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A degradable multi-branched glycopeptide hydrogel against postoperative scars and its preparation method

A multi-branched, hydrogel technology, applied in the field of biomedicine, can solve the problems of increasing patient pain, high price, and difficulty in artificial synthesis of proteoglycans, so as to reduce production and use costs, reduce dosage, and have good biocompatibility Effect

Active Publication Date: 2017-05-24
WUHAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the use of Decorin to clinically inhibit glaucoma postoperative scars has the following disadvantages: the artificial synthesis of proteoglycan is very difficult and expensive, and the water injection method used requires repeated injections to increase the pain of patients, etc.

Method used

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  • A degradable multi-branched glycopeptide hydrogel against postoperative scars and its preparation method
  • A degradable multi-branched glycopeptide hydrogel against postoperative scars and its preparation method
  • A degradable multi-branched glycopeptide hydrogel against postoperative scars and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] (1) Preparation of tripeptide Chol-Phe-Phe-Asp(OtBu)-OH modified with hydrophobic functional group cholesterol (cholesterol, Chol) containing good biocompatibility

[0032]Using 2-chloro-trityl chloride resin (the effective chlorine substitution degree of the resin is 1.08mmol / g) as the solid phase carrier, the cholesterol-linked short peptide Chol-Phe-Phe-Asp was prepared using a peptide solid-phase automatic synthesizer (OtBu)-OH. The peptide chain extends from the carbon end to the nitrogen end on the resin. The specific preparation steps are as follows: Weigh 2.0g of 2-chloro-trityl chloride resin (the amount of total available chlorine is 2.0g × 1.08mmol / g=2.16mmol, then soak the resin with 15mL DMF for 1 hour. Remove the DMF , 15 mL DMF solution of FMOC-Asp(OtBu)-OH (2 × 2.16mmol) and diisopropylethylamine (DIEA, 6 × 2.16mmol) was added to the resin, and the reaction was stirred at room temperature for 1.5 hours. Remove the reaction liquid, wash the resin three ...

Embodiment 2

[0044] (1) Preparation of tripeptide Chol-Phe-Phe-Asp-OH modified with hydrophobic cholesterol (cholesterol, Chol) containing good biocompatibility

[0045]Using 2-chloro-trityl chloride resin (the effective chlorine substitution degree of the resin is 1.08mmol / g) as the solid phase carrier, the cholesterol-linked short peptide Chol-Phe-Phe-Asp was prepared using a peptide solid-phase automatic synthesizer (OtBu)-OH. The peptide chain extends from the carbon end to the nitrogen end on the resin. The specific preparation steps are as follows: Weigh 2.0g of 2-chloro-trityl chloride resin (the amount of total available chlorine is 2.0g × 1.08mmol / g=2.16mmol, then soak the resin with 15mL DMF for 1 hour. Remove the DMF , 15 mL DMF solution of FMOC-Asp(OtBu)-OH (2 × 2.16mmol) and diisopropylethylamine (DIEA, 6 × 2.16mmol) was added to the resin, and the reaction was stirred at room temperature for 1.5 hours. Remove the reaction liquid, wash the resin three times with 15 mL DMF, t...

Embodiment 3

[0052] (1) Preparation of tetrapeptide Chol-Phe-Phe-Asp-Asp-OH modified with good biocompatibility and hydrophobic cholesterol (cholesterol, Chol)

[0053] Using 2-chloro-trityl chloride resin (the effective chlorine substitution degree of the resin is 1.08mmol / g) as the solid phase carrier, the cholesterol-linked short peptide Chol-Phe-Phe-Asp was prepared using a peptide solid-phase automatic synthesizer (OtBu)-OH. The peptide chain extends from the carbon end to the nitrogen end on the resin. The specific preparation steps are as follows: Weigh 2.0g of 2-chloro-trityl chloride resin (the amount of total available chlorine is 2.0g × 1.08mmol / g=2.16mmol, then soak the resin with 15mL DMF for 1 hour. Remove the DMF , 15 mL DMF solution of FMOC-Asp(OtBu)-OH (2 × 2.16mmol) and diisopropylethylamine (DIEA, 6 × 2.16mmol) was added to the resin, and the reaction was stirred at room temperature for 1.5 hours. Remove the reaction liquid, wash the resin three times with 15 mL DMF, t...

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Abstract

The invention relates to anti-postoperation scar degradable multi-branched glycopeptide hydrogel and a preparing method thereof. The hydrogel is formed by self-assembly of multi-branched glycopeptides modified with hydrophobic cholesterol under physiological conditions through hydrophobic forces, pi-pi stacking, hydrogen bonds, and other forces. A glucosamine unit in the structure of the multi-branched glycopeptides can effectively inhibit tissue fibrosis caused by fibroblast proliferation so as to prevent formation of a postoperation scar, so that the hydrogel can be used as an anti-postoperation scar gel phase preparation. By introduction of the hydrophobic cholesterol, biocompatibility of the gel is enhanced, toxic and side effects and inflammation risks of the gel are reduced, and the self-assembly capability and stability of the hydrogel are enhanced. The hydrogel has advantages of high biosecurity, convenient operation, and the like.

Description

technical field [0001] The invention relates to a degradable multi-branched glycopeptide hydrogel for resisting postoperative scars and a preparation method thereof, belonging to the field of biomedicine. [0002] technical background [0003] Glaucoma is the leading cause of blindness worldwide, accounting for about 14.36% of ophthalmic diseases. In my country, with the popularization and application of computer technology and the popularity of new media models, people's eye pressure is increasing with the changes in reading, work and entertainment methods, and the incidence of glaucoma is increasing explosively. It has become the second largest in my country. big eye disease. In recent years, with people's further understanding of the pathogenesis of glaucoma, laser filtration surgery has become more popular among glaucoma patients, with a current market share of nearly 70%. However, the wound is easily scarred after the filtration operation, which leads to the closure of ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K9/00C07K1/107A61K38/14A61K9/06A61P27/06
Inventor 张先正陈巍海曾旋冯俊
Owner WUHAN UNIV
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