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Application of vitisinol D in the preparation of xanthine oxidase inhibitory drugs

A technology of xanthine oxidase and drugs, which is applied in the direction of drug combinations, active ingredients of heterocyclic compounds, and pharmaceutical formulations, can solve problems such as hindering hypoxanthine and xanthine metabolism, aggravating glucose metabolism disorders, and uric acid metabolism disorders. Good xanthine oxidase inhibitory activity, avoid stomach pain, clear pharmacological effect

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

AI Technical Summary

Problems solved by technology

The increase of xanthine oxidase activity will lead to the disorder of uric acid metabolism, and may aggravate the disorder of glucose metabolism at the same time
Xanthine oxidase inhibitory drugs inhibit the activity of xanthine oxidase, hinder the metabolism of hypoxanthine and xanthine into uric acid, thereby reducing the generation of uric acid in the body, and play a role in the treatment of gout. Among them, allopurinol has a significant effect on inhibiting the generation of uric acid , The mechanism of action is clear, and it is often used to reduce uric acid content, but it will cause side effects such as hypersensitivity syndrome, Stevens Johnson syndrome and nephrotoxicity
In 2009, the XO selective inhibitor febuxostat was approved for marketing by the US FDA. Its inhibition of XO activity was further improved, and its effect was better than that of allopurinol, but it still had adverse effects such as stomach pain, diarrhea, liver damage and muscle pain. reaction

Method used

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  • Application of vitisinol D in the preparation of xanthine oxidase inhibitory drugs
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  • Application of vitisinol D in the preparation of xanthine oxidase inhibitory drugs

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Experimental program
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Effect test

Embodiment 1

[0021] The application of Vitisinol D in the preparation of xanthine oxidase inhibitory drugs, the inhibition of xanthine oxidase is manifested by inhibiting the activity of xanthine oxidase, reducing the generation of uric acid in the body, and treating hyperuricemia, gout, diabetic nephropathy, heart disease, etc. Prevention and treatment of diseases related to xanthine oxidase activity, such as vascular diseases.

[0022] The molecular formula of the Vitisinol D is C 28 h 22 o 6 , the chemical name is (+)-(1R,5S,6S,7S)-6-(3,5-Dihydroxyphenyl)-7-(4-hydroxyphenyl)-4-[(1E)-2-(4-hydroxyphenyl) ethenyl]bicyclo[3.2.1]oct-3-ene-2,8-dione, its structural formula is:

[0023]

[0024] The xanthine oxidase inhibitory drug is made of Vitisinol D as an active ingredient and other pharmaceutical excipients or carriers;

[0025] The xanthine oxidase inhibitory drug is an oral agent or an injection; wherein, the oral agent is any one or more of granules, capsules, tablets, powders,...

experiment example 1XO

[0028] Experimental example 1XO inhibitory activity test:

[0029] 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 after incubating at 25 °C for 15 minutes, add 50 μL of xanthine base solution (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 s...

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Abstract

The invention belongs to the technical field of the application of active ingredients of Chinese medicinal materials, and in particular relates to the application of Vitisinol D in the preparation of xanthine oxidase inhibitory drugs. The xanthine oxidase inhibitory drugs are composed of Vitisinol D as an active ingredient and other pharmaceutical excipients or carrier, the molecular formula of the Vitisinol D is C 28 h 22 o 6 , Vitisinol D of the present invention is a monomer compound isolated from gorse root, which has high safety and strong xanthine oxidase inhibitory effect.

Description

technical field [0001] The invention belongs to the technical field of the application of active ingredients of Chinese medicinal materials, and in particular relates to the application of Vitisinol D in the preparation of xanthine oxidase inhibitory drugs. Background technique [0002] At present, the prevalence of gout is increasing year by year, and its incidence is second only to the incidence of diabetes, becoming the second largest metabolic disease. Gout is caused by the long-term increase of purine biological metabolism in the body, excessive production of uric acid or poor excretion of uric acid in the blood. Elevated uric acid crystals are deposited in joints and other places, resulting in a group of clinical syndromes. Sustained high blood uric acid levels are an essential condition for gout. Uric acid is the final product of the metabolism of purine substances in the body. Hyperuricemia is induced by the concentration of uric acid in the body exceeding the normal...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/34A61K36/48A61P19/06A61P3/10A61P13/12A61P9/00A61K125/00
CPCA61K31/34A61K36/48A61P19/06A61P3/10A61P13/12A61P9/00
Inventor 廖尚高廖兴江何迅徐国波朱勤凤关焕玉周孟董莉董永喜罗喜荣邹淑涵王磊张金娟陈腾祥王栋杨雅欣
Owner GUIZHOU MEDICAL UNIV
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