Thrombin-inhibited polypeptide and preparation method and application thereof

A technology for inhibiting peptides and thrombin, applied in the field of medicine, can solve the problem of no thrombin inhibitor coming out

Active Publication Date: 2014-12-10
BEOGENE BIOTECH GUANGZHOU
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At this stage, no mature thrombin inhibitors have been developed for the treatment of atherosclerosis

Method used

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  • Thrombin-inhibited polypeptide and preparation method and application thereof
  • Thrombin-inhibited polypeptide and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Chemical Synthesis of Peptides

[0013] Polypeptide 2 was prepared by Fmoc-protected solid-phase synthesis technique. The synthesis reaction was carried out from C-terminal to N-terminal according to the sequence of polypeptide 2, and there were free amino groups on Rink medium (available from Advanced Chem Tech). During each ligation step, the amino acid residues are activated, and the activation mixture contains 4 times as many HBTU, HOBt, DIEA and Fmoc-amino acids as there are free amino groups on the medium. After each amino acid linking reaction, a mixture of pyridine / acetic acid / N-methylimidazole (3:2:0.5) was used to block unlinked free amino groups for 10 minutes. After each amino acid linking reaction and before the next amino acid linking, the Fmoc-group on the medium should be removed, and the Fmoc-group should be removed using dimethylformamide containing 20% ​​piperidine, which takes 15 minutes. Finally, after all amino acid residues were linked sequentia...

Embodiment 2

[0016] Effect of thrombin inhibitory polypeptide 2 on rabbit model of atherosclerosis

[0017] Animal model of rabbit atherosclerosis model was established. 40 male New Zealand white rabbits were randomly divided into 4 groups, respectively: Group A was the blank control group: fed with common feed; Group B was the model control group: model-building + high-fat feed fed; Model + high-fat feed + thrombin inhibitory polypeptide 2 (2.5 mg / kg / d); D is the positive drug intervention group: model + high-fat feed + rosuvastatin tablets (2.5 mg / kg / d). After 7 days of adaptive feeding with common feed, the right carotid artery intima was frostbited with liquid nitrogen in the model control group, drug intervention group and positive drug intervention group, and the model control group, drug intervention group and positive drug intervention group were fed with high-fat diet after operation , and at the same time administered intragastrically, and performed drug intervention treatment, ...

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Abstract

The invention relates to the field of medicine, in particular to a polypeptide compound for preventing and treating, or preventing atherosclerosis. Thrombin-inhibited polypeptide 2 is characterized by comprising the sequence of RGDLFRKSADGFIALMKLKK, is prepared by adopting the Fmoc protective solid phase synthesis technology, and can be connected with an adjuvant in a covalence manner, wherein the adjuvant is bovine serum albumin, human serum albumin or polyethylene glycol; the thrombin-inhibited polypeptide 2 can be applied in treating atherosclerosis related diseases; the atherosclerosis related diseases comprise angina pectoris, myocardial infarction, arrhythmia, stroke, encephalanalosis, intractable hypertension, renal insufficiency and other diseases; the atherosclerosis related diseases can be treated in various methods of administration, including subcutaneous or intramuscular injection, intravenous injection or intravenous drip, oral medication, such as pills and capsules, nasal spray and the like. The thrombin-inhibited polypeptide 2 can inhibit the thrombin in a targeted manner, inhibits blood coagulation, and achieves the function of preventing or treating atherosclerosis.

Description

Technical field: [0001] The invention relates to the field of medicines, in particular to polypeptide compounds used for preventing and treating or preventing atherosclerosis. Background technique: [0002] Atherosclerosis (Atherosclerosis) is a harmful state caused by the deposition of fat, thrombus, connective tissue and calcium carbonate in blood vessels (mainly arteries, but also veins). It is characterized by thickening and hardening of the arterial wall, loss of elasticity, and narrowing of the lumen. Symptoms of atherosclerosis are mainly determined by vascular lesions and the degree of ischemia of the affected organs. Aortic atherosclerosis is often asymptomatic. In patients with coronary atherosclerosis, if the stenosis of the coronary artery reaches more than 75%, angina pectoris, myocardial Infarction, arrhythmia, and even sudden death. Cerebral arteriosclerosis can cause cerebral ischemia, brain atrophy, or cause cerebral blood vessel rupture and bleeding. Rena...

Claims

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Application Information

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IPC IPC(8): C07K7/08C07K1/06C07K1/04A61K38/10A61P9/10A61P9/06A61P9/12A61P13/12
Inventor 罗瑞雪
Owner BEOGENE BIOTECH GUANGZHOU
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