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Glycine-L-cysteine-homotaurine tripeptide and application thereof

A technology of cysteine ​​and homotaurine, applied in peptides, dipeptide components, cardiovascular system diseases, etc.

Active Publication Date: 2013-03-20
HUANA TIME HEALTH TECH WUHAN CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Glycine-L-cysteine-homotaurine tripeptide is synthesized from three amino acids glycine, cysteine ​​and homotaurine. Glycine-L - The role of cysteine-homotaurine tripeptide in the treatment of stroke has not been reported

Method used

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  • Glycine-L-cysteine-homotaurine tripeptide and application thereof
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  • Glycine-L-cysteine-homotaurine tripeptide and application thereof

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Embodiment 1

[0015] Glycine-L-cysteine-homotaurine tripeptide (Gly-Cys-NHCH 2 CH 2 CH 2 SO 3 H) The preparation includes the following steps: the final product Gly-Cys-NHCH 2 CH 2 CH 2 SO 3 H was synthesized by our company for the first time.

[0016] 1. Synthesis of N-Fmoc-S-trityl-L-cysteine-homotaurine [Fmoc-Cys(Trt)-NHCH 2 CH 2 CH 2 SO 3 H(Compound I)]

[0017] raw material molecular weight amount of substance Dosage N-Fmoc-S-trityl-L-cysteine ​​(Fmoc-Cys(Trt)-OH) 585.73 12mmol 7g N-Hydroxysuccinimide (HOSu) 115.2 14mmol 1.6g Carbodiimide hydrochloride (EDCI) 191.7 14mmol 2.68g Homotaurine (NH 2 CH 2 CH 2 CH 2 SO 3 h) 139.17 10mmol 1.4g Na 2 CO 3 106 10mmol 1.06g

[0018] Fmoc-Cys(Trt)-OH (7 g) and HOSu (1.6 g) were dissolved in 40 ml tetrahydrofuran (THF), then EDCI (2.68 g) was added and stirred overnight at room temperature. Homotaurine (1.4g) and Na 2 CO 3 (1.06g) was dissolved in water (40ml...

Embodiment 2

[0041] Glycine-L-cysteine-homotaurine tripeptide lipid microsphere injection, according to glycine-L-cysteine-homotaurine tripeptide 0.8%, lecithin for injection 2.3%, The injection is prepared by adding 6% of soybean oil, 6% of medium-chain fatty acid for injection, 2% of glycerin, 0.2% of Tween-80, 0.04% of sodium oleate and 100% of water for injection. Specific preparation method: disperse 2% glycerin for injection and 0.04% sodium oleate in appropriate amount of water for injection. Stir at 75°C until completely dissolved, and adjust the pH of the water phase to 6.5; add glycine-L-cysteine-homotaurine tripeptide to the mixed oil phase composed of soybean oil and medium-chain fatty acids, at 80°C Heat and stir for 30 minutes, then remove impurities through a 0.22 μm microporous membrane to obtain a clear primary oil phase, add phospholipids, heat and stir at 80°C, slowly add to the water phase, and stir for 10 minutes; the resulting colostrum is adjusted to pH with hydrochl...

Embodiment 3

[0043] The glycine-L-cysteine-homotaurine tripeptide composition comprises 100 g of glycine-L-cysteine-homotaurine tripeptide plus water for injection to 1 liter, and is packaged in 500 tubes. The preparation method is: take water for injection, add 0.5g of EDTA-2Na, add 100g of glycine-L-cysteine-homotaurine tripeptide to dissolve, add 24g of sodium bicarbonate powder in portions, stir until completely dissolved, and adjust the pH Between 5.8 and 6.2. Sterilized packaging, each containing glycine-L-cysteine-homotaurine tripeptide 200mg.

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Abstract

The invention provides a new matter glycine-L-cysteine-homotaurine tripeptide and an application of the glycine-L-cysteine-homotaurine tripeptide in the preparation of medicines for treating cerebral apoplexy. The anti-cerebral apoplexy medicines prepared by glycine-L-cysteine-homotaurine tripeptide products have better curative effect. The animal experiment shows that the glycine-L-cysteine-homotaurine tripeptide can improve the behaviors of rats and has the effect on cerebral apoplexy treatment. The effect of the tripeptide is obviously superior to the same dose of homotaurine, taurine and other compounds reported by existing literatures or traditional medicines for clinical use.

Description

technical field [0001] The present invention relates to a new compound and its application, in particular to glycine-L-cysteine-homotaurine tripeptide and its application in the preparation of medicine for treating cerebral apoplexy. Background technique [0002] Stroke is a sudden onset of cerebral blood circulation disorders. It refers to patients with cerebrovascular diseases. The cerebral arteries are narrowed, occluded or ruptured due to various predisposing factors, resulting in acute cerebral blood circulation disorders. Clinical manifestations Symptoms and signs of transient or permanent brain dysfunction. Stroke is one of the main causes of disability and dementia among the elderly. According to the data published by WHO, among 57 countries, 40 countries have listed the death rate of stroke among the top three, among which stroke is in Japan and China. The death rate has taken the first place. Ischemic stroke accounts for 60%-70% of the total number of stroke pati...

Claims

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Application Information

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IPC IPC(8): C07K5/062A61K38/05A61P9/10
Inventor 丁虹武双婵岳源
Owner HUANA TIME HEALTH TECH WUHAN CO LTD
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