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Anticoagulant active peptide derivative and preparation method and application thereof
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A technology of anticoagulant activity and peptide derivatives, applied in the field of biomedicine, can solve problems such as short half-life, achieve long half-life, good protection of peptide activity, and high antioxidant performance
Active Publication Date: 2021-03-02
GUANGDONG OCEAN UNIVERSITY
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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
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Embodiment 1
[0042] 1. Synthetic raw materials and related reagents:
[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 anhydrousdichloromethane (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 and a preparation method and application thereof, and relates to the field of biological medicines. The amino acid sequence of the anticoagulant active peptide derivative is X-Phe-Lys-His-Met-Asn-GLu, wherein the terminal group X is p-hydroxycinnamic acid, 2-amino-3-(2, 3-dihydroxyphenyl) propionic acid and 2-amino-3-(4-hydroxy-3-methoxyphenyl) propionic acid. The anticoagulant active peptide derivative prepared by the method has high anticoagulant and thrombolytic activity, long half-life period and high stability, and has high antioxidant 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...
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