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Application of Viniferifuran in the Preparation of Xanthine Oxidase Inhibiting Drugs

A xanthine oxidase and drug technology, applied in the directions of drug combinations, antipyretics, antibacterial drugs, etc., can solve the problems of drug production process that affects the regularity of drug use, unknown active ingredients, unsatisfactory inhibitory effect of a single component, etc. AIDS activity, good xanthine oxidase inhibitory activity, hepatoprotective effect

Active Publication Date: 2022-04-29
GUIZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] However, most of the schemes are combined use of multiple active ingredients, and the inhibitory effect of a single ingredient is still not ideal. The inventor has also found that gorse extract has a certain effect of inhibiting xanthine oxidase activity after many years of research, but for its main The active ingredients of the drug are unknown, which greatly affects the research on the law of medication and the process of drug production

Method used

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  • Application of Viniferifuran in the Preparation of Xanthine Oxidase Inhibiting Drugs
  • Application of Viniferifuran in the Preparation of Xanthine Oxidase Inhibiting Drugs
  • Application of Viniferifuran in the Preparation of Xanthine Oxidase Inhibiting Drugs

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Effect test

Embodiment 1

[0024] Application of Viniferifuran in the preparation of xanthine oxidase inhibitory drugs, the Viniferifuran is a stilbene dimer with a benzofuran structure, and its molecular formula is C 28 h 20 o 6 , the chemical name is 5-{6-Hydroxy-2-(4-hydroxyphenyl)-4-[(Z)-2-(4-hydroxyphenyl)vinyl]-1-benzofuran-3-yl}-1,3-benzonediol ;

[0025] The structural formula of the Viniferifuran is as follows:

[0026]

[0027] The Viniferifuran is extracted from natural medicines (such as gorse root) or synthesized by using stilbene as a monomer through oxidative coupling as a key reaction.

[0028] The inhibition of xanthine oxidase is manifested by inhibiting the activity of xanthine oxidase, reducing the generation of uric acid in the body, and preventing and treating diseases related to xanthine oxidase activity such as hyperuricemia, gout, diabetic nephropathy, and cardiovascular disease. .

[0029] The xanthine oxidase inhibitory drug is made of Viniferifuran as an active ingred...

experiment example 1

[0033] XO inhibitory activity test: at 25°C, using a 96-well plate, with a total reaction volume of 200 μL, first add 50 μL of enzyme solution (the final concentration of the reaction is 0.05 U / mL), 50 μL of sample solution, and incubate at 25°C for 15 minutes. Add 50 μL of xanthine substrate (final concentration 150 μmol / L) to start the reaction. After incubating at 25°C for 20 min, 50 μL of 1 mol / L hydrochloric acid solution was added to terminate the reaction. Absorbance values ​​were detected at 290 nm. Take the difference between this value and the OD value at the time of incubation for 0 min as the final detection result; detect the blank sample in the same way (that is, without the test drug, replace the sample solution with PBS containing 5% DMSO to determine the maximum reactivity of the enzyme) OD value, and the inhibition rate of each extract was calculated according to the following formula: inhibition rate (%)=(1-test sample average OD value / blank sample average ...

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Abstract

The invention belongs to the technical field of the application of active ingredients of Chinese medicinal materials, and specifically relates to the application of Viniferifuran in the preparation of xanthine oxidase inhibitory drugs. The Viniferifuran is a stilbene dimer with a benzofuran structure, and its molecular formula is C 28 h 20 o 6 , exhibits a strong inhibitory effect on xanthine oxidase, and can be used to prepare xanthine oxidase inhibitory drugs or preventive or therapeutic drugs for diseases related to xanthine oxidase.

Description

technical field [0001] The invention belongs to the technical field of the application of effective components of Chinese medicinal materials, and in particular relates to the application of Viniferifuran in the preparation of xanthine oxidase inhibitory drugs. Background technique [0002] In recent years, the incidence of gout and hyperuricemia has continued to increase. Hyperuricemia is a typical purine metabolic disease. When a large amount of uric acid is deposited in the soft tissues and joints of the body in the form of sodium salt, it will It can cause inflammation and lead to gout. Therefore, the important biochemical basis of gout is hyperuricemia. [0003] Uric acid is the end product of purine metabolism. Xanthine oxidase (Xanthine Oxidase, XO for short) can catalyze hypoxanthine to xanthine, which is further metabolized into uric acid and free radicals. target. At present, xanthine oxidase inhibitors are commonly used clinically as a class of uric acid-lowerin...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/343A61P19/06A61P3/10A61P13/12A61P9/00A61P31/04A61P29/00A61P31/12A61P39/06A61P31/18A61P1/16
CPCA61K31/343A61P19/06A61P3/10A61P13/12A61P9/00A61P31/04A61P29/00A61P31/12A61P39/06A61P31/18A61P1/16
Inventor 廖尚高徐国波何迅朱勤凤廖兴江关焕玉董莉董永喜周孟罗喜荣邹淑涵张金娟陈腾祥王栋杨雅欣
Owner GUIZHOU MEDICAL UNIV