A kind of polypeptide and its preparation method and use

A technology of polypeptides and polypeptide fragments, applied in the field of polypeptides and their preparation, can solve the problems of low yield of AstressinB, high production cost of AstressinB, high market price, etc.

Inactive Publication Date: 2016-12-28
HYBIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is Cml residue in AstressinB, and the raw material of amino acid residue used in the synthetic process is Fmoc-Cml-OH, and its market price is comparatively expensive, and there is the difficult coupling situation in coupling process, causes the absorption of Astressin B The 22nd amino acid of Astressin B from the N-terminus is Glu, the Glu and the 25th Lys undergo amide bond cyclization through the side chain, and the amino acid residue raw material used in the solid-phase synthesis process is Fmoc- Glu(OAll)-OH, its market price is also more expensive
Based on these two reasons, the production cost of Astressin B is high and the yield is low

Method used

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  • A kind of polypeptide and its preparation method and use
  • A kind of polypeptide and its preparation method and use
  • A kind of polypeptide and its preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0081] Example 1 Preparation of Polypeptide

[0082] Use the solid phase carrier of Rink Amide resin type, select Fmoc to protect the amino group strategy synthesis, and its operation steps are as follows:

[0083] Weigh 25 g (10 mmol) of Rink Amide resin, add it to a solid-phase reaction column, wash with DMF 2 to 3 times, and swell with DMF for 30 minutes. Use 100 mL of a mixture of piperidine and DMF with a volume ratio of 1:4 to remove the Fmoc protecting group for 20 minutes. Use the ninhydrin method to detect whether the Fmoc is completely removed. The color of the resin indicates that the Fmoc has been removed.

[0084] Weigh 10.6 g of Fmoc-Ile-OH, use DIEA as an activator, activate for 3 to 5 minutes, add to a reaction column and react for 1 to 3 hours to obtain Fmoc-Ile-Rink Amide resin.

[0085] Use 100 mL of a mixture of piperidine and DMF with a volume ratio of 1:4 to remove the Fmoc protecting group for 20 minutes. Use the ninhydrin method to detect whether the F...

Embodiment 2

[0093] Example 2 Preparation of Polypeptide

[0094] Use the solid phase carrier of Rink Amide resin type, select Fmoc to protect the amino group strategy synthesis, and its operation steps are as follows:

[0095] Weigh 25 g of Rink Amide resin, add it to a solid-phase reaction column, wash it with DMF 2 to 3 times, and swell it with DMF for 30 minutes. Use 100 mL of a mixture of piperidine and DMF with a volume ratio of 1:4 to remove the Fmoc protecting group for 20 minutes. Use the ninhydrin method to detect whether the Fmoc is completely removed. The color of the resin indicates that the Fmoc has been removed.

[0096] Weigh 10.6 g of Fmoc-Ile-OH, use DIEA as an activator, activate for 3 to 5 minutes, add to a reaction column and react for 1 to 3 hours to obtain Fmoc-Ile-Rink Amide resin.

[0097] Use 100 mL of a mixture of piperidine and DMF with a volume ratio of 1:4 to remove the Fmoc protecting group for 20 minutes. Use the ninhydrin method to detect whether the Fmoc ...

Embodiment 3

[0105] Example 3 Preparation of Polypeptide

[0106] Use the solid phase carrier of Rink Amide resin type, select Fmoc to protect the amino group strategy synthesis, and its operation steps are as follows:

[0107] Weigh 25 g of Rink Amide resin, add it to a solid-phase reaction column, wash it with DMF 2 to 3 times, and swell it with DMF for 30 minutes. Use 100 mL of piperidine and DMF mixture with a volume ratio of 1:4 to remove the Fmoc protecting group for 20 minutes. Use the ninhydrin method to detect whether the Fmoc is completely removed. The resin has a color, indicating that the Fmoc has been removed.

[0108] Weigh 10.6 g of Fmoc-Ile-OH, use DIEA as an activator, activate for 3 to 5 minutes, add to a reaction column and react for 1 to 3 hours to obtain Fmoc-Ile-Rink Amide resin.

[0109]Use 100 mL of a mixture of piperidine and DMF with a volume ratio of 1:4 to remove the Fmoc protecting group for 20 minutes. Use the ninhydrin method to detect whether the Fmoc is co...

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Abstract

The invention relates to the field of polypeptide synthesis and particularly relates to a polypeptide as well as a preparation method and use thereof. The amino acid sequence of the polypeptide is shown in SEQ ID NO: 1, and the terminal N of the polypeptide is acetylated. From the terminal N, amido bond cyclization is carried out on an X8 main chain at the 22nd site and an X9 side chain at the 25th site in the polypeptide. The polypeptide after amido bond cyclization provided by the invention retains the biological activity of Astressin B, is high in metabolic stability and can be used for effectively preventing and treating alopecia. The preparation method of the polypeptide has the advantages of low production cost and high yield.

Description

technical field [0001] The invention relates to the field of polypeptide synthesis, in particular to a polypeptide and its preparation method and application. Background technique [0002] Alopecia refers to the phenomenon that hair falls out, comprises physiological alopecia and pathological alopecia. Physiological hair loss refers to the phenomenon of hair loss in the catagen and telogen phases. Since the hair entering the catagen and the newly entering the growth phase is constantly in a dynamic balance, it can maintain a normal amount of hair. Pathological alopecia refers to the abnormal or excessive shedding of hair. The main reason is that the heat and toxin in the human blood cannot be discharged, so that certain diseases occur in the human body. The hair follicles shrink, the hair falls off, and the hair is easy to break. Elasticity, the more serious cases are general removal and complete removal. According to different pathogenesis, pathological alopecia is mainly...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K14/00C07K1/06C07K1/04A61K38/16A61P17/14
CPCA61K38/00C07K14/00
Inventor 戴政清刘剑马亚平袁建成
Owner HYBIO PHARMA
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