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Glycine-L-cysteine-L-phenylalanine tripeptide and application thereof to preparation of medicines for treating stroke

A technology of cysteine ​​and phenylalanine, applied in the field of medicine, can solve the problems of central nervous system adverse reactions, toxicity, side effects, and poor effect, and achieve the effect of improving cerebral infarction volume and treating stroke

Inactive Publication Date: 2016-06-22
WUHAN HONGYUE MEDICAL SCI INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Almost all of these neuroprotective drugs have been proven to have neuroprotective effects in animal experiments, but clinical trials have proved to be ineffective or poorly effective, and some drugs even have obvious toxic side effects, resulting in unbearable central nervous system adverse reactions for patients or other organ toxicity, making the study of neuroprotection stagnant

Method used

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  • Glycine-L-cysteine-L-phenylalanine tripeptide and application thereof to preparation of medicines for treating stroke
  • Glycine-L-cysteine-L-phenylalanine tripeptide and application thereof to preparation of medicines for treating stroke
  • Glycine-L-cysteine-L-phenylalanine tripeptide and application thereof to preparation of medicines for treating stroke

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] [Example 1] The preparation process of glycine-L-cysteine-L-phenylalanine tripeptide (Gly-Cys-Phe) is as follows:

[0020] 1. Synthesis of complex IFmoc-L-Phe-resin:

[0021] The tripeptide of this patent uses the method of solid-phase synthesis, weighs 10.7 g of 2-chlorotrityl chloride resin (2-ChlorotritylChloride Resin) with a degree of substitution of 0.4 mmol / g, puts the resin into a polypeptide reaction tube, and adds dichlorotrityl chloride Methane (DCM) 160.5ml, shaken for 30 minutes; filter the DCM solvent through the sand core, add 12mmol of Fmoc-L-Phe-OH amino acid, and then add 40mmol of N,N-diisopropylethylamine (DIEA), Finally, a small amount of dimethylformamide (DMF) was added to dissolve, and shaken for 1 h. Alternately wash 6 times with DMF and DCM. Add 160.5ml of 20% piperidine (piperidine is dissolved in DMF solution), take out the piperidine after 5 minutes, add 160.5ml of 20% piperidine again, wait for 15 minutes, take out the piperidine solution...

Embodiment 2

[0036] [Example 2] Cytotoxicity test of GCF on primary cortical neurons

[0037] In this example, the primary cortical neurons cultured for 10 days were used as the experimental object. After the neurons were treated with different concentrations of GCF, cck8 was used to evaluate the cell viability, so as to judge the cytotoxicity of GCF. The phosphorylation level of Akt was used to illustrate the effect of GCF on Whether nerve cells have a protective effect.

[0038] 1. Main experimental reagents and instruments

[0039] GCF was synthesized by our laboratory; Neurobasal, provided by Gibco; B27, provided by Gibco; FBS, provided by Invitrogen; glutamax, provided by Invitrogen; Glutamicacid, provided by sigma; polylysine, provided by sigma. RIPA lysate was provided by Beijing Pulilai Gene Technology Co., Ltd.; BCA kit was provided by American Thermo Company; protein marker was provided by American Thermo Company; glycine was provided by Wuhan Kerui Biotechnology Co., Ltd.; Tris...

Embodiment 3

[0059] [Example 3] Establish a rat cerebral ischemia model, inject fluorescently labeled GCF intravenously, and observe the ability of GCF to penetrate the blood-brain barrier as a whole

[0060] 1. The main reagents and instruments of the experiment

[0061] FITC, Wuhan Minghao Biotechnology Co., Ltd.; FITC-GCF, Wuhan Minghao Biotechnology Co., Ltd.; OCT glue, Beijing Zhongshan Jinqiao Biotechnology Co., Ltd.; pathological tissue slicer, Leitz, Germany, type 1512; fluorescence microscope, Ningbo Sunny Instrument Co., Ltd.; Paraformaldehyde, Sinopharm Chemical Reagent Co., Ltd.

[0062] 2. Experimental principle

[0063]FITC (fluorescein isothiocyanate): It is yellow or orange-yellow crystalline powder with a molecular weight of 389.4, a maximum absorption wavelength of 490-495nm, and a maximum emission wavelength of 520-530nm, showing bright yellow-green fluorescence. The broadest fluorescein.

[0064] FITC-GCF: GCF is fluorescently labeled. FITC is combined with GCF tripe...

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Abstract

The invention belongs to the field of medicines and provides application of a glycine-L-cysteine-L-phenylalanine tripeptide to preparation of medicines for treating stroke.According to animal experiments, by means of intravenous administration, the tripeptide penetrates blood brain barriers to enter brain tissues and cells so as to evidently reduce cerebral infarction volume of rats, and a stroke treatment function is realized.The glycine-L-cysteine-L-phenylalanine tripeptide available for conventional intravenous administration is functionally superior to existing clinical medicines.

Description

technical field [0001] The invention belongs to the field of medicine, and specifically relates to the application of glycine-L-cysteine-L-phenylalanine (Gly-L-Cys-L-Phe, GCF for short) tripeptide in the preparation of stroke medicine. Background technique [0002] Stroke is a sudden onset cerebral blood circulation disorder, clinically manifested as symptoms and signs of one-time or permanent brain dysfunction. Stroke is divided into ischemic stroke and hemorrhagic stroke according to its nature. Stroke is a refractory disease that seriously endangers human life and safety. It has the characteristics of high morbidity, high disability and high mortality. In 2008, in the ranking of causes of death announced by the Ministry of Health of my country, stroke ranked No. 1 among cities. Three, the second leading cause of death in rural areas, among which ischemic stroke accounts for 75%-85% of stroke patients. Therefore, the development of a drug against ischemic stroke has broad...

Claims

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Application Information

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IPC IPC(8): C07K5/083A61K38/06A61P9/10
Inventor 万芪庄扬陈娟万沙
Owner WUHAN HONGYUE MEDICAL SCI INC
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