Application of benserazide as alpha-glucosidase inhibitor

A kind of technology of glucosidase and benserazide, which is applied in the field of medicine

Pending Publication Date: 2020-09-04
SHENYANG PHARMA UNIVERSITY
View PDF1 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, discovering new indications for old drugs is challenging

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 benserazide as alpha-glucosidase inhibitor
  • Application of benserazide as alpha-glucosidase inhibitor
  • Application of benserazide as alpha-glucosidase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0053] In order to make the technical problems to be solved by the present invention, technical solutions and advantages clearer, the following will describe in detail with reference to the drawings and specific embodiments. The embodiment of the present invention provides a method of structure-based virtual screening combined with in vitro experimental verification to discover the application of benserazide as an α-glucosidase inhibitor.

[0054] (1) Molecular dynamics simulation of 3TOP-acarbose and 6C9X-voglibose

[0055] The molecular dynamics simulation of the α-glucosidase co-crystal (PDB code: 3TOP, 6C9X) complex was used to evaluate the stability of the complex under physiological conditions, and to determine the activity of the protein and acarbose and voglibose. Important amino acid residues acting at the site. like figure 1 and figure 2 As shown, by calculating the RMSD and RMSF of the protein backbone, the conformational structure changes and internal flexibil...

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 technical field of medicine. The invention in particular relates to the applicatoin of benserazide (The International Nonproprietary Names for Pharmaceutical Substances (INN) is Benserazide) as an alpha-glucosidase inhibitor, and a structure-based computational simulation screening method. Benserazide can be stably combined with an active site of alpha-glucosidase to inhibit the activity of alpha-glucosidase, so that the effect of reducing blood sugar is achieved. According to the invention, based on a thought of new use of old drugs, FDA-approved drugs are subjected to pharmacophore-based virtual screening, molecular docking and molecular dynamics simulation processes, and it is found that benserazide can be stably combined at an active site of alpha-glucosidase, and in-vitro experiments show that benserazide is an alpha-glucosidase inhibitor, so that the new application of the benserazide in reducing blood sugar is excavated. The invention not only provides a new angle for benserazide as a hypoglycemic drug, but also provides an example for rapid development of a novel alpha-glucosidase inhibitor.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to the application of benserazide [International Nonproprietary Names for Pharmaceutical Substances, INN] as an α-glucosidase inhibitor, and a structure-based calculation simulation method of screening. Background technique [0002] 1 Diabetes mellitus is a chronic metabolic syndrome in which patients exhibit hyperglycemia. The World Health Organization (WHO) predicts that by 2030, approximately 439 million people worldwide will suffer from diabetes. Diabetes has a very serious negative impact on global economic development, so it is urgent to find a suitable drug to treat this disease. α-Glucosidase is expressed on the cell membrane surface of the small intestine, and it can hydrolyze oligosaccharides and disaccharides into monosaccharides, resulting in increased blood glucose levels after meals. Therefore, α-glucosidase is a very important target for the treatment ...

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): G16C20/30G16C10/00
CPCG16C20/30G16C10/00
Inventor 于治国王健武娇凤赵云丽胡百淳
Owner SHENYANG PHARMA UNIVERSITY
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