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Small peptide capable of resisting thrombosis and platelet aggregation

A platelet aggregation and anti-thrombosis technology, applied in the field of molecular biology, can solve bleeding complications and other problems, and achieve the effect of inhibiting the formation of thrombus

Inactive Publication Date: 2012-03-28
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the adverse reactions of existing antiplatelet drugs such as bleeding complications, thrombocytopenia and drug resistance, new antiplatelet drugs are still the focus of current research

Method used

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  • Small peptide capable of resisting thrombosis and platelet aggregation
  • Small peptide capable of resisting thrombosis and platelet aggregation
  • Small peptide capable of resisting thrombosis and platelet aggregation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Solid phase synthesis of small peptides

[0019] Solid-phase synthesis with FMOC (9-fluorenylmethyloxycarbonyl) as the protecting group, using 95% (v / v) trifluoroacetic acid, 2.5% (v / v) water and 2.5% (v / v) triisopropyl Monosilane (TIA) cleaves it from the resin. After precipitation with ether for 3 times, the peptide was purified by reverse-phase high performance liquid chromatography (RP-HPLC), using 0%-60% (v / v) acetonitrile containing 0.05% (v / v) trifluoroacetic acid as the mobile phase. Gradient elution was performed at a flow rate of 3 mL / min. After elution, the sample was freeze-dried, and the purity was determined to be 95% by high performance liquid chromatography (HPLC) ( figure 1 ), the molecular weight is determined to be 613.76 ( figure 2 ), consistent with the theoretical molecular weight.

Embodiment 2

[0021] In vitro anti-platelet aggregation test

[0022] Human elbow venipuncture blood draw, anticoagulation with ACD solution (9:1) (v / v), 150g centrifugation for 8 minutes, aspirate platelet-rich plasma, and then centrifuge at 650g for 10 minutes; discard the supernatant and add 1g / L The hydroxyethylpiperazine ethanesulfonic acid (HEPES) buffer of bovine serum albumin was blown to disperse the precipitate, and the platelet count was adjusted to (200~300)×109 / L, 300μL was taken for each test, and 10μL of small peptides of different concentrations were added ( 0~2.0mmol / L), and finally add 15μL of the inducer adenosine diphosphate (Sigma-Aldrich, USA) to a final concentration of 5μmol / L; continuous measurement on the LBY-NJ4 platelet agglutinator (Beijing Pulisheng) for 60s, 180s, 300s, and the maximum platelet aggregation rate (RPA); the experiment was repeated 3 times; the platelet aggregation inhibition rate was calculated at the same time {inhibition rate=[1-(RPA without drug...

Embodiment 3

[0028] Effect of small peptide alone or in combination with aspirin on arteriovenous bypass thrombosis in rats

[0029] (1) Experimental animals: 15 male SD rats weighing 250-280 g, purchased from Zhejiang Experimental Animal Center, the animal license number is SCXK (Zhejiang) 2008-0033.

[0030] (2) Experimental process: The rats were randomly divided into 8 groups, each with 3 rats, which were the blank control group (given an equal volume of normal saline), and the positive control aspirin group (Sigma, 10 mg / kg), low and medium , High-dose small peptide (IRTPK) group (0.65, 1.3, 2.6 mg / kg) and low, medium, and high-dose combined with aspirin (10 mg / kg aspirin + 0.65, 1.3, 2.6 mg / kg small peptide) group. The administration volume was 0.5mL / 100g. Except for the aspirin group for intragastric administration, the other groups were administered by femoral vein injection. Before the operation, put a 5cm length of No. 1 surgical silk into the middle section of the three sections of ...

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PUM

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Abstract

The invention discloses a small peptide capable of resisting thrombosis and platelet aggregation, and the sequence of the small peptide is X-Arg-Y-X-Lys, wherein X refers to nonpolar amino acid and the nonpolar amino acid includes alanine, valine, leucine, isoleucine, proline or phenylalanine; while Y refers to polar amino acid and the polar amino acid is glycine, serine, threonine, cysteine, tyrosine, asparagine, glutamine, aspartic acid or glutamic acid. An in vitro platelet aggregation test and an in vivo thrombosis test show that the small peptide can restrain platelet aggregation in a concentration dependent way and simultaneously can remarkably restrain thrombosis of artery-vein bypass in bodies of rats. The small peptide and derivatives of the small peptide can be used for resisting platelet aggregation and thrombosis in treatment. The small peptide can be used for preparing medicaments resisting thrombosis and platelet aggregation.

Description

Technical field [0001] The present invention belongs to the technical field of molecular biology, and specifically relates to a type of small peptides composed of 5 amino acids, in particular to a type of small peptide derivatives with anti-platelet aggregation and anti-thrombosis effects with 5 amino acids as the core sequence and the same application. Background technique [0002] Thrombosis is a common pathological process of a variety of cardiovascular and cerebrovascular diseases, including cardio-cerebrovascular thromboembolism, pulmonary embolism and deep vein thrombosis. It refers to the formation of blood in blood vessels (mostly small blood vessels) under certain conditions. ) Formation of emboli, a series of syndromes caused by the pathological process of partial or complete blockage of blood vessels and blood supply disorders in corresponding parts. With the development of society and the aging of the population, the incidence of thrombotic diseases is increasing yea...

Claims

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Application Information

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IPC IPC(8): C07K7/06A61K38/08A61P7/02
CPCA61K38/00C07K7/06A61K38/08A61P7/02
Inventor 吴国球
Owner SOUTHEAST UNIV
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