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Anti-caries polypeptide capable of preventing bacteria and promoting remineralization, derivative and salt thereof, and applications of anti-caries polypeptide, derivative, and salt

A peptide derivative and remineralization technology, applied in the field of biomedicine, can solve the problems of single anti-cariogenic bacteria or promoting remineralization function, increase the burden of medication for patients, and poor compliance, so as to promote the remineralization of early artificial caries , Reliable effect of promoting remineralization, small molecular weight effect

Active Publication Date: 2017-11-28
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these peptides only have a single function of anti-cariogenic bacteria or promoting remineralization. For patients with dual needs of anti-bacteria and remineralization, two drugs need to be used at the same time. The two drugs may interact with each other, reducing the efficacy of each

Method used

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  • Anti-caries polypeptide capable of preventing bacteria and promoting remineralization, derivative and salt thereof, and applications of anti-caries polypeptide, derivative, and salt
  • Anti-caries polypeptide capable of preventing bacteria and promoting remineralization, derivative and salt thereof, and applications of anti-caries polypeptide, derivative, and salt
  • Anti-caries polypeptide capable of preventing bacteria and promoting remineralization, derivative and salt thereof, and applications of anti-caries polypeptide, derivative, and salt

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0081] The anti-caries polypeptide of the present invention has an amino acid sequence such as SEQ ID NO.1-9.

[0082] Prepare as follows:

[0083] 1. Select Fmoc-His(Trt)-Wang Resin as the resin (carrier);

[0084] 2. Fully swell the resin with DCM;

[0085] 3. Use an appropriate concentration of DBLK (hexahydropyridine + DMF) to remove the Fmoc-protecting group;

[0086] 4. Wash several times with DMF to remove DBLK;

[0087] 5. Weigh a suitable condensing agent and activator (HBTU, NMM) and the second Fmoc-protected amino acid (Fomc-Leu-OH) at the C-terminal for coupling;

[0088] 6. The ninhydrin detection method is used for detection to ensure that the connection is relatively complete;

[0089] 7. Wash several times with DMF to wash away the remaining residues and activator condensation agent;

[0090] 8. Coupling is carried out according to the amino acid sequence of the polypeptide, and the method refers to steps 3-7;

[0091] 9. After connecting all the amino ac...

Embodiment 2

[0096] Preparation of C-terminal amidated derivatives:

[0097] The preparation was carried out with reference to the method described in Example 1, the only difference being that Rink-Amide-Am Resin was selected as the resin (carrier).

Embodiment 3

[0098] Example 3 "Double Effect" Polypeptide Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC) Determination

[0099]The minimum inhibitory concentration MIC (Minimal inhibitory concentration) refers to the lowest concentration of antibacterial drugs that can inhibit the growth of bacteria in the medium in vitro tests. Minimal bactericidal concentration MBC (Minimal bactericidal concentration) refers to the minimum concentration of antibacterial drugs that can kill viable bacteria in the medium in vitro tests. MIC and MBC are indicators of drug antibacterial activity, showing the ability of drugs to inhibit and kill pathogenic microorganisms. Bacteria were used in the experiment as the main oral cariogenic bacteria: Streptococcus mutans UA159, provided by the State Key Laboratory of Oral Diseases. The test polypeptide is the C-terminal amidate of SEQ ID NO.1 (hereinafter referred to as SH18).

[0100] The experimental steps of MIC and MBC de...

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Abstract

The invention discloses an anti-caries polypeptide capable of preventing bacteria and promoting remineralization, a polypeptide derivative or a polypeptide pharmaceutical salt thereof. The anti-caries polypeptide contains an amino acid sequence a and an amino acid sequence b; the amino acid sequence a is Xn, wherein X is used for representing S, T, Y, K, R, N, or Q, n is used for representing the amino acid repeat times, and is an integer selected from 5 to 8; the amino acid sequence b is of a alpha double helix structure, is positively charged, and contains 8 to 12 amino acids, and the hydrophilic amino acids and hydrophobic amino acid in the amino acid sequence b appear alternately. The functional anti-caries polypeptide capable of preventing cariogenic bacteria and promoting remineralization is capable of inhibiting growth of streptococcus mutans, inhibiting formation of biological membrane of streptococcus mutans, reducing the metabolism capability of formed biological membrane of streptococcus mutans, killing viable bacteria in the formed biological membrane of streptococcus mutans, promoting remineralization of demineralization tooth enamel, and reducing caries depth and mineral loss of demineralization tooth enamel, and possesses excellent stability, and no obvious cytotoxicity.

Description

technical field [0001] The invention belongs to the field of biomedicine, and specifically relates to an anti-caries polypeptide, a polypeptide derivative, a pharmaceutically acceptable salt of the polypeptide and applications thereof, which have the functions of resisting cariogenic bacteria and promoting remineralization. Background technique [0002] Dental caries is a disease in which dental hard tissues are chronically and progressively destroyed under the action of multi-factors mainly composed of bacteria. It is also the most common oral disease in humans. It exists widely in all parts of the world. One of the three major diseases of human health. A large amount of evidence shows that the existence of bacteria is a prerequisite for the occurrence of caries, oral cariogenic bacteria metabolize carbohydrates to produce acid, leading to demineralization of dental hard tissue is the direct cause of caries. The development of caries is a process of repeated alternating an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K19/00A61K38/08A61K38/10A61P1/02
CPCA61K38/00C07K7/06C07K7/08C07K2319/00
Inventor 张凌琳王秀清韩思理郑雯月周学东李伟
Owner SICHUAN UNIV
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