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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
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

However, discovering new indications for old drugs is challenging

Method used

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

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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...

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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

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Application Information

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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
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