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Application of Caraphenol A in preparation of xanthine oxidase inhibition drugs

A xanthine oxidase and drug technology, applied in the directions of drug delivery, drug combination, pharmaceutical formulation, etc., can solve the problems of allergies, liver and kidney damage, bone marrow suppression, limited clinical use, etc., and achieve widened drug routes and good compatibility. Effect

Pending Publication Date: 2021-08-27
GUIZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The uric acid-lowering drug allopurinol has been used as a first-line anti-gout drug since it was used clinically in 1963. However, due to adverse reactions such as allergies, liver and kidney damage, and bone marrow suppression, the total incidence of side effects is 5-20%. Its clinical use is greatly limited; in 2009, the XO selective inhibitor febuxostat was approved for marketing by the US FDA. Adverse reactions such as liver damage and muscle pain

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  • Application of Caraphenol A in preparation of xanthine oxidase inhibition drugs
  • Application of Caraphenol A in preparation of xanthine oxidase inhibition drugs
  • Application of Caraphenol A in preparation of xanthine oxidase inhibition drugs

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Experimental program
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Effect test

Embodiment 1

[0022] The application of Caraphenol A 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;

[0023] The xanthine oxidase inhibitory drug is made of Caraphenol A as an active ingredient and other pharmaceutical excipients or carriers;

[0024] The Caraphenol A is a diphenylethylene trimer, and its molecular formula is C 42 h 28 o 9 , the chemical name is (2S,2aS,7R,7aR)-2,7,12-Tris(4-hydroxyphenyl)-2,2a,7,7a-tetrahydrobis[1]benzofuro[3',4':4,5 ,6; 3",4":7,8,9]cyclonona[1,2,3-cd][1]benzofuran-4,9,14-triol;

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

[0026]

[0027] The Caraphenol A is directly extracted from plant flower ro...

Embodiment 1X

[0029] Embodiment 1XO inhibitory activity test:

[0030] 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 sample aver...

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Abstract

The invention belongs to the technical field of application of active ingredients of traditional Chinese medicinal materials, and particularly relates to application of Caraphenol A in preparation of xanthine oxidase inhibition drugs. The Caraphenol A is a stilbene tripolymer, the molecular formula of the Caraphenol A is C42H28O9, and the Caraphenol A can be prepared into drug dosage forms suitable for clinical use, such as injections, granules, capsules, tablets, powder, dripping pills and sustained release preparations. The effect of remarkably inhibiting the activity of xanthine oxidase is achieved.

Description

technical field [0001] The invention belongs to the technical field of application of active ingredients of Chinese medicinal materials, and in particular relates to the application of Caraphenol A in the preparation of xanthine oxidase (Xanthine Oxidase, XO for short) inhibitory medicine. Background technique [0002] Gout is an inflammatory arthritis caused by the deposition of urate crystals in joints caused by persistent hyperuricemia. Usually hyperuricemia is considered a sign of gout, and according to statistics, about 5%-12% of hyperuricemia will eventually develop into gout. When the blood uric acid level exceeds its saturation in the blood or tissue, crystals will form in joints and other parts, local inflammation and tissue destruction; hyperuricemia is typically characterized by an increase in the level of uric acid in the body, control the level of uric acid The elevation of is an important way to treat hyperuricemia and gout. Usually, the goal of clinical trea...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/343A61P19/06A61P3/10A61P13/12A61P9/00
CPCA61K31/343A61K9/0053A61K9/0019A61P19/06A61P3/10A61P13/12A61P9/00
Inventor 廖尚高何迅徐国波王栋朱勤凤廖兴江关焕玉董莉董永喜周孟罗喜荣邹淑涵王磊张金娟陈腾祥杨雅欣
Owner GUIZHOU MEDICAL UNIV