Application of 5,6,7,4'-tetrahydroxy flavone and derivatives thereof in preparation of drugs for preventing and treating hyperuricemia and gout

A technology for hyperuricemia and gout, applied in the field of medicine, can solve the problems of low activity of hyperuricemia and lower blood uric acid level

Active Publication Date: 2012-02-01
KPC PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, flavonoids have attracted much attention as a class of natural products. Quercetin, morin, myricetin, kaempferol, baicalein, puerarin, luteolin, daidzein, etc. have been found to have xanthine oxidase inhibitory activity , and quercetin, morin, myricetin, kaempferol, puerarin 50, 100mg / kg intragastric administration significantly reduced the blood uric acid level of mice with hyperuricemia caused by potassium oxonate, however, with yellow The purine oxidase inhibitor allopurinol is less active in reducing hyperuricemia in vivo

Method used

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  • Application of 5,6,7,4'-tetrahydroxy flavone and derivatives thereof in preparation of drugs for preventing and treating hyperuricemia and gout
  • Application of 5,6,7,4'-tetrahydroxy flavone and derivatives thereof in preparation of drugs for preventing and treating hyperuricemia and gout
  • Application of 5,6,7,4'-tetrahydroxy flavone and derivatives thereof in preparation of drugs for preventing and treating hyperuricemia and gout

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1 : Effects of 5,6,7,4'-tetrahydroxyflavone and its derivatives on hyperuricemia mice

[0039] Healthy male Kunming mice, weighing 18-22 g, were provided by the Experimental Animal Center of Kunming Medical College (Experimental Animal Production License Number: SCXK (Dian) 2005-0008). Breeding conditions: room temperature is 22±2°C, relative humidity is 45-55%.

[0040]

[0041] In formula Ⅰ, R 1 -H, -CH 3 、-COCH 3 or glucuronic acid; R 2 -H, -CH 3 or -COCH 3 .

[0042] Among them, when R 1 = Gluconic acid, R 2 =H, the corresponding compound is scutellarin, the number is DZHS-001;

[0043] When R 1 =R 2 =H, the corresponding compound is 5,6,7,4'-tetrahydroxyflavone, the number is DZHS-002;

[0044] When R 1 =R 2 =-CH 3 , the corresponding compound is 5,6,7,4'-tetramethoxyflavone, number DZHS-004;

[0045] When R 1 =R 2 =-COCH 3 , the corresponding compound is 4',5,6,7-tetraacetoxyflavone, number DZHS-006;

[0046]When R 1 = H, R 2 =-CO...

Embodiment 2

[0056] Example 2 : Study on the dose-effect relationship of 5,6,7,4'-tetrahydroxyflavone and its derivatives in reducing hyperuricemia

[0057] In order to evaluate the dose-effect relationship of 5,6,7,4'-tetrahydroxyflavone and its derivatives in reducing hyperuricemia, 5,6,7,4'-tetrahydroxyflavone (DZHS-002) and Dengzhan Anthocyanin (DZHS-001) conducts dose-effect relationship research, the specific method is as follows:

[0058] 110 healthy male Kunming mice, weighing 18-22 g, were provided by the Experimental Animal Center of Kunming Medical College (the experimental animal production license number: SCXK (Dian) 2005-2008). Animals were randomly divided into normal control group, hyperuricemia model group, 5,6,7,4'-tetrahydroxyflavone 2.5, 5, and 10 dose groups, scutellarin 2.5, 5, and 10 dose groups, and allopurinol 2.38mg / kg 3.13mg / kg Positive control group, 10 rats in each group. The test compound was formulated into a suspension with 0.5% sodium carboxymethylcellu...

Embodiment 3

[0065] Example 3 : Effect of 5,6,7,4'-tetrahydroxyflavone and its derivatives on xanthine oxidase in vitro

[0066] In order to evaluate the effect of 5,6,7,4'-tetrahydroxyflavone and its derivatives on xanthine oxidase, 5,6,7,4'-tetrahydroxyflavone (DZHS-002) and breviscapine B Xanthine oxidase (DZHS-001) was studied in vitro, the specific method is as follows:

[0067] Xanthine oxidase (EC 1.1.3.22) is a product of Sigma Company, prepared with PBS to an appropriate concentration for use. 5,6,7,4'-Tetrahydroxyflavone and its derivatives were prepared into a series of concentrations with PBS for future use, and DMSO was used to aid in dissolution. Xanthine oxidase assay kit is a product of Nanjing Jiancheng Bioengineering Institute.

[0068] After incubating 5, 6, 7, 4'-tetrahydroxyflavone and its derivative solutions with serial concentrations and xanthine oxidase at 37°C for 30 minutes, the activity of xanthine oxidase was measured with a xanthine oxidase assay kit, and ...

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Abstract

The invention relates to the field of medicines, and particularly discloses application of 5,6,7,4'-tetrahydroxy flavone and derivatives thereof in preparation of drugs for preventing and treating hyperuricemia and gout. The invention also provides capsules and sustained-release tablets for preventing and treating hyperuricemia and gout. The invention discovers that 5,6,7,4'-tetrahydroxy flavone and derivatives thereof have strong anti-gout action, can significantly reduce the serum uric acid level of mouse suffering from hyperuricemia at low dosage, have activity equivalent to that of allopurinol, have low toxic and side effects, have safety higher than that of anti-gout drugs such as colchicine, allopurinol and anturan used clinically at present, can be used for preparing drugs for preventing and treating hyperuricemia and gout, and have broad clinical application prospects.

Description

technical field [0001] The invention relates to the field of medicine, in particular to the use of 5,6,7,4'-tetrahydroxyflavone and derivatives thereof in the preparation of medicines. Background technique [0002] Gout is a group of metabolic diseases caused by excessive production of uric acid and / or decreased excretion of uric acid due to purine metabolic disorders, and accumulation of uric acid in the body. Uric acid is a product of purine metabolism in humans, and hyperuricemia is the main biochemical basis of gout. At present, there are very limited drugs for the treatment of gout and hyperuricemia, mainly allopurinol, benzbromarone and colchicine, etc. These drugs have large side effects and are often not tolerated by patients, which limits their use to a certain extent. Therefore, finding new anti-gout and hyperuricemia drugs with high efficiency and low toxicity is still a hot spot in current pharmaceutical research. [0003] Xanthine oxidase is a key enzyme in th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61K31/7048A61P19/06A61K9/48A61K9/66A61K9/22
Inventor 张伟普俊学刘一丹刘国光杨兆祥杨旭娟
Owner KPC PHARM INC
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