Application of octadecyl-modified polypeptide in preparing drugs for inhibiting platelet aggregation

A platelet aggregation and octadecyl technology, applied in the field of biomedicine, can solve the problems of increased bleeding risk, gastrointestinal irritation, weakened drug efficacy, etc., and achieve the effect of reducing bleeding risk.

Active Publication Date: 2020-10-16
KUNMING INST OF ZOOLOGY CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the clinically used drugs for the prevention and treatment of thrombotic diseases mainly include anticoagulant drugs, thrombolytic drugs and antiplatelet aggregation drugs, but

Method used

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  • Application of octadecyl-modified polypeptide in preparing drugs for inhibiting platelet aggregation
  • Application of octadecyl-modified polypeptide in preparing drugs for inhibiting platelet aggregation
  • Application of octadecyl-modified polypeptide in preparing drugs for inhibiting platelet aggregation

Examples

Experimental program
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Effect test

preparation example Construction

[0027] The present invention has no special limitation on the pharmaceutical dosage form and the preparation method of the dosage form, and the pharmaceutically acceptable dosage form and conventional preparation method of the polypeptide can be used for preparation. In the present invention, the polypeptide is the only active substance in the drug.

[0028] In the present invention, the sequence of the polypeptide is as follows:

[0029] SEQ ID No. 1: KEATSTF;

[0030] SEQ ID No.2 (Myristoylated-KafitidepT1):

[0031] Myristoylated-PLYKEA{pT}STFT;

[0032] SEQ ID No.3 (Myristoylated-KafitidepT2):

[0033] Myristoylated-PLYKEATS{pT}FT;

[0034] SEQ ID No.4 (Myristoylated-KafitidepT1-1-10AA): Myristoylated-PLYKEA{pT}STF;

[0035] SEQ ID No.5 (Myristoylated-Kafitide-6AA): Myristoylated-KEATST;

[0036] SEQ ID No.6 (Kafitidep-6AA): KEA{pT}ST;

[0037] SEQ ID No.7 (Kafitidep-51AA): KEA{pT}S;

[0038] SEQ ID No.8 (Kafitidep-5AA): EA{pT}ST;

[0039] SEQ ID No.9 (Kafitidep-4...

Embodiment 1

[0050] 1. Kafitide polypeptide (octadecylated polypeptide, hereinafter referred to as Kafitide polypeptide, amino acid sequence as shown in SEQ ID No.1) and phosphorylated analogs thereof (amino acid sequence as shown in SEQ ID No.2 and 3) and 14- 3-3ζ protein binding assay

[0051] The 14-3-3ζ protein (response value 9810RU) was bound to the CM5 chip (use 0.4M EDC (1-ethyl-3-[3-dimethylaminopropyl]carbodiimide hydrochloride) and 10mM NHS (N-Hydroxysuccinimide) to activate the chip, and use On 1M ethanolamine (ethanolamine) blocking), use the surface plasmon resonance instrument to the combination of different concentrations of Kafitide polypeptide and its phosphorylated analog (amino acid sequence shown in SEQ ID No.2 and 3) and 14-3-3ζ protein The conditions were detected, and the Kafitide polypeptide and its phosphorylated analogue (amino acid sequence shown in SEQ ID No.2 and 3) and 14-3-3ζ protein were obtained under different concentrations (0.37, 1.1, 3.3, 10, 30 μM res...

Embodiment 2

[0054] platelet aggregation inhibition test

[0055] platelet aggregation inhibition test

[0056] 1. After washing the platelets of healthy people with bench-top solution, dilute to 2.5×10 with bench-top solution B. 8 / mL. Take 300 μL of washed platelets, add samples of different concentrations, incubate at 37°C for 5 min, add 0.03 U / mL thrombin and 1 μg / mL collagen to induce aggregation, and draw the aggregation curve within 5 min on a platelet aggregometer. Platelet aggregation treated with the sample solvent was used as a control.

[0057] 2. If figure 2 As shown, Myristoylated-Kafitide polypeptide (amino acid sequence such as SEQ ID No.1) and its phosphorylated analogues (amino acid sequence such as SEQ ID No.2 and 3) inhibit the aggregation of platelets induced by Thrombin in a gradient-dependent manner. 10 μM Myristoylated-Kafitide polypeptide can inhibit the aggregation of about 50% platelets, and 1 μM Myristoylated-Kafitide polypeptide (amino acid sequence such a...

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PUM

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Abstract

The invention provides application of octadecyl-modified polypeptide in preparing drugs for inhibiting platelet aggregation, and belongs to the technical field of biomedicine. The octadecyl-modified polypeptide of the present invention can significantly inhibit platelet aggregation. 14-3-3 xi protein can promote platelet aggregation by promoting the interaction between c-Src protein and an integrin aIIB beta 3 protein, and the polypeptide of the present invention achieves the function of anti-platelet aggregation by inhibiting the interaction between 14-3-3 xi protein and the integrin aIIB beta 3 protein.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and particularly relates to the application of octadecylated modified polypeptides in the preparation of drugs for inhibiting platelet aggregation. Background technique [0002] A thrombus is a small clotted plaque formed by blood flow on the surface of a peeled or repaired vessel in the cardiovascular system. In the physiological process of coagulation, thrombus is the final product of the cascade reaction of the coagulation system, which is mainly composed of deposited platelets, insoluble fibrin, accumulated white blood cells and red blood cells. The formation of thrombus in the blood vessel will hinder the flow of blood flow, and even lead to the complete occlusion of the blood vessel. The thrombus peels off and detaches from the inner wall of the blood vessel and easily forms a migratory embolism. The resulting cardiovascular and cerebrovascular diseases include myocardial infarction, c...

Claims

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Application Information

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IPC IPC(8): A61K38/08A61K38/07A61K38/06A61P7/02
CPCA61K38/08A61K38/07A61K38/06A61P7/02
Inventor 赖仞申传斌吕秋敏刘明李东升
Owner KUNMING INST OF ZOOLOGY CHINESE ACAD OF SCI
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