Application of oligopeptide to preparation of medicine for treating angiogenesis ophthalmic diseases

A technology for angiogenesis and ophthalmic diseases, applied in the field of biomedicine, can solve problems such as high treatment costs and increased patient burden

Inactive Publication Date: 2012-10-10
JIANGYIN STEMEASY BIOTECH LTD
View PDF6 Cites 5 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The British National Institute of Health and Clinical Care Optimization also recommends Lucentis as an effective drug for the treatment of all age-related macular degeneration (AMD), but the price of Lucentis is as high as $1,

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
  • Application of oligopeptide to preparation of medicine for treating angiogenesis ophthalmic diseases
  • Application of oligopeptide to preparation of medicine for treating angiogenesis ophthalmic diseases
  • Application of oligopeptide to preparation of medicine for treating angiogenesis ophthalmic diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] The preparation of embodiment 1 short peptide FpAT

[0036] Put the peptide synthesis column filled with 4-(2', 4'2-dimethoxyphenyl-Fmoc-aminomethyl)phenoxyacetamidoethyl resin in the PioneerTM peptide synthesizer according to the following sequence Peptide synthesis was performed under nitrogen:

[0037] 1) Solvate the resin in DMF for 5min;

[0038] 2) Treat the resin with 20% pipecolinic acid in DMF for about 15 minutes to remove the protecting group Fmoc on the resin grafted group (or on the resin-bound amino acid a-amino group);

[0039] 3) Wash the resin with DMF for about 20 minutes;

[0040] 4) Activate the α- Carboxyl;

[0041] 5) Coupling the activated amino acid obtained in step 4 with the resin (or resin-bound amino acid) of step 2 in DMF for about 30 min;

[0042] 6) washing the resin with DMF for 5 min;

[0043] 7) Repeat steps 2-6 with the following amino acids: Fmoc-Val, Fmoc-Gly, Fmoc-Gly, Fmoc-Gly, Fmoc-Glu(γ-0tBu), Fmoc-Ala, Fomc-Leu, Fomc-Phe...

Embodiment 2

[0047] Method or technology used in the experiment of embodiment 2

[0048] 1. Laser-induced CNV method:

[0049] 1% sodium pentobarbital (50mg / Kg) was injected intraperitoneally into BN rats; compound tropicamide eye drops were used to dilate the pupils; contact lenses (ocular three-way mirror) were placed in the eyes of the rats, and the rats were placed in the slit lamp by an assistant Before, use 532 frequency doubled laser (parameters: spot diameter 100μm, power 125mv, exposure time: 0.1s), photocoagulate 8 points in the vascular space 1-1.5PD away from the optic disc, bubbles will be generated after photocoagulation, accompanied by a small amount of bleeding ( or accompanied by a light sound) indicates that the Bruch's membrane has been broken, and it is judged as an effective laser spot.

[0050] 2. Fluorescence angiography (fluorescent angiography, FA): 5 to 7 days after the laser, routine intraperitoneal injection of anesthesia, mydriasis, intraperitoneal injection...

Embodiment 3

[0122] Pharmacodynamic evaluation of embodiment 3 logarithmic dose-effect relationship

[0123] 1. Fluorescence contrast analysis:

[0124] 12-14 days after intravitreal injection, fluorescein contrast examinations were performed in batches, and the pictures were recorded and saved for analysis.

[0125] FA display: blank control group, PBS (NaCl: 8.00g, KCl: 0.20g, NaCl 2 HPO 4 : 1.145g, KH 2 PO 4 : 0.20g, water: 1000ml; the same below) in the mid-term images of the group all showed strong fluorophores in the laser area, the borders were blurred and expanded, and even fused light groups appeared, and the late stage was strongly stained. The irrelevant peptide (randomly designed according to computer software, sequence: Met-Asp-Asp-Asp-Asn-Gly-Ser-Gly-Cys) group also presents a strong fluorophore, with blurred and enlarged boundaries, but the retinal capillary layer is not clear. The Lucentis (commercially available, purchased from Novartis) group showed irregular weak ...

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

No PUM Login to view more

Abstract

The invention relates to an application of oligopeptide FpAT or pharmacy acceptable salt with the amino acid sequences shown by Asp-Ser-Gly-Glu-Gly-Asp-Phe-Leu-Ala-Glu-Gly-Gly-Gly-Val-Arg to the preparation of medicine for preventing and/or treating ophthalmic diseases relevant to angiogenesis. The medicine prepared from the oligopeptide FpAT has the advantages of good curative effect and high safety on ophthalmic diseases relevant to angiogenesis, particularly on diseases relevant to CNV (choroidal neovascularization). In addition, because the chemical ingredients are polypeptide, the preparation technology is mature, the medication cost is low, and the oligopeptide is very suitable for clinic use or popularization.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to the application of short peptides inhibiting angiogenesis in the preparation of drugs for preventing or treating angioproliferative ophthalmic diseases. Background technique [0002] Vascular endothelial growth factor (VEGF) is a homodimeric glycoprotein connected by disulfide bonds, with a molecular weight of 34-45kD, a highly conserved sequence, and an important sequence that is structurally homologous to PDGF , Stable when exposed to heat and acid. VEGF is a member of the platelet-derived growth factor family and is the most direct mitogen for vascular endothelial cells. VEGF is an important angiogenesis factor, which has important biological functions such as increasing the permeability of blood vessels, promoting the proliferation of endothelial cells, and promoting angiogenesis. VEGF is expressed under both physiological and pathological conditions. Under physiologic...

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
IPC IPC(8): A61K38/10A61P9/10A61P27/02A61P27/10
Inventor 陈慧敏徐念沁刘涛顾传虎巩慧
Owner JIANGYIN STEMEASY BIOTECH LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap