Efficient alpha-helix antibacterial peptide GV and preparation method and application thereof

An antimicrobial peptide and α-helix technology, applied in the field of high-efficiency α-helix antimicrobial peptide GV and its preparation and application, can solve the problems of high cytotoxicity such as hemolysis

Inactive Publication Date: 2017-02-01
NORTHEAST AGRICULTURAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Melittin has broad-spectrum antibacterial activ

Method used

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  • Efficient alpha-helix antibacterial peptide GV and preparation method and application thereof
  • Efficient alpha-helix antibacterial peptide GV and preparation method and application thereof
  • Efficient alpha-helix antibacterial peptide GV and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0014] Using the α-helical peptide GRX2RX3RX2RG (X represents W, F, V, I, A and L) as a template to design a new α-helical peptide GW, GF, GV, GI, GA, GL.

[0015] Its amino acid sequence is:

[0016]

[0017]

[0018] The above two antimicrobial peptides were synthesized using a peptide synthesizer. The method was solid-phase chemical synthesis, and the specific steps were:

[0019] 1) The preparation of antimicrobial peptides is carried out one by one from the C-terminus to the N-terminus, and is completed by a peptide synthesizer. First, Fmoc-X (X is the first amino acid at the C-terminal of each antimicrobial peptide) is inserted into Wang resin, and then the Fmoc group is removed to obtain X-Wang resin; then Fmoc-Y-Trt-OH (9 -Fmoxy-trimethyl-Y, Y is the second amino acid at the C-terminus of each antimicrobial peptide); according to this procedure, it is synthesized from the C-terminus to the N-terminus until the synthesis is completed, and the side of the Fmoc gro...

Embodiment 2

[0025] The designed and synthesized antimicrobial peptides were compared and detected by in vitro antibacterial and hemolytic activity tests;

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Abstract

The invention relates to an efficient alpha-helix antibacterial peptide GV and a preparation method and application thereof. The antibacterial peptide GV is an antibacterial peptide with high cell selectivity and achieves an optimal point of junction of the antibacterial activity and cell toxicity of the antibacterial peptide. A sequence of the antibacterial peptide GV is represented by a sequence table SEQ ID No. 1. The preparation method comprises the following steps: (1) carrying out designing in accordance with alpha-helix peptide GRX2RX3RX2RG serves as a template, so as to obtain a brand-new antibacterial peptide GV, wherein X= V; (2) synthesizing a polypeptide crude product through a polypeptide synthesizer by a solid-phase chemical synthesis method; purifying the synthesized polypeptide by using out-phase high-performance liquid chromatography, and carrying out identification on the synthesized polypeptide by using electrospray mass spectrography, thereby preparing the polypeptide. The antibacterial peptide GV provided by the invention has relatively high bacteriostatic activity and relatively low hemolytic activity and is the highest in therapeutic index, thereby having great development potential.

Description

technical field [0001] The invention relates to a high-efficiency α-helical antibacterial peptide GV and its preparation method and application. Background technique [0002] Antimicrobial peptides, also known as antimicrobial peptides or peptide antibiotics, are a class of small molecule polypeptides produced by specific bacterial genes, with broad-spectrum antibacterial, antiviral, antifungal, antiparasitic and antitumor biological activities. Antimicrobial peptides are electrostatically attracted to negatively charged groups on the bacterial cell membrane through basic positively charged residues, and their hydrophobic amino acids are inserted into the lipid bilayer of the bacterial cell membrane, causing physical damage to the membrane and causing cell contents to extravasation and death. The action of antimicrobial peptides does not involve specific receptors, and it can quickly kill microorganisms without producing drug resistance. In addition, antimicrobial peptide ...

Claims

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Application Information

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IPC IPC(8): C07K7/08C07K1/20C07K1/04A61K38/10A61P31/04
CPCA61K38/00C07K7/08
Inventor 董娜陈志辉杨洋
Owner NORTHEAST AGRICULTURAL UNIVERSITY
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