Fusion polypeptide with cerebral ischemia resistant effect and application thereof

An anti-ischemic and anti-inflammatory technology, applied in the direction of medical preparations containing active ingredients, peptides, drug combinations, etc., can solve the problems of inaccurate curative effect, adverse reactions, etc., and achieve the effect of good application prospects

Active Publication Date: 2017-07-07
HEBEI UNIVERSITY OF SCIENCE AND TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] N-methyl-D-aspartate (NMDA) receptor is an important anti-ischemic target. Researchers have developed

Method used

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  • Fusion polypeptide with cerebral ischemia resistant effect and application thereof
  • Fusion polypeptide with cerebral ischemia resistant effect and application thereof
  • Fusion polypeptide with cerebral ischemia resistant effect and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1. Preparation of polypeptide (YGRKKRRQRRRGDPV)

[0023] 1. Peptide synthesis process: Peptide synthesis process: first soak the resin (Fmoc-Val-Wang Resin) in DCM for 5-10 minutes, wash it with DMF for 5 times, deprotect it with 20% hexahydropyridine for 10-20 minutes, and use DMF Wash 5 times, then add protected amino acid raw materials, condensing agent, etc. to condense for 30 minutes, wash 5 times with DMF, then deprotect—wash—condense—clean, finally deprotect, wash, drain, cut with TFA, and use cutting fluid Precipitate with ether, wash with ether 2-3 times, and drain. This is a general process of the whole peptide synthesis.

[0024] 2. Polypeptide synthesis starts from the C-terminal, that is, synthesis from right to left. First, this sequence YGRKKRRQRRRGDPV is synthesized with conventional amino acid raw materials. The amino acid raw materials used are Fmoc-Pro-OH, Fmoc-Asp(otbu)- OH, Fmoc-Gly-OH, Fmoc-Gln(Trt)-OH, Fmoc-Arg(pbf)-OH, Fmoc-Lys(Boc)-OH, ...

Embodiment 2

[0025] Example 2. Effect of polypeptide on glutamic acid excitotoxicity

[0026] Fetal mouse cortical neuron cells cultured in vitro for 11 days were washed with HBSS for 3 times, and incubated with 50 μM glutamic acid for 20 minutes. Distilled water, YV-15 or YA-15 were given respectively during the incubation with glutamic acid. 0.05, 0.5, and 2 μmol / L. After the incubation, remove all drugs, wash the plate with HBSS for 3 times, add maintenance medium, and place at 37°C, containing 5% CO 2 The culture was continued for 24 h in an incubator, and the damage of the cells was detected by the MTT assay.

Embodiment 3

[0027] Example 3. Effects of polypeptides on neurobehavioral scores and mortality of animals after cerebral ischemia

[0028] 1. Establishment and administration of rat MCAO model: Sprague Dawley (SD) rats, male, body weight (300±20) g. The cerebral ischemia model of middle cerebral artery occlusion (MCAO) was established by the internal carotid artery suture method. Rats were anesthetized with 10% chloral hydrate (300 mg·kg - 1 , i.p. ), fixed on the operating table in the supine position, and a median incision was made in the neck to separate the right common carotid artery, external carotid artery, and internal carotid artery. , Gently strip the vagus nerve and ligate all branches on the external and internal carotid arteries. External carotid artery incision, insert a nylon fishing line with an outer diameter of 0.28 mm (the head end is treated with silicone resin to make it smooth), turn around the bifurcation of the common carotid artery and enter the internal carotid a...

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Abstract

The invention provides a fusion polypeptide with a cerebral ischemia resistant effect and application thereof. The fusion polypeptide has a peptide chain fragment sequence of YGRKKRRQRRRGDPV. The polypeptide provided by the invention can rapidly and effectively enter cells; through interfering with the signal conduction of CAPON, the neuron excitatory toxicity injury induced by glutamic acid is obviously inhibited; the cerebral ischemia injury of MCAO model rats can be effectively resisted. The polypeptide has good application prospects in the preparation of medicine for treating cerebrovascular diseases.

Description

technical field [0001] The invention belongs to the technical field of drugs for cerebrovascular diseases, and relates to a polypeptide with anti-cerebral ischemia effect and its application. Background technique [0002] Cerebral ischemia is a common and frequently-occurring disease with high mortality and disability. So far, the only effective treatment is thrombolytic therapy, but this therapy not only has low efficiency, but also must be given within a short time after the occurrence of cerebral ischemia to be effective. Therefore, it is of great significance to further study the molecular mechanism of cerebral ischemic injury, discover new targets, and develop new anti-ischemic drugs. [0003] N-methyl-D-aspartate (NMDA) receptor is an important anti-ischemic target. Researchers have developed a variety of NMDA receptor antagonists, but due to uncertain efficacy or serious adverse reactions is deactivated. In recent years, researchers have focused on the study of NMD...

Claims

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Application Information

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IPC IPC(8): C07K7/08A61K38/10A61P9/10
CPCA61K38/00C07K7/08
Inventor 孙勇军程晓昆高子彬
Owner HEBEI UNIVERSITY OF SCIENCE AND TECHNOLOGY
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