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A kind of anticoagulant active peptide derivative and its preparation method and application

A technology of anticoagulant activity and peptide derivatives, applied in the field of biomedicine, can solve problems such as short half-life, and achieve the effects of long half-life, improved stability and strong antioxidant activity

Active Publication Date: 2021-10-26
GUANGDONG OCEAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Polypeptide factors with a molecular weight of less than 20kDa are easily filtered by the glomeruli during metabolism; when passing through the renal tubules, the polypeptide factors are partially degraded by proteases and excreted from the urine, so the half-life is short

Method used

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  • A kind of anticoagulant active peptide derivative and its preparation method and application
  • A kind of anticoagulant active peptide derivative and its preparation method and application
  • A kind of anticoagulant active peptide derivative and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] 1. Synthetic raw materials and related reagents:

[0043] Fmoc-L-GLu(ODmab)-OH, Aimeijie Technology Co., Ltd.;

[0044] Fmoc-L-Asn(Trt)-OH, Suzhou Tianma Pharmaceutical Group;

[0045] Fmoc-L-Met(O 2 )-OH, Gill Biochemical (Shanghai) Co., Ltd.;

[0046] Fmoc-L-His(Boc)-OH, Gill Biochemical (Shanghai) Co., Ltd.;

[0047] Fmoc-L-Lys(Boc)-OH, Gill Biochemical (Shanghai) Co., Ltd.;

[0048] Fmoc-L-Phe-OH, Gill Biochemical (Shanghai) Co., Ltd.;

[0049]p-Hydroxycinnamic acid was purchased from Shanghai Jizhi Biochemical Technology Co., Ltd.

[0050] 2. The preparation of an anticoagulant active peptide derivative is synthesized by FMOC-short peptide solid-phase synthesis method, specifically:

[0051] S1: Weigh 0.8g AM Resin resin with a substitution degree of 0.4mmoL / g into a solid-phase synthesizer, add 10mL of anhydrous dichloromethane (hereinafter referred to as DCM), place on a shaker and shake for 30min to fully swell the resin ;

[0052] S2: Connect the first ...

Embodiment 2

[0062] A structural formula of an anticoagulant active peptide derivative is as follows:

[0063]

[0064] The preparation process of an anticoagulant active peptide derivative is the same as that in Example 1, and the purity of the obtained anticoagulant active peptide derivative is 96.4%.

Embodiment 3

[0066] A structural formula of an anticoagulant active peptide derivative is as follows:

[0067]

[0068] The preparation process of an anticoagulant active peptide derivative is the same as that in Example 1, and the purity of the obtained anticoagulant active peptide derivative is 96.9%.

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Abstract

The invention discloses an anticoagulant active peptide derivative, a preparation method and application thereof, and relates to the field of biomedicine. The amino acid sequence of the anticoagulant active peptide derivative is: X-Phe-Lys-His-Met-Asn-Glu. Wherein, the end group X is p-hydroxycinnamic acid, 2-amino-3-(2,3-dihydroxyphenyl)propionic acid and 2-amino-3-(4-hydroxy-3-methoxyphenyl) propane acid. The anticoagulant active peptide derivative prepared by the invention has high anticoagulant and thrombolytic activity, long half-life, high stability and strong antioxidative activity.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to an anticoagulant active peptide derivative and its preparation method and application. Background technique [0002] Thromboembolic disease is known as the invisible killer of cardiovascular and cerebrovascular diseases. It can affect various organs and systems of the whole body. About 3‰ people suffer from different forms of thrombotic diseases every year. The number of people who die of cardiovascular and cerebrovascular diseases in my country reaches 3 million every year. More than 51% of the total annual death toll worldwide is caused by it. 75% of the surviving patients are disabled, and more than 40% of them are severely disabled, which seriously threatens human health. [0003] Thrombus refers to a semi-clot-like substance formed on the surface of blood vessels or the intima of the heart during blood flow. Thrombotic diseases include arterial thrombosis, venous thro...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K7/02C07K1/08C07K1/06C07K1/04A61K38/08A61P7/02A23L33/18
CPCA23V2002/00A61K38/00A23L33/18A61P7/02C07K7/02A23V2200/326
Inventor 苗艳丽李泳赵云涛胡章张兆霞廖铭能张刘
Owner GUANGDONG OCEAN UNIVERSITY
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