Cyclic antibacterial peptide and preparation method and application thereof

A technology of antimicrobial peptides and cyclic polypeptides, applied in the field of antibacterial agents, can solve the problems of low biosynthesis efficiency, in vivo activity and drug resistance, difficult protein separation, etc., achieve low MIC value, improve peptide stability, and antibacterial good effect

Active Publication Date: 2019-05-17
CHANGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although defensins are potential drug candidates, several hurdles still need to be addressed: 1) the protein is difficult to isolate; 2) the biosynthesis efficiency of defesins is low; 3) in vivo activity and drug resistance still need to be improved

Method used

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  • Cyclic antibacterial peptide and preparation method and application thereof
  • Cyclic antibacterial peptide and preparation method and application thereof
  • Cyclic antibacterial peptide and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] The method of the present invention adopts the conventional solid-phase Fmoc method, that is, the monomer amino acid protected by Fmoc on the solid-phase resin is deprotected to expose the amino group, and forms a peptide bond with the carboxyl group of the amino acid in the solution through a condensation reaction, thereby linking the amino acid to the On the resin, the peptide chain is extended from the C-terminus to the N-terminus.

[0029] 1. Basic materials:

[0030] (1) Resin and linking molecule: The resin selected by the solid-phase Fmoc method is Rink Amide- resin. This kind of resin has very good swelling property, which can make the condensation reaction between the peptide chains better, and there is enough network space to meet the growing peptide chains. HBTU and HOBt are used as linking molecules to immobilize the polypeptide molecules on the resin.

[0031] (2) Monomer: The monomer used in the synthesis is a chemically modified α-amino acid.

[0032...

Embodiment 2

[0057] The fourth step, repeat the second and third steps, add monomer amino acids repeatedly, according to KWKWHLLWRRCR D PPFRCWE 48 The order of RR sequences is synthesized from right to left until the synthesis is complete.

[0058] Other steps are the same as in Example 1, and the polypeptide sequence AM-23( figure 1 ).

[0059] The MIC value of the synthesized cyclic polypeptide is 4.46.

Embodiment 3

[0061] The fourth step, repeat the second and third steps, add monomer amino acids repeatedly, according to KWKWHLLWRRCR D PPFRCWE 58 The order of RR sequences is synthesized from right to left until the synthesis is complete.

[0062] Other steps are the same as in Example 1, and the polypeptide sequence AM-24( figure 1 ).

[0063] The MIC value of the synthesized cyclic polypeptide is 30.98.

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Abstract

The invention belongs to the technical field of antibacterial agents, and particularly relates to the cyclic antibacterial peptide and a preparation method and application thereof. The amino acid sequence of the cyclic antibacterial peptide is as shown in SEQ ID NO:1; the cyclic antibacterial peptide is an intramolecular cyclic polypeptide, wherein the proline located at a beta-corner of the polypeptide is replaced with DPRO-LPRO to improve the stability of the beta-corner, and an intramolecular cyclic structure is formed by forming an intramolecular cyclic disulfide bond between two cysteineresidues in the amino acid sequence. The antibacterial peptide has the advantages that the amino acid sequence is short, the structure is simple, the synthesizing is convenient, the antibacterial activity is high, and the antibacterial peptide can be used for preventing and treating diseases caused by candida albicans.

Description

technical field [0001] The invention belongs to the technical field of antibacterial agents, and in particular relates to a cyclic antibacterial peptide and its preparation method and application. Background technique [0002] The emergence of drug-resistant fungal pathogens urgently requires a new generation of antifungal drugs with improved pharmacokinetics and pharmacodynamics. Antimicrobial peptides (AMPs) are mainly cationic and amphiphilic peptides composed of less than 50 amino acids, produced by a variety of organisms, and used to kill various invading bacteria, fungi, and viruses, while having low cellularity to the organism itself. toxicity. Due to their novel mechanism of microbicidal action and drug resistance, they have been recognized as a gold mine of antimicrobial drugs. At present, there are limited types of antifungal drugs clinically, mainly antibiotics, but antibiotics are prone to drug resistance. [0003] Defensins are widely distributed antimicrobia...

Claims

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Application Information

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Patent Type & AuthorityApplications(China)
IPC IPC(8): C07K14/00C07K1/04A61K38/16A61P31/04
Inventor王建浩王建鹏滕一万贾文静邱琳蒋林伯雷晓玲刘晓骞
OwnerCHANGZHOU UNIV