Micromolecule synthesized anti-microbial peptide, as well as preparation method and application thereof

An antimicrobial peptide and small molecule technology, which is applied in the field of small molecule synthesis of antimicrobial peptide and its preparation, can solve the problems of low antibacterial activity, complex structure, high hemolytic toxicity, etc., and achieve good antibacterial effect, low hemolysis rate, and low hemolytic toxicity. Effect

Inactive Publication Date: 2015-01-21
SOUTHWEST UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the currently disclosed cationic antimicrobial peptides have complex structures, low antibacterial activity and high hemolytic toxicity. Therefore, it is urgent to develop cationic antimicrobial peptides with simple structure, high antibacterial activity, easy chemical synthesis and low hemolytic toxicity.

Method used

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  • Micromolecule synthesized anti-microbial peptide, as well as preparation method and application thereof
  • Micromolecule synthesized anti-microbial peptide, as well as preparation method and application thereof
  • Micromolecule synthesized anti-microbial peptide, as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] (1) Preparation of small molecule synthetic antimicrobial peptides (take the preparation of 0.1 mmol as an example):

[0033] The preparation is carried out one by one from the N-terminal to the C-terminal, and is automatically controlled by the pioneer peptide synthesizer. First weigh 0.1 mmol of the resin combined with the first amino acid, i.e. Arg (purchased from Applied Biosystems, USA), pack it into a column, and then use 20% (v / v) piperidine dimethylformamide solution for deprotection, and then Washed with dimethylformamide, the amino acid Arg protected with 9-Fat methoxycarbonyl (Fmoc) was dissolved in carbodiimide (DCC), and hydroxybenzotriazole (HOBt) / diisopropylethyl Amine (DIPEA), the dissolved solution was circulated on the column for coupling reaction for 30 minutes, washed with trifluoroacetic acid (TFA), and the above deprotection to coupling reaction steps were repeated until all amino acids in the SQ1 sequence were inserted, and the preparation was com...

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Abstract

The invention discloses a micromolecule synthesized anti-microbial peptide, as well as a preparation method and application thereof. The sequence of a cationic anti-microbial peptide is SQ1: R-W-W-R-F-NH2 (Arg-Arg-Trp-Trp-Arg-NH2), and the preparation method is the solid-phase chemosynthesis method. The micromolecule synthesized anti-microbial peptide has broad-spectrum cytotoxicity to gram-positive bacteria and gram-negative bacteria, has stronger bactericidal activity than a natural anti-microbial peptide, is simple in structure, convenient for artificial synthesis without any modification and connection, has the advantages of small hemolytic toxicity and no poison effects on animal and plant cells, and has an important value in development and application of antimicrobial agents.

Description

technical field [0001] The invention belongs to the technical field of biopharmaceuticals, and in particular relates to a small molecule synthetic antibacterial peptide and its preparation method and application. [0002] Background technique [0003] Since the invention of antibiotics, humans have made great achievements in controlling and treating microbial infections. However, with the continuous use of antibiotics, microbial resistance has become a major problem in microbial infection control, so that some microbial bacteria have no control to kill substances, such as in clinical drug treatment, vancomycin-resistant grapes coccus, enterococci, and other Gram-negative bacterial infections, and the treatment of these diseases is a worldwide problem. [0004] Antimicrobial peptides are a class of small molecular polypeptides widely present in microorganisms, animals and plants, usually composed of more than 30 amino acid residues, with a molecular weight of 2-7KDa. The b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06C07K1/20C07K1/06C07K1/04A61K38/08A61P31/04
Inventor 王远强周朋朋夏庆友赵萍林治华丁元钟晓武
Owner SOUTHWEST UNIVERSITY
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