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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 less effective drugs, and achieve the effects of less toxic and side effects, improving neurobehavior, and small molecular weight

Active Publication Date: 2014-03-05
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

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1: the preparation method of pentapeptide and metabolite thereof

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

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

[0028] The amino acid sequence of the 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 Shengnuo Technology Development Co., Ltd., with a purity of more than 98%.

Embodiment 2

[0031] Example 2: Cell experiment of pentapeptide metabolites for treating 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, 37 ℃ constant temperature culture. The cells were subcultured when the confluence reached 90%.

[0034] 2. Drugs

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

[0036] Normal group: normal culture of cells

[0037] Hypoxia group: cell hypoxia treatment

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

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

[0040] Drug group 3: after hypoxia treatment, QCNS26.16mg / kg was administered.

[0041] Drug group 4: after hypoxia treatment, MLIF50mg / kg was administered.

[0042] 3. Experi...

Embodiment 3

[0052] Embodiment 3: Pentapeptide metabolite is used for the animal experiment of treating ischemic cerebrovascular disease

[0053] The pharmacological experiment of the rat electrocoagulation method to make the regional cerebral ischemia model is a commonly used animal experiment to verify that the drug has the effect of preventing and treating ischemic cerebrovascular disease (Xu Shuyun, Bian Rulian, Chen Xiu. Pharmacological Experimental Methodology (Third Edition). People's Health Publishing House, 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 reared in groups of 6 rats / cage, and divided into 10 groups. Purchased from Shanghai Slack Experimental Animal Co., Ltd., quality certificate number (animal certificate number: SCXK (Shanghai) 2007-0005). Raised in a clean animal room.

[0056] 2. Drugs

[0...

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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 the preparation of drugs 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 rate in the world, which greatly threatens the health and quality of life of human beings, especially the elderly, and has become a global Huge burden on society's health resources. Clinically, the mortality and disability rate of ischemic stroke has taken the first place among neurological diseases. At present, there are few effective drugs used in 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 in...

Claims

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Application Information

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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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