Polypeptide having protection effect on cerebral ischemic injuries, and its application

A technology of protection and cerebral ischemia, applied in the field of drugs for cerebrovascular disease, can solve the problems of improper thrombolytic therapy, increase the risk of cerebral hemorrhage, etc., and achieve the effect of clear protection.

Inactive Publication Date: 2013-08-28
NANJING MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The application of thrombolytics helps to restore the blood flow in the ischemic area, but inappropriate thrombolytic therapy can also increase the risk of cerebral hemorrhage

Method used

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  • Polypeptide having protection effect on cerebral ischemic injuries, and its application
  • Polypeptide having protection effect on cerebral ischemic injuries, and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Example 1. Preparation of polypeptide (RKKRRQRRRTDRLFMNSIWPG)

[0038] Using chemical synthesis, starting from the C-terminal, that is, synthesis from right to left. Select 0.5 g of Fmoc-GLy-Wang Resin, soak the resin with DCM for 5-10 minutes, wash with DMF 5 times, deprotect with 20%wt hexahydropyridine for 10-20 minutes, and wash with DMF for 5 times. Amino acid condensation: according to the sequence order (C-terminal to N-terminal), the raw materials used are Fmoc-Pro-OH, Fmoc-Trp(Boc)-OH, Fmoc-Ile-OH, Fmoc-Ser(tbu)-OH, Fmoc -Asn(trt)-OH, Fmoc-Met-OH, Fmoc-Phe-OH, Fmoc-Leu-OH, Fmoc-Arg(pbf)-OH, Fmoc-Asp(otbu)-OH, Fmoc-Thr(tbu) -OH, Fmoc-Gln(trt)-OH, Fmoc-lys(Boc)-OH, FITC. Add corresponding amino acids and condensing agents to the treated resin one by one to condense for 30 minutes to 1 hour, wash with DMF 5 times, remove Fmoc protection with decapping solution, decap for 15 minutes, and then wash with DMF. Repeat condensation-cleaning-deprotection-cleaning. Th...

Embodiment 2

[0039] Example 2. Effect of polypeptide on SR-A-mediated macrophage apoptosis

[0040]SR-A is involved in the apoptosis process of macrophages. When macrophages are co-treated with fucoidan sulfate [fucoidan, Fuc (SR-A ligand)] and thapsigargin (Tg), it will cause its apoptosis. RAW264.7 mouse macrophages were stimulated with 50 μg / mL fucoidan, 0.5 μM thapsigargin alone and 50 μg / mL fucoidan+0.5 μM thapsigargin at the same time. The polypeptide treatment group was pretreated with 10 μM polypeptide for half an hour, and then the above treatment was continued, and after 12 hours Cells were harvested for Annexin V / PI staining, and then apoptotic cells were detected by flow cytometry. When fucoidan or thapsigargin is used alone, RAW264.7 cells will not undergo apoptosis; however, when fucoidan and thapsigargin are used to stimulate RAW264.7 cells, it is observed that a large number of RAW264.7 cells undergo apoptosis, and RAW264.7 cells undergo apoptosis in the peptide treatment ...

Embodiment 3

[0041] Example 3. Effect of polypeptide on cerebral infarct size after cerebral ischemia

[0042] Experimental animal models and groups:

[0043] After the mice were anesthetized with 5% chloral hydrate (0.07mL / 10g body weight), they were fixed supine on a 37°C constant temperature operating table, and the anterior neck skin was incised in the middle, and the right common carotid artery, internal carotid artery and External carotid artery, ligate the common carotid artery, cut a small incision about 2-3 mm from the bifurcation of the external carotid artery, and insert an 8.0 MCAO thread plug into the internal carotid artery through the incision to block the beginning of the middle cerebral artery . After the operation, the mice were fed in cages and had free access to food and drink. The sham-operated animals were the same as the model animals except that no suture was inserted.

[0044] The experiment was divided into two groups: ①WT+MCAO; ②peptide (0.5mg / kg)+MCAO.

[00...

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Abstract

The invention provides a polypeptide having a protection effect on cerebral ischemic injuries, and its application in the preparation of medicines for treating cerebrovascular diseases. The peptide chain fragment sequence of the polypeptide is RKKRRQRRRTDRLFMNSIWPG. The polypeptide can enter cells in a high speed and high efficiency manner, can enter the cells in a 10mum concentration within 30min, has a dose-dependent inhibition effect on the macrophage SR-A expression, and has a clear protection effect on the cerebral ischemic injuries.

Description

technical field [0001] The invention belongs to the technical field of medicines for cerebrovascular diseases, and the invention relates to a kind of polypeptide with protective effect on cerebral ischemia injury and application thereof. Background technique [0002] Cerebrovascular disease is a disease that seriously endangers human health, and has become one of the important causes of human disability and death. Cerebrovascular disease (CVD for short) refers to brain lesions caused by abnormalities in cerebrovascular vessels. Stroke generally refers to acute cerebrovascular disease. [0003] Cerebrovascular diseases can be simply divided into two categories, one is ischemic cerebrovascular disease caused by the reduction or interruption of blood flow, and the other is hemorrhagic cerebrovascular disease caused by rupture of blood vessels. Ischemic stroke accounts for 60%-70% of the total number of stroke patients. Thrombolytic agent-tissue plasminogen activator (tissue ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/00A61K38/16A61P9/10
Inventor 陈琪李楠王晓花李晓宇
Owner NANJING MEDICAL UNIV
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