Peptide compounds with antibacterial and anti-inflammatory activities

A technology of peptide compounds and drugs, applied in anti-inflammatory agents, antibacterial drugs, local antibacterial agents, etc., can solve problems such as high production costs, high difficulty in synthesis and purification, and limited application of LL-37

Active Publication Date: 2021-08-17
SOUTHERN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] LL-37 is a polypeptide with 37 amino acid residues, which has high antibacterial activity against various bacteria and fungi, and even has an inhibitory effect on bacterial biofilms, but due to its 37 amino acid residues, its synthesis and Difficult to purify and expensive to produce
These factors limit the application of LL-37 in caries prevention and treatment

Method used

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  • Peptide compounds with antibacterial and anti-inflammatory activities
  • Peptide compounds with antibacterial and anti-inflammatory activities
  • Peptide compounds with antibacterial and anti-inflammatory activities

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] 1. Experimental method

[0033] 1.1 Polypeptide synthesis

[0034]The standard Fmoc solid-phase synthesis method 1 was used for peptide synthesis, Rink Amide MHBA resin was selected to synthesize peptides in ABI 433A peptide synthesizer, and the purified peptide (85.0%-90.0%) was completely dissolved in sterile deionized water at a concentration of 5mg / mL , and stored in a freezer at 4°C; the amino acid of the Fmoc protecting group needs an 8-fold excess; HBTU and HOBt are in an 8-fold excess, and DIEA is in a 16-fold excess. DMF is used as a solvent to dissolve HBTU, HOBt, and DIEA. After the last amino acid is condensed completely, a 10-fold excess fatty acid reaction is connected to the resin, and the reaction conditions are standard amino acid coupling reaction conditions. The synthesized lipopeptide is cleaved from the resin with the M reagent, the M reagent is trifluoroacetic acid: ethanedithiol: sulfide anisole: water = 100:1:2:2, the reaction time is 3h, and th...

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Abstract

The invention discloses a polypeptide compound with antibacterial and anti-inflammatory activities, belonging to the field of biotechnology. The amino acid sequence of the polypeptide compound is: IGKLFKRIVQLIK or IGKLFKRIVQLIL, respectively denoted as IG-13-1 and IG-13-2. This is a new type of polypeptide compound that effectively acts on the bacterial membrane structure of Streptococcus mutans, inhibits the activity of Streptococcus mutans and the formation of its biofilm by interfering with the integrity of the bacterial membrane, thereby preventing and treating dental caries. The antibacterial activity test showed that the MIC value of the two peptides was 5.0 μM, and their bactericidal rate was better than CHX, an anti-caries drug widely used at present. Notably, biofilm formation inhibition assays showed that IG‑13‑1 and IG‑13‑2 were 50 Both the concentrations of 5.91±0.91 and 7.58±0.23 μM can inhibit the growth of Streptococcus mutans biofilm.

Description

technical field [0001] The invention belongs to the field of biotechnology, and in particular relates to a polypeptide compound with antibacterial and anti-inflammatory activities. Background technique [0002] Dental caries is one of the most common chronic infectious diseases with the highest incidence and wide distribution in the world. Lesions that are left untreated may gradually develop into deep cavities, resulting in complete destruction of the crown. [0003] At present, a large number of studies have shown that Streptococcus mutans ( Streptococcus mutans ) plays a key role in tooth occurrence and development. Among them, the formation of adhesive bacterial biofilm is one of the main pathogenic mechanisms in which Streptococcus mutans participates in pathogenicity. Biofilms can allow bacteria to adhere to tooth surfaces and protect them from harmful stimuli, thereby reducing bacterial susceptibility to antibiotics and increasing bacterial immune resistance agains...

Claims

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Application Information

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Patent Type & AuthorityPatents(China)
IPC IPC(8): C07K7/08A61K38/10A61P1/02A61P31/04A61P31/02A61P29/00A61K8/64A61Q11/00
CPCA61K8/64A61K38/00A61Q11/00A61P1/02A61P29/00A61P31/02A61P31/04C07K7/08
Inventor何坚陈昭
OwnerSOUTHERN MEDICAL UNIVERSITY