Preparation method of anti-microbial star type poly-polypeptide

The technology of polypolypeptide and antibacterial agent is applied in the field of preparation of antibacterial star-shaped polypolypeptide, which can solve the problems of being easily degraded by enzymes, complicated extraction process, difficult industrialization, etc., and achieves less toxic and side effects on human body, improved antibacterial efficiency, and easy synthesis. Effect

Active Publication Date: 2015-11-25
UNIV OF SCI & TECH OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, at present, natural antimicrobial peptides still have problems such as limited sources (limited natural extraction resources, difficult to industrialize), high cost, complicated extraction process, and easy degradation by enzymes.

Method used

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  • Preparation method of anti-microbial star type poly-polypeptide
  • Preparation method of anti-microbial star type poly-polypeptide
  • Preparation method of anti-microbial star type poly-polypeptide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Add propargylamine: benzyl carbamate-protected N-carboxy-α-lysine anhydride: DMSO = 1:50:50 into a three-necked flask, and react with nitrogen gas for 60-70 hours. Precipitate benzylcarbamate-protected star polypeptides in water, followed by alkyne-terminated linear polypolypeptides: DMF: trifunctional azide core: CuBr: pentamethyldiethylenetriamine = 1 Add the ratio of :150:0.1:0.3:0.3 into a three-necked flask, pass nitrogen gas to react for 2-4 hours, and then precipitate in water, the resulting solid is catalyzed by palladium carbon according to the product: H2=1:3000 for reduction hydrogenation reaction, Dialyze in a 3kDa dialysis bag for one day, remove water under reduced pressure, and vacuum dry overnight to obtain pure star polypeptide, with a yield of 96%.

Embodiment 2

[0060] Add propargylamine: benzyl carbamate-protected N-carboxy-α-lysine anhydride: DMSO = 1:150:150 into a three-necked flask, and react with nitrogen for 60-70 hours. Precipitate benzylcarbamate-protected star polypeptides in water, followed by alkyne-terminated linear polypolypeptides: DMF: trifunctional azide core: CuBr: pentamethyldiethylenetriamine = 1 Add the ratio of :200:0.1:0.3:0.3 into a three-necked flask, and react with nitrogen gas for 2-4 hours, and then precipitate in water, and the resulting solid is catalyzed by palladium carbon according to the product: H2=1:3000. Reductive hydrogenation reaction, Dialyze in a 3kDa dialysis bag for one day, remove water under reduced pressure, and vacuum dry overnight to obtain pure star polypeptide, with a yield of 95%.

Embodiment 3

[0062] Add propargylamine: benzyl carbamate-protected N-carboxy-α-lysine anhydride: DMSO = 1:200:200 into a three-necked flask, and react with nitrogen gas for 60-70 hours. Precipitate benzylcarbamate-protected star polypeptides in water, followed by alkyne-terminated linear polypolypeptides: DMF: trifunctional azide core: CuBr: pentamethyldiethylenetriamine = 1 Add the ratio of :50:0.1:0.3:0.3 into the three-necked flask, pass nitrogen gas to react for 2-4 hours, and then precipitate in water, the resulting solid is catalyzed by palladium carbon according to the product: H2=1:3000 for reduction hydrogenation reaction, Dialyze in a 3kDa dialysis bag for one day, remove water under reduced pressure, and vacuum dry overnight to obtain pure star polypeptide, with a yield of 96%.

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Abstract

The invention relates to the technical field of anti-microbial materials, in particular to a preparation method of anti-microbial star type poly-polypeptide. According to the method, an arm-first method is adopted, an N-carboxyl-alpha-amino anhydride polymerization method (NCA polymerization method) serves as a measure, and the three-arm star type poly-polypeptide with the controllable molecular structure is synthesized. The artificial macromolecule anti-microbial agent has the efficient targeted anti-microbial property, is not prone to degradation and has good anti-microbial activity for gram negative and gram-positive bacteria. In addition, no drug-resistant bacterium is caused by the macromolecule anti-microbial agent, and the macromolecule anti-microbial agent cannot permeate into the skin and the pores of the human body and is an ideal substitute object for antibiotic drugs.

Description

technical field [0001] The invention relates to the technical field of antibacterial materials, in particular to a preparation method of an antibacterial star polypeptide. Background technique [0002] The abuse of antibiotic antibacterial agents will lead to the generation of super-resistant bacteria, which will penetrate into the skin or circulate in the blood to organs that are not infected by bacteria, resulting in toxic side effects. Therefore, how to use new antibacterial agents to replace traditional antibiotic antibacterial agents has always been a global scientific topic. [0003] In the 1990s, when biologists induced the chrysalis chrysalis with microorganisms, they discovered that the immune system of the chrysalis chrysalis produced a polypeptide substance that had bactericidal activity. Scientists named this polypeptide Cecmpins, and Cecmpins was officially recognized as the world's first antibacterial peptide. The number of amino acid residues of natural anti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G69/48C08G69/16A61K31/785A61P31/04
Inventor 贺晨李军配王攀张国庆
Owner UNIV OF SCI & TECH OF CHINA
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