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Polypeptide polymer having antitumor activity and its preparation method and use

A peptide polymer and polymer technology, applied in the field of peptide polymer with anti-tumor activity and its preparation, can solve the problems of low bioavailability, short half-life, and difficulty in entering cells

Active Publication Date: 2014-08-13
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, polypeptide molecules generally have large molecular weight and hydrophilic characteristics, making it difficult for them to enter cells, so they have low bioavailability
In addition, due to the presence of polypeptide hydrolase in the body, it is easier to be degraded, the stability is poor, and the half-life of the circulation in the body is shorter

Method used

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  • Polypeptide polymer having antitumor activity and its preparation method and use
  • Polypeptide polymer having antitumor activity and its preparation method and use
  • Polypeptide polymer having antitumor activity and its preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Example 1: with R 1 Polyethylene glycol with a structure of 10 repeating units as an example to prepare polypeptide polymers

[0057] 1. First introduce the synthesis method of polypeptide polymer:

[0058] The 10mM (total amount) peptide molecule CCGGGRGD (targeting peptide) and CCGGGKLAKLAKKKLAKLAK (therapeutic peptide) were mixed in different molar ratios (100:0, 90:10, 80:20, 70:30, 60:40, 50:50, 40 :60, 30:70, 20:80, 10:90, 0:100) were dissolved in water and placed in a reaction vessel, 2 mL of phosphate buffer solution with pH 7.4 was added, stirred and dissolved, and 10 mM phosphate buffer solution with a molecular weight of 575 was added Polyethylene glycol diacrylate, a sealed system, nitrogen gas for 20 minutes, and a constant temperature of 37 ° C for 3 days; the reacted solution was added to a dialysis bag, dialyzed for 24 hours, and freeze-dried to obtain a white powdery solid. By gel permeation chromatography analysis, the molecular weight of the polymer...

Embodiment 2

[0061] Example 2: with R 1 Preparation of Polypeptide Polymers with Methylene Amide as an Example

[0062] 1. First introduce the synthesis method of polypeptide polymer:

[0063] The 10mM (total amount) peptide molecule CCGGGRGD (targeting peptide) and CCGGGKLAKLAKKKLAKLAK (therapeutic peptide) were mixed in different molar ratios (100:0, 90:10, 80:20, 70:30, 60:40, 50:50, 40 :60, 30:70, 20:80, 90:10, 0:100) dissolved in water, and placed in a reaction vessel, added 20mM sodium bicarbonate, stirred to dissolve, then added 10mM N,N'-methylene Bisacrylamide, sealed system, nitrogen gas for 20 minutes, constant temperature 37 ° C reaction for 3 days; the reaction solution was added to a dialysis bag, dialyzed for 24 hours, and freeze-dried to obtain a white powdery solid. Through gel permeation chromatography analysis, the molar ratio of targeting peptide and therapeutic peptide is 10:90, the polymer molecular weight is 31200, and the dispersion degree is 1.58.

[0064] 2. Pe...

Embodiment 3

[0066] Example 3: with R 1 Preparation of Polypeptide Polymer with Structure 1,6-Hexanediol as an Example

[0067] Dissolve 10mM (total amount) polypeptide molecules CCGGGRGD (targeting peptide) and CCGGGKLAKLAKLAKKLAKLAK (therapeutic peptide) in dimethyl sulfoxide at different molar ratios, and place them in a reaction vessel, add 20mM triethylamine, stir to dissolve, Add 10mM 1,6-hexanediol diacrylate, seal the system, pass nitrogen gas for 20 minutes, and react at a constant temperature of 30°C for 3 days; put the reacted solution into a dialysis bag, dialyze for 24 hours, and freeze-dry to obtain a white powdery solid . Through gel permeation chromatography analysis, the molar ratio of targeting peptide and therapeutic peptide is 10:90, the molecular weight of the polymer is 35600, and the dispersion is 1.42.

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Abstract

The invention relates to a polypeptide polymer having antitumor activity and its preparation method and use. The polypeptide polymer has a general structural formula shown in the description, and in the general structural formula, R1 represents -O-R3-O-, -O-R4-O-R5-O-, -(O-R6)<m>-O-, -NH-R7-NH- or -NH-R8-O-R9-O-R10-NH-, R3, R4, R5 and R6 respectively and individually represent straight chain or branched chain alkylidene groups, m is a natural number of 2 to 22, R7 represents a substituted or unsubstituted alkylidene group, R8, R9 and R10 respectively and individually represent straight chain or branched chain alkylidene groups, R2 represents a polypeptide chain and n is a natural number more than 5. The polypeptide polymer has targeting and treatment functions, can produce synergism, has high-efficiency cancer treatment effects superior to that of a polypeptide micromolecule, has better cycling stability and can realize in-vivo application.

Description

technical field [0001] The invention relates to the technical field of functional polypeptides, in particular to a polypeptide polymer with anti-tumor activity and its preparation method and application. Background technique [0002] In the treatment of cancer, the current traditional chemotherapy methods use some small molecule anticancer drug preparations, which can cause harm to normal tissue cells while killing tumor cells. Therefore, people have developed macromolecule drug delivery systems, which help to increase the probability of anticancer drugs selectively entering tumor tissues and reduce the side effects caused by chemotherapy. However, for synthetic polymer drug carriers, there are potential biological toxicity and immune rejection problems. [0003] At the same time, people have also developed a new class of functional polypeptide molecules for cancer treatment, making them biocompatible and capable of inhibiting tumor cells efficiently. However, polypeptide ...

Claims

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Application Information

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IPC IPC(8): C08G75/04A61K38/10A61K47/48A61K49/00A61P35/00C08G75/045
Inventor 王浩乔增莹侯春园
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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