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Preparation and application of combined antibacterial peptide having high stability and anti-drug-resistance activity

A high-stability, antimicrobial peptide technology, applied in the field of biochemistry, can solve problems such as limited application, and achieve strong antibacterial activity, high stability, and strong anti-drug-resistant bacterial activity in clinical isolation.

Active Publication Date: 2016-03-30
倪京满 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Antimicrobial peptides are usually small molecule polypeptides composed of L-type amino acids. Since the body contains a variety of degrading enzymes, they can specifically bind to certain sites in the antimicrobial peptide sequence, causing the antimicrobial peptide to be degraded and inactivated in the body, which greatly limits the its application

Method used

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  • Preparation and application of combined antibacterial peptide having high stability and anti-drug-resistance activity
  • Preparation and application of combined antibacterial peptide having high stability and anti-drug-resistance activity
  • Preparation and application of combined antibacterial peptide having high stability and anti-drug-resistance activity

Examples

Experimental program
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Effect test

Embodiment 1

[0038] Embodiment 1, the synthesis of combination antimicrobial peptide J-RR-1

[0039] with H 2 O and DMF (100:1, V / V) are the reaction medium, CuSO 4 ·5H 2 O is catalyst (consumption is peptide Ac-Nle(N 3 )-RW-1 molar weight 10 times), sodium ascorbate is antioxidant (dosage is peptide Ac-Nle(N 3 )-RW-1 molar amount of 15 times), the purified peptide Ac-Pra-RW-1 and peptide Ac-Nle(N 3 )-RW-1 with a molar ratio of 1:1, after 24h of click chemical 1,3-dipolar cycloaddition reaction, the reaction solution was purified by RP-HPLC to obtain the target peptide J-RR-1, and the yield was 18.4%. The purity is 100.00%. The mass spectrum of the product is shown in figure 1 , the purity analysis chart see figure 2 .

Embodiment 2

[0040] Embodiment 2, the synthesis of combination antimicrobial peptide J-RR-1

[0041] with H 2 O and DMF (20:1, V / V) are the reaction medium, CuSO 4 ·5H 2 O is a catalyst (amount is peptide Ac-Nle(N 3 )-RW-1 molar weight 5 times), sodium ascorbate is antioxidant (dosage is peptide Ac-Nle(N 3 )-RW-1 molar amount 20 times), the purified peptide Ac-Pra-RW-1 and peptide Ac-Nle(N 3 )-RW-1 with a molar ratio of 2:1, after 28 hours of click chemical 1,3-dipolar cycloaddition reaction, the reaction solution was purified by RP-HPLC to obtain the target peptide J-RR-1, and the yield was 19.6%, yielding a purity of 100.00%. Spectrum see figure 1 , the purity analysis chart see figure 2 .

Embodiment 3

[0042] Embodiment 3, the synthesis of combination antimicrobial peptide J-RR-1

[0043] with H 2 O and DMF (10:1, V / V) are the reaction medium, CuSO 4 ·5H 2 O is a catalyst (amount is peptide AC-Nle(N 3 )-RW-1 molar weight 15 times), sodium ascorbate is antioxidant (dosage is peptide Ac-Nle(N 3 )-RW-1 molar amount 30 times), the purified peptide Ac-Pra-RW-1 and peptide Ac-Nle(N 3 )-RW-1 with a molar ratio of 5:1, after 26 hours of click chemical 1,3-dipolar cycloaddition reaction, the reaction solution was purified by RP-HPLC to obtain the target peptide J-RR-1, and the yield was 18.2%, the purity is 100.00%. The mass spectrum of the product is shown in figure 1 , the purity analysis chart see figure 2 .

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Abstract

The invention discloses a combined antibacterial peptide having high stability and anti-drug-resistance activity, and belongs to the biochemical technical field. With precursor peptides containing propargyl glycine and azide lysine as a substrate, CuSO4.5H2O as a catalyst, sodium ascorbate as an antioxidant, and a water-N,N-dimethyl formamide mixed liquid as a solvent, a 1,3-dipolar cycloaddition reaction of click chemistry is carried out for 24-28 hours, and a 1,4-disubstituted-1H-1,2,3-triazole structure is generated and links the two precursor peptide chains to obtain the product. Antibacterial experiments of common standard bacteria and clinically isolated drug-resistant bacteria indicate that the synthesized J-RR-1 peptide has relatively strong antibacterial activity and clinically isolated drug-resistant bacteria resisting activity, and also has relatively high stability on pancreatin. Therefore, the peptide has a good application prospect in preparation of clinical treatment drugs.

Description

technical field [0001] The invention belongs to the technical field of biochemistry and relates to a D-type amino acid combined antibacterial peptide, in particular to a D-type amino acid combined antibacterial peptide with high stability and anti-drug resistance activity and a preparation and synthesis method thereof. Background technique [0002] The widespread occurrence of infectious diseases is a serious threat to human health, and antibiotics are widely used as first-line drugs against infectious diseases. However, the abuse of antibiotics has led to the emergence of drug resistance, so the research and development of new antibacterial drugs has become a research hotspot in recent years. Antimicrobial peptides (Antimicrobial peptides) are important components in the innate immune effect, widely present in prokaryotes, plants, insects, amphibians and mammals, have the characteristics of broad antibacterial spectrum, high specificity and other biological activities, and ...

Claims

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Application Information

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IPC IPC(8): C07K7/06A61K38/08A61P31/04
CPCA61K38/00C07K7/06C07K19/00
Inventor 倪京满王锐王一杰黄海凤韩秀凤
Owner 倪京满
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