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

Use of glucagons-like peptide-1 analogue in preparation of ophthalmic disease drug

A technology for ophthalmic diseases and analogs, which is applied in the field of preparation of drugs for the treatment of ischemic or nerve-injured ophthalmic diseases, glucagon-like peptide-1 analogs, which can solve problems such as unsatisfactory prognosis and improve visual function , the effect of inhibiting the retinal inflammatory response

Inactive Publication Date: 2014-07-09
AFFILIATED HUSN HOSPITAL OF FUDAN UNIV
View PDF2 Cites 16 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although these treatments can delay the progression of the disease or improve symptoms to a certain extent, most of them are relatively late interventions that cannot fundamentally eliminate the cause of diabetes, so the prognosis is not ideal

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
  • Use of glucagons-like peptide-1 analogue in preparation of ophthalmic disease drug
  • Use of glucagons-like peptide-1 analogue in preparation of ophthalmic disease drug
  • Use of glucagons-like peptide-1 analogue in preparation of ophthalmic disease drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1 Intravitreal injection of Exendin-4 has the effect of protecting the retinal function of rats, making the total amplitude of ERG b wave and 0ps close to the normal level

[0039]The degree of diabetic retinopathy in rats and the functional state of the retina were detected by the method of full-field flash ERG. The results showed that at 16 weeks, the amplitudes of b waves and Ops waves of rats injected with GK normal saline decreased significantly, which was higher than that of Wistar. Rats were reduced by 43.9±4.7% (eg figure 2 A, B shown) and 37.4±6.8% (as shown figure 2 Shown in C and D), while the amplitude of GK rats E4 treatment group was significantly increased, the amplitude of b wave was 206.7±21.5mV (121.2±12.9mV for GK rats, P<0.05), and the amplitude of Ops was 91.7±9.0mV (GK rats are 49.6 ± 9.1mV, P<0.05), there is no significant statistical difference between the b wave and Ops amplitude of GK rat E4 treatment group and Wistar rats, suggestin...

Embodiment 2

[0040] Example 2 Intravitreal injection of Exendin-4 can prevent the thinning of diabetic retina and the loss of cells in each nuclear layer, and make the morphological indicators such as retinal thickness and outer nuclear layer cell count in diabetic rats approach to normal levels.

[0041] The results of HE staining and morphological examination showed that in the retina of 16-week-old GK rats, GCL, INL, and ONL layers were significantly reduced compared with Wistar rats, and the initial cell loss appeared in the ganglion cell layer (61.3% ± 4.8%, n=12; p image 3 Shown in A and B) and outer nuclear layer (72.5±1.8% of Wistar rats, n=12; p image 3 Shown in A), in the inner nucleus layer of the retina, there is also obvious cell loss (78.7±5.3% for Wistar rats, n=12; p image 3 Shown in A), Exendin-4 can significantly reduce the cell reduction in the ganglion cell layer and the outer nuclear layer, and the ganglion cell count and the outer nuclear layer cell count in the Exendin...

Embodiment 3

[0042] Example 3 Intravitreal injection of Exendin-4 can increase the expression of GLP-1R and increase the expression of anti-apoptotic gene Bcl-xL Bcl-2, thereby inhibiting the apoptosis of diabetic retinal cells

[0043] The expression of GLP-1R was significantly down-regulated in 16-week-old GK rats compared with Wistar rats (75.1±2.8% of Wistar rats, such as image 3 shown in B), but the Exendin-4 treatment group was significantly up-regulated (131.3±6.2% of GK rats, such as image 3 Shown in B), the immunostaining of retinal GLP-1R is consistent with the expression of GLP-1R detected by Western blot (such as image 3 C), immunohistochemistry showed that GLP-1R was mainly expressed in the inner retinal layer (including ganglion cell layer, inner plexiform layer, inner nuclear layer) and the inner segment of photoreceptors (such as image 3 C shown);

[0044] Western blot detection of the expression of mitochondria-dependent apoptosis-related genes (Bcl-2, Bcl-xL and Bax...

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 belongs to the field of medicine, relates to a use of a glucagons-like peptide-1 analogue in pharmacy, and particularly relates to the use of the glucagons-like peptide-1 analogue Exendin-4 in preparation of an ophthalmic disease drug. With adopting of the exogenous glucagons-like peptide-1 analogue Exendin-4, a diabetic retinopathy animal model experiment is carried out, and results show that the Exendin-4 can inhibit retinal inflammatory responses caused by glial cell activation, resists retinal cell apoptosis caused by diabetes and the like, significantly improves visual functions, can be used as the drug for treating some ophthalmic diseases and especially as the drug for treating ocular ischemic and optic nerve injury diseases, and treats ophthalmic diseases comprising diabetic retinopathy, hypertensive retinopathy, retinal vein occlusion and the like.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to the use of glucagon-like peptide-1 analogues in pharmacy, in particular to the use of glucagon-like peptide-1 analogue Exendin-4 in the preparation of medicines for ophthalmic diseases, in particular to the use of Use of glucagon-like peptide-1 analogue Exendin-4 in the preparation of medicines for treating ischemic or nerve-damaging ophthalmic diseases (such as diabetic retinopathy, etc.). Background technique [0002] The prior art discloses that Exendin-4 is a GLP-1 (glucagons-like peptide-1) analog extracted from lizard salivary glands, which has the same amino acid sequence as mammalian GLP-1 53% homology. At the same time, it can promote the secretion of pancreatic insulin, increase insulin sensitivity and improve the function of pancreatic islet cells, and is not decomposed by dipeptidyl peptidase IV (DPP-IV), and has a longer plasma half-life. According to reports, it has been used...

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): A61K38/17A61P27/02A61P9/10A61P25/02A61P27/10
Inventor 叶纹张瑜范毅超肖以钦张晓燕
Owner AFFILIATED HUSN HOSPITAL OF FUDAN UNIV
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