Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

A synthetic peptide for the treatment of neurological diseases

A technology for synthesizing peptides for nervous system diseases, applied in the fields of nervous system diseases, cardiovascular system diseases, peptides, etc., can solve the problems of serious side effects, large doses, limited clinical application, etc., to achieve less side effects and improve oxidative stress damage. , improve the effect of cognitive dysfunction and dementia

Active Publication Date: 2019-09-17
WUHAN HONGYUE MEDICAL SCI INC
View PDF3 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Although both glycine and cysteine ​​have obvious brain protective effects, the peripheral doses of glycine (800mg / kg) and cysteine ​​(500mg / kg) are too large, resulting in severe side effects, which limit their clinical application

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • A synthetic peptide for the treatment of neurological diseases
  • A synthetic peptide for the treatment of neurological diseases
  • A synthetic peptide for the treatment of neurological diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] [Example 1] This patent takes L-proline-glycine-L-cysteine-L-phenylalanine tripeptide (PGCF) as an example to illustrate the preparation process of the solid-phase synthetic peptide as follows:

[0056] 1. Synthesis of Complex I Fmoc-L-Phe-resin:

[0057] The tripeptide of this patent uses the method of solid-phase synthesis, weighs 10.7g of 2-chlorotrityl chloride resin (2-Chlorotrityl Chloride Resin) with a degree of substitution of 0.4mmol / g, puts the resin into a polypeptide reaction tube, and adds Dichloromethane (DCM) 160.5ml, shaken for 30 minutes; filter the DCM solvent through sand core, add 12mmol of Fmoc-L-Phe-OH amino acid, then add 40mmol of N,N-diisopropylethylamine (DIEA ), and finally add a small amount of dimethylformamide (DMF) to dissolve, shake for 1h. 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 ...

Embodiment 2

[0078] [Example 2] Cytotoxicity test of the patent synthetic peptide on primary cortical neurons

[0079] In this example, the primary cortical neurons cultured for 10 days were used as the experimental object to establish an isolated glucose-oxygen deprivation (OGD) model of cortical neurons. In the case of OGD injury, the neurons were treated with 500 μM of each synthetic peptide. Use cck8 to evaluate the viability of cells, so as to judge whether each synthetic peptide has a protective effect on neurons. The synthetic peptide used in this embodiment is as follows:

[0080]

[0081] 1. Main experimental reagents and instruments

[0082]Each synthetic peptide in the experiment was independently synthesized by our laboratory; Neurobasal, provided by Gibco; B27, provided by Gibco; FBS, provided by Invitrogen; glutamax, provided by Invitrogen; Glutamicacid, provided by sigma; , provided by sigma company. Incubator, from SANYO company, the culture condition is 37 ℃, 5% CO2;...

Embodiment 3

[0102] [Example 3] Establish a rat cerebral ischemia model, inject fluorescently labeled synthetic peptides intravenously, and observe the ability of the synthetic peptides to penetrate the blood-brain barrier as a whole

[0103] 1. The main reagents and instruments of the experiment

[0104] FITC, Wuhan Minghao Biotechnology Co., Ltd.; FITC-GC, FITC-GCF, FITC-PGCF, 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.

[0105] 2. Experimental principle

[0106] 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.

[0107] FITC-PGCF: PGCF...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
correlation coefficientaaaaaaaaaa
Login to View More

Abstract

The invention belongs to the technical field of biological medicines, and particularly relates to a synthetic peptide and application thereof to the preparation of a medicine for treating brain injury. The amino acid sequence of the synthetic peptide is X1-X2-X3- (Gly-L-Cys)n-X4-X5-X6-X7, wherein X1 is null or L-Phe, X2 is null or Gly, X3 is null or L-Pro, X4 is null or Gly, X5 is null or L-Pro, X6 is null or Gly and X7 is null or L-Phe; X3 and X5 cannot be null at the same time, when X3 is null, X2 is also null, and when X5 is null, X6 is also null; X1 and X7 cannot be null at the same time, when X3 and X5 are L-Pro, n is smaller than or equal to 6, and when X3 or X5 is L-Pro, n is smaller than or equal to 8. Animal experiments show that the synthetic peptide can run through a blood-brain barrier to reach the brain through intravenous administration at a very low dosage.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to a synthetic peptide and its application in preparing medicine for treating brain injury. Background technique [0002] Glycine is the amino acid with the simplest chemical structure, but it has complex functions. Glycine is an important inhibitory neurotransmitter in the central nervous system, playing an important role in controlling neuronal excitability. Animal experiments have found that glycine has obvious neuroprotective effects, and it has also been found in some clinical trials that glycine can significantly improve cognitive dysfunction and dementia, especially as a conventional neuroleptic for the treatment of schizophrenia. In addition to this, glycine can also treat heart damage and stroke. [0003] L-cysteine ​​is a neuromodulatory substance and an antioxidant with neuroprotective effects. At the same time, it is also an important synthesis unit of...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): C07K7/06C07K7/08A61K38/08A61K38/10A61P25/00A61P9/10A61P25/28A61P25/16
Inventor 万芪陈娟庄杨张娅万沙
Owner WUHAN HONGYUE MEDICAL SCI INC
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com