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Application of stilbene derivatives and pharmaceutically acceptable salts thereof in the preparation of medicines for treating hyperuricemia

A technology of stilbene derivatives and hyperuricemia, which is applied in food science, drug combination, medical preparations containing active ingredients, etc., can solve the problems of high toxicity and side effects, and achieve the effect of no toxicity and side effects and good safety

Active Publication Date: 2017-06-06
NANJING BAOHE BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But above-mentioned medicine toxic and side effects are big, for example allopurinol can cause severe toxic and side effects such as allergic reaction (incidence rate 10-15%), hypersensitivity syndrome (27.5% maculopapular patient's death), myelosuppression; Probenecid, phenyl bromide Malone has side effects such as gastrointestinal reactions, renal colic, and acute attacks of gout, which limits the clinical application of these drugs to a certain extent

Method used

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  • Application of stilbene derivatives and pharmaceutically acceptable salts thereof in the preparation of medicines for treating hyperuricemia
  • Application of stilbene derivatives and pharmaceutically acceptable salts thereof in the preparation of medicines for treating hyperuricemia
  • Application of stilbene derivatives and pharmaceutically acceptable salts thereof in the preparation of medicines for treating hyperuricemia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Example 1: Effects of compounds on xanthine oxidase in vitro

[0058] In order to evaluate the impact of the test compound on xanthine oxidase, this experiment studies the impact on xanthine oxidase in vitro, and the specific methods are as follows:

[0059] Add 200 μL of xanthine substrate solution (final concentration: 400 μM), 100 μL of different concentrations of test product solution (negative control XOD group plus PB, positive control group plus allopurinol) and xanthine oxidase solution in a 2 mL centrifuge tube. 200 μL (final concentration: 0.08 U / mL), vortexed for 5 s, then placed in a 25°C water bath for 5 min, after the reaction was completed, 1.5 mL of absolute ethanol was added and vortexed for 5 s to terminate the reaction. After the reaction was terminated, the sample was centrifuged at 3500rpm for 5min, 200μl was drawn into a 1.5ml centrifuge tube, and the UA value was detected with a biochemical analyzer (BECKMAN COULTER AU480) in sequence according to...

Embodiment 2

[0064] Example 2: Effects of Compounds on Serum Uric Acid Levels in Hyperuricemia Mice

[0065] The present invention verifies the effect of the compound on hyperuricemia mice through animal experiments

[0066] experimental method:

[0067] Take 100 Shanghai Lingchang male KM mice with a body weight of 15-18g, divide them into cages at a rate of 5 per cage, and then adaptively feed them in the company's barrier system for 4 days. Random grouping was carried out on the fourth day of the adaptation period, and 90 mice with concentrated weight were selected from 100 mice and randomly divided into 9 groups according to body weight, with 10 animals in each group, which were blank control group and hyperuricemia model group respectively. , a positive control group, and a test compound group (5 groups in total, namely compound 1, compound 2, compound 3, compound 4, and compound 5).

[0068] Immediately after the adaptation period, intragastric administration was started, once a da...

Embodiment 3

[0077] Example 3: Study on the dose-effect relationship of compounds reducing serum uric acid levels in mice with hyperuricemia

[0078] In order to evaluate the dose-effect relationship of the test compound in reducing serum uric acid levels in mice with hyperuricemia, three compounds, Compound 1, Compound 2, and Compound 4, were selected for dose-effect relationship evaluation in this experiment. The specific methods are as follows:

[0079] experimental method:

[0080] Take 140 Shanghai Lingchang male KM mice weighing 13-15g, divide them into cages at a rate of 5 per cage, and then adaptively feed them in the company's barrier system for 4 days. On the 4th day of the adaptation period, random grouping was carried out, and 120 mice with concentrated weight were selected from 140 mice and randomly divided into 12 groups according to body weight, with 10 animals in each group, which were blank control group and hyperuricemia model group respectively. , positive control group...

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Abstract

The invention relates to application of a stilbene derivative and pharmaceutically acceptable salts thereof to preparation of medicines or health-care products for preventing and / or treating hyperuricemia, and acute gout, chronic gout, gouty arthritis, gout attack, uric acid nephrolithiasis and gouty nephropathy caused by the hyperuricemia. The stilbene derivative is used as an active component for preparing the medicines for treating the hyperuricemia, can reduce the concentration of uric acid in blood, has a significant effect on treatment of the hyperuricemia, does not have toxic or side effects and has good safety.

Description

technical field [0001] The invention relates to a new medicine application of stilbene derivatives. Background technique [0002] In recent years, with the improvement of people's living standards and changes in dietary structure, the intake of sugar, fat, and protein has increased significantly, and the incidence of hyperuricemia and gout has increased day by day, which has become a common disease. [0003] It is generally believed that when the blood uric acid is 465 μmol / L, it is hyperuricemia, and about 5%-12% of patients with hyperuricemia will develop gout. The clinical features are: recurrent gouty acute arthritis, tophi deposition, characteristic chronic arthritis and joint deformities, often involving the kidneys to cause chronic interstitial nephritis and renal uric acid stone formation. The acute attack of gout is an acute inflammatory reaction caused by the deposition of monosodium urate crystal (MSU) in the form of crystals in joints and periarticular tissues. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/09A61K31/7034A61K31/085A61K31/357A61K31/352A61P19/06A61P19/02A61P13/12A23L33/105A23L33/00
CPCA61K31/085A61K31/09A61K31/352A61K31/357A61K31/7034A61K2300/00
Inventor 温尧林张小芸
Owner NANJING BAOHE BIOTECH
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