CN-121974983-A - Antibacterial peptide, preparation method and application thereof in preventing and treating oral problems

Abstract

The invention discloses an antibacterial peptide, a preparation method and application thereof in preventing and treating oral problems, and belongs to the technical field of antibacterial peptides. The amino acid sequence of the antibacterial peptide is FIRLLKSAGKAIHKLIRRGH. In vitro experiments show that the composition has broad-spectrum antibacterial activity on oral pathogenic bacteria such as fusobacterium nucleatum, porphyromonas gingivalis, streptococcus mutans and the like, has the minimum antibacterial concentration of 31.25-125 mug/mL, has no obvious hemolysis, has a therapeutic index of 50.79, has high cell selectivity, plays a certain role in protecting and resisting inflammation in a Pg-induced human gingival fibroblast in-vitro inflammatory model, and has a certain role in potentially inhibiting gingivitis of oral cavity. The invention provides an important research and development thought for the development of novel oral disease treatment medicines and nursing products, and has good application prospect.

Inventors

• FENG QIANG
• LIU BIN
• SONG WENZHU
• MENG LEI
• LIU XU
• GU XIUFENG
• WANG PEIYU

Assignees

• 山东大学
• 上海芒歌科技有限公司

Dates

Publication Date

20260505

Application Date

20260403

Claims (10)

1. 1. The antibacterial peptide is characterized in that the amino acid sequence of the antibacterial peptide is shown as SEQ ID NO. 1.
2. 2. A method for preparing the antibacterial peptide according to claim 1, comprising: The antibacterial peptide is synthesized according to the amino acid sequence shown in SEQ ID NO.1 by a solid phase synthesis method and purified.
3. 3. Use of the antibacterial peptide of claim 1 for preparing a product for preventing and treating oral problems.
4. 4. The use according to claim 3, wherein the oral problem comprises any one or more of bacterial infection, plaque, gingivitis, periodontitis.
5. 5. The use according to claim 4, wherein the bacteria are selected from any one or more of fusobacterium nucleatum, porphyromonas gingivalis and streptococcus mutans.
6. 6. The use according to claim 3, wherein the product is in a dosage form comprising any one or more of a spray, aerosol, mouthwash, paste, film and effervescent.
7. 7. The use of claim 3, wherein the product comprises any one or more of a pharmaceutical and an oral care product.
8. 8. The use according to claim 7, wherein the oral care product comprises any one or more of toothpaste, mouthwash, effervescent tablets and oral care solutions.
9. 9. A product comprising the antimicrobial peptide of claim 1.
10. 10. The product of claim 9, wherein the product comprises any one or more of an antibacterial agent and an oral care product; the bacteria are any one or more of Fusobacterium nucleatum, porphyromonas gingivalis and Streptococcus mutans.

Description

Antibacterial peptide, preparation method and application thereof in preventing and treating oral problems Technical Field The invention belongs to the technical field of antibacterial peptides, and particularly relates to an antibacterial peptide, a preparation method and application thereof in preventing and treating oral problems. Background The disclosure of this background section is only intended to increase the understanding of the general background of the invention and is not necessarily to be construed as an admission or any form of suggestion that this information forms the prior art already known to those of ordinary skill in the art. The antibacterial peptide is used as a small molecular polypeptide with broad-spectrum antibacterial activity and unique membrane action mechanism, and is a novel candidate drug for overcoming the drug resistance of antibiotics. The cationic and amphiphilic characteristics of the composite can target and destroy bacterial membranes with negative charges, and the composite has important potential in the treatment of diseases such as oral infection and the like. Chrysophsin3 from red sea bream is a histidine-rich alpha-helical antibacterial peptide, whose C-terminal unique RRRH domain confers significant antibacterial activity against a variety of oral pathogenic bacteria. However, natural Chrysophsin at low concentrations (about 1 μm) induces about 10% of hemolytic activity, which is significantly higher than bombesin 2, although lower than melittin, severely limiting clinical safety. Prior studies have attempted to reduce cytotoxicity by removing or modifying the C-terminal RRRH sequence, but how to simultaneously reduce hemolytic toxicity while enhancing antibacterial activity remains a key challenge. Disclosure of Invention In order to solve the defects in the prior art, the invention aims to provide an antibacterial peptide, a preparation method and application thereof in preventing and treating oral problems. In order to solve the bottleneck of the prior art and improve the antibacterial efficacy of the antibacterial peptide, the invention designs the antibacterial peptide Chrysophsin-2 containing 20 amino acid residues on the basis of systematically analyzing the amino acid sequence and the spatial structure of the red sea bream antibacterial peptide Chrysophsin, and provides a new theoretical basis and technical path for the research and development of oral disease treatment medicines. Mainly comprises the following design ideas: For the antibacterial peptide, physicochemical indexes such as net positive charge, amphipathic alpha-helicity, hydrophobic moment and the like jointly determine the membrane cleavage efficiency. The method has the advantages that the electrostatic adsorption between the bacterial outer membrane and the electronegative bacterial outer membrane can be remarkably enhanced by improving the net positive charge, the hydrophobic moment is moderately improved, so that peptide chains are easier to vertically insert when contacting a phospholipid bilayer to form a stable transmembrane pore channel, and the cooperative transformation of the peptide chains from random curling to alpha-helix on the membrane surface is promoted by reducing conformational entropy loss when the helicity is optimized, so that the cooperative effect of membrane disturbance and lipid arrangement disorder is improved. Therefore, the balance window for rationally regulating the parameters can lay a molecular design foundation for constructing the high-activity antibacterial peptide. The antibacterial peptide Chrysophsin-2 disclosed by the invention obviously enhances the comprehensive inhibition and killing capability on oral pathogenic bacteria on the basis of keeping the basic antibacterial activity of the template peptide, greatly reduces the hemolytic toxicity on mammal erythrocytes by optimizing the amino acid sequence, shows more excellent cell selectivity and safety, and provides a better candidate molecule for the treatment of oral diseases. In order to achieve the above purpose, the technical scheme of the invention is as follows: in a first aspect of the present invention, there is provided an antibacterial peptide having an amino acid sequence shown in SEQ ID NO. 1. The invention provides a novel antibacterial peptide Chrysophsin-2 obtained by accurately modifying an antibacterial peptide Chrysophsin from red sea bream. Compared with template peptide, the polypeptide obviously enhances the comprehensive inhibition and killing capability of oral pathogenic bacteria, especially improves the inhibition and killing capability of porphyromonas gingivalis (Pg) by 8 times and improves the inhibition and killing capability of streptococcus mutans (Sm) by 4 times. Meanwhile, the polypeptide can effectively inhibit the formation of oral pathogenic bacteria biological films, can obviously inhibit the formation of Sm biological films at the concentration of 31.25 mug/mL,