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An anti-angiogenic polypeptide [d-ala1]as16

An anti-angiogenesis, AS16 technology, applied in the field of polypeptide [D-Ala1] AS16, can solve the problems of treatment effect, easy to be degraded by enzymes, short half-life, etc., and achieve the goal of delaying animal weight growth, not easy to be degraded by enzymes, and long half-life Effect

Active Publication Date: 2018-12-21
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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  • An anti-angiogenic polypeptide [d-ala1]as16
  • An anti-angiogenic polypeptide [d-ala1]as16
  • An anti-angiogenic polypeptide [d-ala1]as16

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] The anti-angiogenic polypeptide provided by the application [D-Ala 1 ]AS16, containing 16 amino acids, with a molecular weight of 1683.0, the specific amino acid sequence is:

[0053] D-Ala-Thr-Trp-Leu-Pro-Pro-Arg-Ala-Ala-Asn-Leu-Leu-Met-Ala-Ala-Ser; ie

[0054] D-ATWLPPRAANLLMAAS;

[0055] Wherein said D-Ala and D-A represent that the first amino acid alanine in the polypeptide sequence is in D-configuration.

[0056] Polypeptide [D-Ala 1 ]AS16 is prepared by Fomc solid-phase peptide synthesis method, the specific preparation process is as follows:

[0057] (1) To swell the resin, weigh 0.3g of Wang resin, then pour the weighed Wang resin into the cleaned and dried peptide synthesizer, then add 5 mL of DMF, and swell the resin for 30 minutes. After swelling, use a vacuum pump Extract the DMF from the peptide synthesizer;

[0058] (2) the addition of the first amino acid,

[0059] Calculate and weigh 316.5 mg of serine, 111.5 mg of HOBT (1-hydroxybenzotriazole) an...

Embodiment 2

[0097] This example mainly introduces the relevant drug experiments using the Balb / c mouse transplanted tumor model (loaded with H22 mouse liver cancer cells) as the biological material, including the tumor inhibition rate experiment, tail vein injection experiment, mouse survival experiment, etc. Multiple, so that a more comprehensive response to the polypeptide [D-Ala 1] The effect of AS16 on anti-tumor angiogenesis. The details of relevant experiments are introduced as follows.

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Abstract

The invention belongs to the bio-pharmaceutical technology field, and particularly relates to anti-angiogenesis polypeptide [D-Ala1]AS16. The polypeptide [D-Ala1]AS16 contains 16 amino acids, the molecular weight is 1683.0, and the specific amino acid sequence is D-ATWLPPRAANLLMAAS. Compared with existing AS16 polypeptide, the polypeptide [D-Ala1]AS16 has the advantages that tumor angiogenesis can be well restrained so that tumor growth can be restrained, the tumor control rate is increased remarkably, and the survival time of organisms is prolonged remarkably; long-term toxicity experiment results show that the polypeptide [D-Ala1]AS16 can reduce the weight gaining speed of a rat; the weight of the rat returns to normal after the recovery phase. In general, the polypeptide [D-Ala1]AS16 has broad prospects when applied to cancer therapy drugs in the future.

Description

technical field [0001] The invention belongs to the technical field of biopharmaceuticals, in particular to a polypeptide [D-Ala 1 ] 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 molecule may be applicable to a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K7/08C07K1/06C07K1/04A61K38/10A61P35/00
Inventor 祁元明高艳锋吴春景郭有泉陈鲤翔吴亚红郝艳静李国栋
Owner ZHENGZHOU UNIV