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Biomimetic anti-caries polypeptide based on salivary statherin, its derivative and salt and application

A stather protein, anti-caries technology, applied in the biological field, can solve the problems of natural salivary protein extraction difficulty, high price, variability, etc., and achieve the effect of stable and simple structure, low production cost, and small molecular weight

Active Publication Date: 2020-02-07
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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  • Biomimetic anti-caries polypeptide based on salivary statherin, its derivative and salt and application
  • Biomimetic anti-caries polypeptide based on salivary statherin, its derivative and salt and application
  • Biomimetic anti-caries polypeptide based on salivary statherin, its derivative and salt and application

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Experimental program
Comparison scheme
Effect test

Embodiment 1

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

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

Embodiment 2

[0032] Example 2 Preparation of the serine phosphorylation modification of SEQ ID NO. 1 (hereinafter referred to as DE11)

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

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

[0035] 3. Use 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 performs detection to ensure that the connection is relatively complete;

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

[0040] 8. Perform coupling according to the amino acid sequence of SEQ ID NO. 1, and refer to steps 3-7 for the method;

[0041] 9. After all the amino acids are connected, the final Fmoc-protecting group is r...

Embodiment 3

[0045] Example 3 Detection of the nucleation ability of hydroxyapatite by polypeptide

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

[0047] 2. Take 10μl of the reaction solution and drop it on the copper net. The negative control is Na without peptide 2 HPO 4 And CaCl 2 Solution. Observe the morphology of the precipitate on the copper net under a transmission electron microscope. figure 1 It shows that the crystals formed in the DE11 polypeptide group are denser than the negative control group, showing a bundle or column shape, suggesting that DE11 has a good ability to promote the nucleation and growth of hydroxyapatite.

[0048] 3. Selecting electron diffraction shows that the crystal precipitate formed by the polypeptide DE11 group has hydroxyapatite 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 present invention belongs to the field of biotechnology, and specifically relates to a biomimetic anti-caries functional polypeptide, polypeptide derivative or salt thereof based on saliva saccharin and its application in pharmacy. Background technique [0002] Caries is an infectious disease and the most common oral disease in humans. It has a high incidence and a wide spread area, which seriously affects oral and general health. The World Health Organization has listed it as the three major non-communicable diseases for humans to prevent and treat. one. The pathogenesis of caries is the continuous demineralization of tooth hard tissues under the action of oral cariogenic bacteria. Therefore, promoting the remineralization of demineralized tooth hard tissues is an important aspect of caries prevention and treatment. [0003] As a classic anti-caries preparation, fluoride can reduce the prevalence of caries in the population to varying degrees and is rec...

Claims

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Application Information

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Patent Type & Authority Patents(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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