Polypeptide compound with antimicrobial and anti-inflammatory activities

A technology of peptide compounds and drugs, applied in anti-inflammatory agents, antibacterial drugs, local antibacterial agents, etc., can solve the problems of high production cost, high difficulty in synthesis and purification, and limit the application of LL-37, so as to prevent and treat dental caries Effect

Active Publication Date: 2018-10-16
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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  • Polypeptide compound with antimicrobial and anti-inflammatory activities
  • Polypeptide compound with antimicrobial and anti-inflammatory activities
  • Polypeptide compound with antimicrobial and anti-inflammatory activities

Examples

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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 5 mg / 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 ...

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Abstract

The invention discloses a polypeptide compound with antimicrobial and anti-inflammatory activities and belongs to the technical field of biology. The polypeptide compound has an amino acid sequence ofIGKLFKRIVQLIK or IGKLFKRIVQLIL, named as IG-13-1 and IG-13-2 respectively. The polypeptide compound is a novel polypeptide compound which efficiently acts on bacterial membrane of Streptococcus mutans, inhibits activity of Streptococcus mutans and the formation of its biological membrane by interfering the integrity of the bacterial membrane, and therefore, prevents and treats dental caries. Antibacterial activity test shows that the two polypeptides have MIC value of 5.0 mu M, having antimicrobial rate prior to anti-caries drug CHX used often at present. It is worth notification: the biological membrane formation inhibition test shows that both IG-13-1 and IG-13-2 can inhibit the growth of the biological membrane of Streptococcus mutans when MBIC50 have the concentrations of 5.91+/-0.91and 7.58+/-0.23 mu M.

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 plays a key role in the occurrence and development of teeth. 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 against the host. Theref...

Claims

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Application Information

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Patent Type & Authority Applications(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
Owner SOUTHERN MEDICAL UNIVERSITY
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