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

Application of GLP-1R micromolecule agonist in diabetes and related complications and medicine

A GLP-1R, 1.GLP-1R technology is applied in the field of drug preparation for diabetes-related complications, which can solve the problems of complex cost, unclear research on the hypoglycemic mechanism of components with hypoglycemic effect, etc., and achieves improvement of diabetes-related complications. Effect

Pending Publication Date: 2022-08-05
XI AN JIAOTONG UNIV
View PDF5 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, as a complex cost of traditional Chinese medicine, its components that exert hypoglycemic effects and their hypoglycemic mechanisms are still unclear
In addition, the role of GLP-1R small molecule agonists in the treatment of diabetes and its complications is still blank

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 GLP-1R micromolecule agonist in diabetes and related complications and medicine
  • Application of GLP-1R micromolecule agonist in diabetes and related complications and medicine
  • Application of GLP-1R micromolecule agonist in diabetes and related complications and medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1. Alizarin and Schisandrin B have specific binding to GLP-1R protein

[0039] CMC is an affinity chromatography. By preparing a specific receptor overexpressed cell membrane into a stationary phase, high-throughput screening of components that specifically bind to membrane receptors can be achieved under biomimetic conditions. It is an effective method for screening complex components. reliable means. Construct GLP-1R high expressing cells, prepare cell membrane, adsorb with activated silica gel to prepare cell membrane chromatographic stationary phase, and use wet method to pack the column to obtain SiO 2 - GLP-1R / CMC chromatographic column for HPLC detection. SiO 2 - NC-HEK293 / CMC is a CMC control for protein specific binding. The results are shown in Table 1, rubidin and schisandra B have retention on the GLP-1R high-expressing cell membrane chromatographic column, but no retention on the blank control chromatographic column. The above results show that ...

Embodiment 2

[0043] Example 2. Investigation of the protein binding sites of alizarin, schisandrin B and GLP-1R

[0044] Molecular docking studies were performed using AutoDock Vina software. Enter the protein X-ray crystal structure (PDB code: 5VAi). The protein structure removes water molecules and adds hydrogen atoms, and uses the Tripos force field and Pullman charge for minimum energy processing. ChemDraw version 19.0 was used to draw the structure of rubiacin, and ChemDraw 3D software was used to optimize the structure. The ligand structure was optimized by AutoDock software, the charges in the ligand residues were dispersed, the root of the ligand was determined and the twistable bond was selected. Run the AutoDock software under the Linux terminal, load the optimized protein and the energy-optimized rubidin in sequence, calculate the grid energy by Autogrid, and use the Lamarck genetic algorithm to evaluate the binding of the ligand and the receptor by the free energy method. . ...

Embodiment 3

[0049] Example 3. Protective effects of rubidin and schisandrin B on adrenal pheochromocytoma cells in rats injured by high glucose

[0050] PC12 cells at 3 x 10 3 The density was inoculated in a 96-well plate, and the medium was supplemented to 100 μL per well. 37°C, 5% CO 2 Incubate adherent for 24 hours. Aspirate the medium, add 90 μL of 125 mM glucose to each well, add 10 μL of different concentrations of rubiacin prepared in the medium to the experimental wells, add 10 μL of medium to the control wells, and continue to culture at 37°C for 48 h. After 48 hours, 10 μL of 5 mg / mL MTT solution was added to the medium, incubated at 37°C for 4 hours, the medium was aspirated, 100 μL of DMSO solution was added to it, and 100 μL of DMSO solution was added to it. The absorbance of the solution was measured, and the effect of rubidin on cell viability was calculated.

[0051]

[0052] The result is as figure 1 As shown, it can be seen that alizarin and schisandrin B have pr...

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 discloses application of a GLP-1R micromolecular agonist in diabetes and related complications thereof and a medicine, and belongs to the technical field of preparation of medicines for the related complications of diabetes mellitus. The GLP-1R micromolecular agonist represented by rubimagin and schisandrin B is determined through research, and the GLP-1R micromolecular agonist can be used for preparing the medicines for the related complications of diabetes mellitus through specific binding with GLP-1R protein. The traditional Chinese medicine composition plays a wide and comprehensive role and can be used for treating diabetes mellitus and related complications thereof.

Description

technical field [0001] The invention belongs to the technical field of medicine preparation for diabetes-related complications, and relates to the application and medicine of a GLP-1R small molecule agonist in the preparation of diabetes-related complications with GLP-1R protein as a target. Background technique [0002] Diabetes mellitus is a metabolic syndrome caused by a combination of genetic and environmental factors, characterized by chronic hyperglycemia, and is often accompanied by extensive damage to multiple organs and systems. Diabetes has become one of the most serious social health problems facing the world in the 21st century. Among them, type 2 diabetes mellitus (T2DM) is the most common type of diabetes, accounting for about 90% of the total number of diabetic patients in the world. T2DM is a metabolic disease characterized by insulin resistance and chronic low-level inflammation, which can lead to multiple complications as the disease progresses, including ...

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 Applications(China)
IPC IPC(8): A61K45/00A61K31/352A61K31/36A61P3/10A61P25/00A61P1/18A61P1/16A61P13/12
CPCA61K45/00A61K31/352A61K31/36A61P3/10A61P25/00A61P1/18A61P1/16A61P13/12
Inventor 陈莉娜尚佳王转转刘娜颜文慧崔鑫马维娜郭婷莉卫晓彤贺浪冲
Owner XI AN JIAOTONG 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