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A biocompatible antimicrobial peptide with self-assembly potential, its preparation method and application

A biocompatible, antimicrobial peptide technology, applied to biocompatible antimicrobial peptides with self-assembly potential and their preparation and application fields, can solve the problems of low cytotoxicity of antibacterial activity and poor cell selectivity of natural antimicrobial peptides with strong toxicity

Active Publication Date: 2021-12-14
NORTHEAST AGRICULTURAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The object of the present invention is to provide a biocompatible antibacterial peptide F2I-LL with self-assembly potential and its preparation method and application. The antibacterial peptide has self-assembly ability, high antibacterial activity and low cytotoxicity; The problem of poor selectivity for toxic cells

Method used

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  • A biocompatible antimicrobial peptide with self-assembly potential, its preparation method and application
  • A biocompatible antimicrobial peptide with self-assembly potential, its preparation method and application
  • A biocompatible antimicrobial peptide with self-assembly potential, its preparation method and application

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Embodiment 1

[0012] Design and preparation of embodiment 1 antimicrobial peptide synthesis

[0013] Combining diphenylalanine dipeptide FF with Ile to introduce hairpin structure D The PG corner unit stabilizes the internal hydrophobic structure and makes it a hydrophobic assembly motif. Combined with the amino acid composition required for the design of antibacterial peptides, the positively charged amino acid arginine and the hydrophobic amino acid leucine are selected as repeating binary sequence units and distributed on both sides. On the other hand, to ensure the hydrophobicity and positive charge required for its antibacterial function, the antibacterial peptide F2I-LL was newly designed, and its amino acid sequence is shown in Table 1.

[0014] The amino acid sequence of table 1 antimicrobial peptide FI-LL

[0015]

[0016] The charge number of F2I-LL is +5, the hydrophobic value is 0.716, and the hydrophobic moment is 0.198. N-terminal acetylation increases stability by adding...

Embodiment 2

[0018] 1 Bacteriostatic activity of antimicrobial peptides

[0019] The peptide was configured as a 2.56mM / L storage solution for future use. The minimum inhibitory concentrations of several antimicrobial peptides were determined by the broth microdilution method. Using 0.01% acetic acid (containing 0.2% BSA) as the diluent, a series of gradient antimicrobial peptide solutions were sequentially prepared using the double dilution method. Take 100 μL of the above solution and place it in a 96-well cell culture plate, then add an equal volume of the bacteria solution to be tested (~10 5 individual / mL) in each well. Positive controls (containing bacterial fluid but not antimicrobial peptides) and negative controls (neither bacterial fluid nor peptides) were set up. Incubate at a constant temperature of 37°C for 18 hours, and the minimum inhibitory concentration is the one where no turbidity is seen at the bottom of the well with the naked eye. The results are shown in Table 2 ...

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Abstract

The invention provides a biocompatible antimicrobial peptide with self-assembly potential and its preparation method and application, which solves the problem of poor cell selectivity of the strong toxicity of the natural antibacterial peptide. This antimicrobial peptide contains hairpin structure D PG corner unit, its sequence is shown in SEQ ID No.1. The preparation method is: combine FF with Ile, introduce hairpin structure D The PG corner unit selects the positively charged amino acid arginine, and the hydrophobic amino acid leucine is distributed on both sides as a repeating binary sequence unit to ensure the hydrophobicity and positive charge required for its antibacterial function. The new design has a low assembly capacity Toxic and highly selective antimicrobial peptide F2I‑LL. The application of the antibacterial peptide in the preparation of drugs for treating Gram-positive bacteria or / and Gram-negative bacteria infectious diseases. The antibacterial peptide has a certain assembly ability, has strong antibacterial activity, and produces very low hemolysis on blood cells.

Description

technical field [0001] The invention specifically relates to a biocompatible antimicrobial peptide with self-assembly potential, its preparation method and application. Background technique [0002] The misuse and overuse of antibiotics has posed a great threat to human health, resulting in more and more serious problems of drug resistance. Therefore, it is imminent to develop other antibacterial substances. Antimicrobial peptides are promising drug candidates due to their nonspecific targeting of cell membranes and their broad-spectrum antibacterial activity. However, the widespread application and clinical use of antimicrobial peptides are still subject to some limitations, including severe toxicity to host cells, weak antibacterial activity, and poor cell selectivity. [0003] In recent years, new self-assembled antimicrobial peptides have become a research hotspot. Peptides form nano-aggregates such as nanofibers, nanotubes, vesicles and micelles through supramolecular...

Claims

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Application Information

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IPC IPC(8): C07K7/08C07K1/04A61K38/10A61P31/04
CPCC07K7/08A61P31/04A61K38/00
Inventor 单安山陈婷婷杨城义吕银凤
Owner NORTHEAST AGRICULTURAL UNIVERSITY
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