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Double-effect anticariogenic polypeptide, polypeptide derivatives, polypeptide pharmaceutical salts and application

A technology of peptide derivatives and medicinal salts, applied in the field of biomedicine, can solve the problems of single anti-cariogenic bacteria or promoting remineralization function, increase patient's medication burden, poor compliance, etc., and achieve reliable promoting remineralization, The effect of promoting early artificial caries remineralization and small molecular weight

Active Publication Date: 2017-11-17
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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  • Double-effect anticariogenic polypeptide, polypeptide derivatives, polypeptide pharmaceutical salts and application
  • Double-effect anticariogenic polypeptide, polypeptide derivatives, polypeptide pharmaceutical salts and application
  • Double-effect anticariogenic polypeptide, polypeptide derivatives, polypeptide pharmaceutical salts and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] The anti-caries polypeptide of the present invention has an amino acid sequence such as SEQ ID NO.1: TKREEVDGLLWHLLHHLLH; SEQ ID NO.2: TKRQQVNGLLWHLLHHLLH; SEQ ID NO.3: TKRQQVVGLLWHLLHHLLH; SEQ ID NO.4: TKRQQVVLLRRLLRRLLRR; SEQ ID NO.5: TKRQQVVLLKKLLKKLLKK.

[0058] Prepare as follows:

[0059] 1. Select Fmoc-His(Trt)-Wang Resin as the resin (carrier);

[0060] 2. Fully swell the resin with DCM;

[0061] 3. Use an appropriate concentration of DBLK (hexahydropyridine + DMF) to remove the Fmoc-protecting group;

[0062] 4. Wash several times with DMF to remove DBLK;

[0063] 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;

[0064] 6. The ninhydrin detection method is used for detection to ensure that the connection is relatively complete;

[0065] 7. Wash several times with DMF to wash away the remaining residues and activator condensation agent;

[0066] 8. Coupling...

Embodiment 2

[0072] Preparation of C-terminal amidated derivatives:

[0073] 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

[0074] Embodiment 3 Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC) Determination

[0075] 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 Disease Research, for the polypeptide C-terminal amides of SEQ ID NO.1~3 (sample 1~3) Conduct a liveness test.

[0076] The experimental steps of MIC and MBC determination are as f...

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Abstract

The invention discloses double-effect anticariogenic polypeptide with functions of resisting cariogenic bacteria and promoting remineralization, polypeptide derivatives or polypeptide pharmaceutical salts. The polypeptide contains an amino-acid sequence a and an amino-acid sequence b; the amino-acid sequence a is TKRX1X2VX3, wherein X1 and X2 are respectively E or Q, and X3 is D, N or V; and the amino-acid sequence b is antibacterial peptide with an alpha helical structure, positive charges, amphiphilicity, 8-12 amino acids and alternation of hydrophilic-hydrophobic amino acids in the sequence. The double-effect anticariogenic polypeptide has the exact double functions of resisting the bacteria and promoting remineralization, is low in molecular weight, is stable in structure in an oral cavity, has no obvious cytotoxicity, has great potential for preventing the cariogenic disease, makes up the defect of shortage of effective and safe drugs with double functions of resisting cariogenic bacteria and promoting remineralization in the prior art, and has important clinical significance in the anticariogenic field.

Description

technical field [0001] The invention belongs to the field of biomedicine, and specifically relates to a double-effect anti-caries polypeptide, a polypeptide derivative, a pharmaceutically acceptable salt of the polypeptide and its application, 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 altern...

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 张凌琳王秀清王雨霏任倩周学东李伟
Owner SICHUAN UNIV
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