Add Fmoc protected amino acid (1mmol), 2.1mL 0.45M HBTM / HOBT (1mmol), 248uL DIEA (2mmol) solution to the resin...

Embodiment 2

[0031] Antibacterial activity detection of antimicrobial peptides

[0032] 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.

[0033] The antibacterial activities of synthetic antimicrobial peptide b and antimicrobial peptide a were detected by agar plate diffusion method, and the natural antimicrobial peptide Lfcin B 4-9 As a control, to evaluate the bactericidal activity of antimicrobial peptide b and antimicrobial peptide a in the present invention.

[0034] The antibacterial activity of antimicrobial peptides was determined by the following steps:

[0035] a. Bacterial recovery: Use an inoculation loop to pick appropriate amounts of Escherichia coli, Staphylococcus aureus, Acinetobacter baumannii, Pseudomonas aeruginosa, Enterococcus faecalis, MRSA, and single drug-resistant Acinetobacter baumannii (for Ceftazidim...

Embodiment 3

[0043] Example 3 Detection of antibacterial activity of synthetic antimicrobial peptides

[0044] 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.

[0045] The bactericidal activity of synthetic antimicrobial peptides was detected by 96-well plate method, and the natural antimicrobial peptide Lfcin B was used to detect the bactericidal activity. 4-9 As a control, to evaluate the antibacterial activity of antimicrobial peptides a and b.

[0046] The antibacterial activity of antimicrobial peptides was determined according to the following steps:

[0047] a. Sterilize Escherichia coli, Staphylococcus aureus, Acinetobacter baumannii, Pseudomonas aeruginosa, Enterococcus faecalis, MRSA, single-drug-resistant Acinetobacter baumannii, and multidrug-resistant Acinetobacter baumannii Culture on NA medium plate overnight, pic...

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Abstract

The invention discloses an antimicrobial hexapeptide. The antimicrobial hexapeptide has a sequence of Arg-Arg-Trp-Trp-Arg-Trp. The antimicrobial hexapeptide can be used in preparation of drugs for treating or preventing bacterial infection. The invention also provides an antimicrobial hexapeptide derivative. The antimicrobial hexapeptide derivative has a sequence of Arg-Arg-Trp-Trp-Arg-Trp-beta-phenylethylamine. The antimicrobial hexapeptide derivative can be used in preparation of drugs for treating or preventing bacterial infection. The bacterium is drug-resistant acinetobacter baumannii. The artificially designed synthetic antimicrobial hexapeptide and its phenylethylamine-modified product can be conveniently obtained by a solid phase synthesis method. The synthetic antimicrobial peptide and its derivative have broad spectrum killing activity to Gram-positive bacteria and Gram-negative bacteria, and particularly, the derivative exhibits stronger antibacterial activity to drug-resistant acinetobacter baumannii, has very small hemolytic toxicity and can be used in drugs for treatment or prevention of diseases caused by drug-resistant acinetobacter baumannii.

Description

technical field [0001] The invention relates to an antibacterial hexapeptide and derivatives thereof and their applications, belonging to the field of biotechnology. Background technique [0002] The number of bacterial infections in the world is as high as 1.5 billion every year, and 4.6 million of them die. Especially the high mortality rate caused by multidrug-resistant bacteria (MDRB) infection is a serious threat to public health. Europe and the United States spend up to 7 billion euros and 6.5 billion U.S. dollars a year on the prevention and control of bacterial infections, and developing countries have to pay a higher price for this. The rapid spread of MDRB infection in the world is closely related to the abuse of antibiotics and their research and development, that is, no new structural types of antibiotics were developed from 1962 to 2000; only 3 new structural types of antibiotics have entered the market since 2000. The Infectious Diseases Society of America (ID...

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 王远强唐光辉张玉萍周朋朋高阳阳胡勇林治华
Owner 湖南湃洵生物科技有限公司
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