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Anti-tumor angiogenesis polypeptide mPEG-Mal-Cys-AS16

A technology of mpeg-mal-cys-as16 and cys-as16 is applied to the anti-tumor angiogenesis polypeptide mPEG-Mal-Cys-AS16. It can solve the problems of being easily degraded by enzymes, affecting the therapeutic effect, and short half-life.

Active Publication Date: 2016-02-10
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, as a polypeptide drug, due to its small molecular weight, it is easily degraded by enzymes in the body and has a short half-life, so the therapeutic effect is easily affected. At the same time, its effect on inhibiting tumor angiogenesis also has further improvement. space

Method used

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  • Anti-tumor angiogenesis polypeptide mPEG-Mal-Cys-AS16
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  • Anti-tumor angiogenesis polypeptide mPEG-Mal-Cys-AS16

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] The anti-tumor angiogenesis polypeptide mPEG-Mal-Cys-AS16 provided by the present invention is prepared according to the following steps:

[0057] (1) Preparation of chemically modified precursor substance Cys-AS16 , prepare the precursor substance polypeptide Cys-AS16 according to the prior art, that is, the sequence of the precursor substance is: CATWLPPRAANLLMAAS;

[0058] The precursor polypeptide Cys-AS16 used in this example was synthesized and provided by Shanghai Keyept Biotechnology Co., Ltd.

[0059] (2) Chemical modification

[0060] In this example, mPEG5k-Mal and mPEG20K-Mal with a molecular weight of 5000 and 20000 were used for chemical modification, and the process is as follows:

[0061] First, dissolve the polypeptide in step (1) in 20mM phosphate buffer, the final concentration of the polypeptide is 1mg / mL, and adjust the pH value to 6;

[0062] In terms of molar ratio, mPEG-Mal modifier was added at a ratio of 1:1, and reacted at 4°C for 1 h to...

Embodiment 2

[0083] For the mPEG5K-Mal-Cys-AS16 and mPEG20k-Mal-Cys-AS16 prepared in Example 1, the inventors conducted in vitro bioactivity and in vitro bioenzyme hydrolysis experiments, which are briefly introduced as follows.

[0084] In vitro biological activity test

[0085] The in vitro biological activity experiment mainly uses the scratch test to detect the effect of the modified polypeptide mPEG5K-Mal-Cys-AS16 or mPEG20k-Mal-Cys-AS16 on the migration of human umbilical vein endothelial cells (HUVEC). The specific experimental process is as follows:

[0086] (1) Take HUVEC cells in good growth state, digest with 0.25% trypsin, and make monolayer cell suspension with RPMI1640 containing 10% fetal bovine serum;

[0087] (2) Count the cells, dilute and adjust the cell concentration to 1×10 5 Each well was inoculated in a 24-well plate, and routinely cultured with RPMI1640 containing 10% fetal bovine serum for 24 hours;

[0088] (3) After 24 hours, the cell enrichment degree is abo...

Embodiment 3

[0102] Example 2 is mainly a part of the in vitro experiment on the chemically modified mPEG-Mal-Cys-AS16 polypeptide provided by the present invention. This example focuses on the specific application effect experiment of the polypeptide provided by the present invention in vivo, mainly including rat in vivo drug Kinetics experiment and tumor-bearing experiment, the experiment process is introduced as follows.

[0103] Pharmacokinetic experiment

[0104] Nine 7-week-old clean SD rats (male, weighing 250-280 g) were randomly divided into 3 groups, with 3 rats in each group. They are AS16 experimental group, PEG5K-AS16 experimental group, and PEG20K-AS16 experimental group.

[0105] Fasting within 12 hours before administration and 4 hours after administration, free drinking water during the test.

[0106] The pharmacokinetic experiment process is as follows:

[0107] (1) Preparation of dosing solution,

[0108] Accurately weigh AS-1640mg, mPEG5K-Mal-Cys-AS16144mg, mPEG20...

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Abstract

The invention belongs to the technical field of biological medicine, and particularly relates to anti-tumor angiogenesis polypeptide mPEG-Mal-Cys-AS16. The peptide comprises 17 amino acids, and the specific amino acid sequence is mPEG-Mal-CATWLPPRAANLLMAAS. AS16 is subjected to proper chemical modification through adopting polyethylene glycol, so that the purpose that the half-life period of the modified AS16 in an organism is prolonged is achieved. Experiments prove that compared with the original polypeptide AS16, the polypeptide mPEG-Mal-Cys-AS16 subjected to chemical modification provided by the invention has the advantages that the biological activity is well maintained, the polypeptide is prevented from being subjected to enzymolysis of a plurality of enzymes in the organism or being filtered by the glomerulus, and the half-life period of the polypeptide is prolonged well, so that better application value is achieved when the polypeptide is applied to tumor inhibition.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to an anti-tumor angiogenesis polypeptide mPEG-Mal-Cys-AS16. Background technique [0002] Angiogenesis is the natural process of forming new blood vessels on the basis of existing vascular endothelial cells. Studies have shown that the growth of solid tumors depends on angiogenesis, and angiogenesis plays a very important role in the process of tumor growth and metastasis. It can not only provide essential oxygen and nutrients for tumor growth and metastasis, but also excrete metabolites. Anti-tumor angiogenesis therapy has many advantages: ①It is highly effective, destroying a small amount of blood vessels can lead to ischemic necrosis of a large number of tumor cells that rely on it to grow; Medication; ③Extensive anti-tumor spectrum, vascular endothelial cells of different tumors often express the same specific protein molecule, a therapy targeting this protein ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/08C07K1/14C07K1/107A61K38/10A61P35/00
Inventor 李国栋祁元明吴春景高艳锋郭有泉陈鲤翔郝艳静吴亚红
Owner ZHENGZHOU UNIV
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