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Pentapeptide metabolite and application of pentapeptide metabolite in preparation of medicament for preventing and treating ischemic cerebrovascular diseases

A technology for cerebrovascular disease and metabolites, applied in the field of medicine, can solve the problem of few effective drugs and achieve the effect of small toxic and side effects, small molecular weight and strong protective effect

Active Publication Date: 2015-05-27
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are few effective drugs used in the treatment of ischemic cerebrovascular disease at home and abroad

Method used

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  • Pentapeptide metabolite and application of pentapeptide metabolite in preparation of medicament for preventing and treating ischemic cerebrovascular diseases
  • Pentapeptide metabolite and application of pentapeptide metabolite in preparation of medicament for preventing and treating ischemic cerebrovascular diseases
  • Pentapeptide metabolite and application of pentapeptide metabolite in preparation of medicament for preventing and treating ischemic cerebrovascular diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1: Preparation method of pentapeptide and its metabolites

[0026] The amino acid sequence of monocyte migration inhibitor Met-Gln-Cys-Asn-Ser (MLIF) is shown in SEQ ID NO: 1;

[0027] The amino acid sequence of dipeptide Met-Gln (MQ) is shown in SEQ ID NO: 2;

[0028] The amino acid sequence of dipeptide Asn-Ser (NS) is shown in SEQ ID NO: 3;

[0029] The amino acid sequence of the tetrapeptide Gln-Cys-Asn-Ser (QCNS) is shown in SEQ ID NO: 4;

[0030] The above polypeptide molecules were synthesized by Chengdu Sunna Technology Development Co., Ltd., and the purity was above 98%.

Embodiment 2

[0031] Example 2: Cell experiments of pentapeptide metabolites for the treatment of ischemic cerebrovascular disease

[0032] 1. Cells

[0033] Brain microvascular endothelial cells (bEnd3 cells, purchased from ATCC, USA) were cultured in high glucose DMEM medium containing 10% fetal bovine serum (FBS), 5% CO 2 cell culture incubator at 37°C. Subculture was carried out when the cell confluence reached 90%.

[0034] 2. Drugs

[0035] Experimental grouping: (molar concentration is 8.6 × 10 -5 mol / L)

[0036] Normal group: cells cultured normally

[0037] Hypoxia group: cellular hypoxia treatment

[0038] Drug group 1: After the cells were treated with hypoxia, MQ23.84mg / L was given.

[0039] Drug group 2: After the cells were treated with hypoxia, NS18.85mg / kg was given.

[0040] Drug group 3: After the cells were treated with hypoxia, QCNS 26.16 mg / kg was given.

[0041] Drug group 4: After the cells were treated with hypoxia, MLIF was given at 50 mg / kg.

[0042] 3. E...

Embodiment 3

[0052] Example 3: Animal experiments of pentapeptide metabolites for the treatment of ischemic cerebrovascular disease

[0053] The pharmacological experiment of rat electrocoagulation to make focal cerebral ischemia model is a commonly used animal experiment to verify that drugs can prevent and treat ischemic cerebrovascular disease (Xu Shuyun, Bian Rulian, Chen Xiu. Pharmacological Experiment Methodology (Third Edition). People's Health Press, 2002: 1061-1062.), so it was used to verify the protective effect of pentapeptide metabolites on cerebral ischemia in experimental animals.

[0054] 1. Animals

[0055] Healthy male Wistar rats, weighing 200-250 g, were group-housed with 6 rats / cage in each group, and were divided into 10 groups. Purchased from Shanghai Slack Laboratory Animal Co., Ltd., quality certificate number (animal certificate number: SCXK (Shanghai) 2007-0005). Housed in a clean-grade animal room.

[0056] 2. Drugs

[0057] Group experimental rats into grou...

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Abstract

The invention relates to the technical field of medicines. A monocyte locomotion inhibiting factor, which is called pentapeptide or MLIF for short, has the effects of inhibiting locomotion of monocytes and inhibiting expression of IL-1beta (interleukin-1beta), IFN-gamma (interferon-gamma), IL-5 (interleukin-5), IL-6 (interleukin-6) and other inflammation factors, and has the effects of preventing and treating ischemic cerebrovascular diseases and myocardial ischemia. The invention further discovers that partial metabolites dipeptide Met-Gln and tetrapeptide Gln-Cys-Asn-Ser in the body of MLIF have the effect of preventing and treating ischemic cerebrovascular diseases. The invention provides application of the pentapeptide metabolite shown in SEQ ID No:2 or SEQ ID NO:4 in prevention of medicaments or health-care foods for prevention or treating ischemic cerebrovascular diseases.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to pentapeptide metabolites and their application in preparing medicines for preventing and treating ischemic cerebrovascular diseases. Background technique [0002] Ischemic cerebrovascular disease (ischemic stroke) is one of the diseases with the highest morbidity, mortality and disability rates in the world, which greatly threatens the health and quality of life of human beings, especially the elderly. Huge burden on social health resources. Clinically, the mortality and disability rate of ischemic stroke have taken the first place among neurological diseases. At present, there are few effective drugs for the treatment of ischemic cerebrovascular disease at home and abroad. Therefore, it is of great significance to carry out in-depth research on drug prevention and treatment of ischemic cerebrovascular disease. [0003] Monocyte locomotion inhibitor factor (abbreviation: pent...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/05A61K38/07C07K5/06C07K5/10A23L1/29A61P9/10A61P29/00A23L33/00
Inventor 章越凡芮耀诚李铁军张恩德黄景华王习著
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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