Novel synthesis antibacterial peptides and application thereof

An antibacterial peptide and combination technology, which is applied in the field of new synthetic antibacterial peptides, can solve the problems of low yield, high cost, complicated process and the like of antibacterial peptides, and achieve the effects of broad antibacterial spectrum, simple structure and strong bactericidal activity.

Inactive Publication Date: 2012-05-02
CHONGQING UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since the content of antimicrobial peptides in animals is very small, the extraction of antimicrobial peptides from animals is low in yield, time-consuming, complicated and expensive, which has become the biggest obstacle restricting the practical application of antimicrobial peptides

Method used

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  • Novel synthesis antibacterial peptides and application thereof
  • Novel synthesis antibacterial peptides and application thereof
  • Novel synthesis antibacterial peptides and application thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0042] 1. Preparation of antimicrobial peptides (take the preparation of 0.1 mmol of WYQ-a as an example)

[0043] All the following reagents for the preparation of antimicrobial peptides were purchased from Applied Biosystems.

[0044] The prepared WYQ-a polypeptide sequence is: Arg-Arg-Trp-Trp-Arg-NH 2

[0045] The preparation is carried out one by one from the C-terminal to the N-terminal, and is automatically controlled by the synthesizer.

[0046]First, weigh 0.1 mmol of the resin combined with the first amino acid, Arg (purchased from Applied Biosystems, USA), and pack it into a column; then protect it with 20% piperidine dimethyl formamide solution and wash it with dimethyl formamide , the free amino acid protected by 9-hut methoxycarbonyl (Fmoc) is dissolved in carbodiimide (DCC), hydroxybenzotriazole (HOBt) / diisopropylethylamine (DIPEA), and the dissolved solution is on the column Coupling reaction in the upper cycle for 30 minutes, washing with trifluoroacetic aci...

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Abstract

The invention provides novel synthesis antibacterial peptides and application thereof. The novel synthesis antibacterial peptides are designed and synthesized on the basis of analyzing sequences and structures of natural antibacterial peptides, and the sequences of the novel synthesis antibacterial peptides comprise WYQ-a: ArgArgTrpTrpArg and WYQ-b: PheArgTrpTrpArg. The synthesis antibacterial peptides have the broad spectrum killing activity on gram-positive bacteria and gram-negative bacteria, have higher bactericidal activity than that of the natural antibacterial peptides, and do not have a toxic effect on animal and plant cells. The synthesis antibacterial peptides have broad antibacterial spectra and simple structures, are not needed to be modified and connected and are convenient to synthesize artificially. Experiments prove that: for G+bacteria (the gram-positive bacteria) and G-bacteria (the gram-negative bacteria), the novel synthesis antibacterial peptides have the obvious bacteriostatic and bactericidal activity and do not have hemolysis activity, so the synthesis antibacterial peptides have significant value in the development and application of antibacterial medicines.

Description

technical field [0001] The invention relates to a group of novel synthetic antibacterial peptides and their application in treating bacterial infection diseases. The series of antibacterial peptides have significant bactericidal activity on Gram-positive bacteria and Gram-negative bacteria. [0002] Background technique [0003] Since the invention of antibiotics, humans have made great achievements in the control and treatment of microbial infections, but with the continuous use of antibiotics, microbial resistance has become a major problem in microbial infection control, so that some microbial bacteria have no First-line drugs for controlled killing. For example, in clinical drug treatment, vancomycin-resistant Staphylococcus, Enterococcus and other Gram-negative bacterial infections are currently a worldwide clinical treatment problem. [0004] Antimicrobial peptides are a class of small molecular polypeptides widely present in microorganisms, animals and plants, usual...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06A61K38/08A61P31/04
Inventor 王远强林治华丁元蔡家利韩英子
Owner CHONGQING UNIV OF TECH
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