Bionic anti-caries polypeptide based on casein-rich saliva, derivative, salt and application thereof

A technology of statcasein and peptide derivatives, applied to polypeptide derivatives or their salts and their applications in pharmaceuticals, in the field of biomimetic anti-caries functional polypeptides, can solve problems such as high price, difficulty in extracting natural saliva proteins, and variability , to achieve the effect of low production cost, stable and simple structure, 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, natural salivary protein has the disadvantages of difficulty in extraction, high price, and easy denaturation. Therefore, in order to prevent or block dental caries, we use salivary protein as a natural template to develop and synthesize it, which is stable in the oral cavity and has the ability to promote mineralization. Functional biomimetic anti-caries functional peptide has important research significance

Method used

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  • Bionic anti-caries polypeptide based on casein-rich saliva, derivative, salt and application thereof
  • Bionic anti-caries polypeptide based on casein-rich saliva, derivative, salt and application thereof
  • Bionic anti-caries polypeptide based on casein-rich saliva, derivative, salt and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] A mineralization-promoting and anti-caries functional polypeptide, the amino acid sequence of which is shown in SEQ ID NO.1;

[0031] The serine phosphorylation modifier of SEQ ID NO.1 is: DpSpSEEKEEEEE.

Embodiment 2

[0032] Example 2 Preparation of Serine Phosphorylated Modifier of SEQ ID NO.1 (hereinafter referred to as DE11)

[0033] 1. Select Fmoc-His(Trt)-Wang Resin as the resin (carrier);

[0034] 2. Fully swell the resin with DCM;

[0035] 3. Use an appropriate concentration of DBLK (hexahydropyridine + DMF) to remove the Fmoc-protecting group;

[0036] 4. Wash several times with DMF to remove DBLK;

[0037] 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;

[0038] 6. The ninhydrin detection method is used for detection to ensure that the connection is relatively complete;

[0039] 7. Wash several times with DMF to wash away the remaining residues and activator condensation agent;

[0040] 8. Carry out coupling according to the amino acid sequence of SEQ ID NO.1, the method refers to steps 3-7;

[0041] 9. After connecting all the amino acids, use steps 3 and 4 to remove the fina...

Embodiment 3

[0045] Example 3 Detection of Polypeptide Nucleation Ability to Hydroxyapatite

[0046] 1. Prepare 50μM polypeptide DE11 solution, add the final concentration of 1.6mM Na 2 HPO 4 and 3.3mM CaCl 2 solution, the pH was adjusted to 7.4, and incubated on a shaker at 37°C for 24h (100 rpm).

[0047] 2. Take 10 μl of the reacted solution and add it dropwise on the copper grid. The negative control is Na without peptide. 2 HPO 4 and CaCl 2 solution. The shape of the precipitate on the copper grid was observed under a transmission electron microscope. figure 1 It showed that the crystals formed in the polypeptide DE11 group were denser than those in the negative control group, showing fascicular or columnar shapes, suggesting that DE11 has a good ability to promote the nucleation and growth of hydroxyapatite.

[0048] 3. Select electron diffraction to show that the crystal precipitate formed by the polypeptide DE11 group has the characteristic diffraction rings 004, 002 and 211...

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Abstract

The invention discloses a bionic anti-caries functional polypeptide based on casein-rich saliva, a polypeptide derivative or a pharmaceutically acceptable salt and an application in pharmacy thereof. The bionic anti-caries functional polypeptide is based on an anti-caries functional segment of the casein-rich saliva, the adjustment and improvement for the amino acid sequence are performed on the anti-caries functional segment and the bionic anti-caries functional polypeptide contains the amino acid sequence shown as SEQ ID NO.1. The polypeptide mainly utilizes the 'DpSpSEEK' amino acid sequence to realize the adsorption combination of polypeptide and de-mineralized enamel and the 'DpSpSEEK' amino acid sequence thereof can react with calcium phosphate ions so as to induce hydroxyapatite nucleation, so that the in-situ mineralizing repairing function for early enamel caries can be realized. The polypeptide is characterized by lower molecular weight, convenience in compound, low cost, better anti-caries effect, structure stability, safety and reliability. The invention utilizes the bionic thought to simulate natural saliva protein, designs the anti-caries polypeptide with a re-mineralization function and provides an ideal new method for preventing and controlling caries.

Description

technical field [0001] The invention belongs to the field of biotechnology, and in particular relates to a bionic anti-caries functional polypeptide based on salivary statherin, a polypeptide derivative or a salt thereof and the application thereof in pharmacy. Background technique [0002] Dental caries is an infectious disease and the most common oral disease in humans. It has a high incidence rate and a wide range of epidemic areas, seriously affecting oral and general health. The World Health Organization has listed it as the three major non-communicable diseases that human beings should focus on one. The pathogenesis of caries is the continuous demineralization of tooth hard tissue under the action of oral cariogenic bacteria acid production. Therefore, promoting the remineralization of demineralized tooth hard tissue is an important aspect of caries prevention and treatment. [0003] As a classic anti-caries preparation, fluoride can reduce the caries rate in the popu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/47A61K38/17A61P1/02
CPCA61K38/00C07K14/47
Inventor 张凌琳王琨丁隆江倪超周学东李伟
Owner SICHUAN UNIV
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