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Application of 1,3,6,7-tetrahydroxy diphenylpyrrone derivative in preparing drug for preventing hyperuricemia and/or gout

A kind of technology of tetrahydroxybenzopyrone and its derivatives, applied in the field of medicine, can solve the problems affecting the quality of life, abnormality, diarrhea, headache, joint-related signs and symptoms and musculoskeletal/connective tissue symptoms, see gastrointestinal reactions, Rashes, fever and other adverse reactions

Active Publication Date: 2014-12-24
KPC PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although these drugs have a good curative effect on the treatment of gout, they all show certain toxic and side effects in clinical practice. Among them, the adverse reactions of febuxostat include abnormal liver function, diarrhea, headache, joint-related signs and symptoms and muscle pain. Bone / connective tissue symptoms; allopurinol common adverse reactions such as rash, diarrhea, abdominal pain, low fever, transient transaminase elevation or neutropenia; colchicine is highly toxic, common nausea, vomiting, diarrhea, abdominal pain, gastrointestinal reactions, Hematuria, oliguria, direct inhibitory effect on bone marrow, causing agranulocytosis, aplastic anemia, etc.; benzbromarone can cause neutropenia; probenecid common gastrointestinal reactions, rash, fever and other adverse reactions, long-term The use of these drugs brings great pain to patients, threatens health and affects quality of life

Method used

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  • Application of 1,3,6,7-tetrahydroxy diphenylpyrrone derivative in preparing drug for preventing hyperuricemia and/or gout
  • Application of 1,3,6,7-tetrahydroxy diphenylpyrrone derivative in preparing drug for preventing hyperuricemia and/or gout
  • Application of 1,3,6,7-tetrahydroxy diphenylpyrrone derivative in preparing drug for preventing hyperuricemia and/or gout

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] Example 1 The research on the uric acid excretion effect of 1,3,6,7-tetrahydroxybenzopyrrole derivatives shown in formula I

[0069] Select 21 male Wistar rats, weighing 340±20g, provided by the Experimental Animal Center of Kunming Medical University [Experimental animal production license number: SCXK (Dian) 2005-2008]. Breeding conditions: Room temperature is 22±2°C, relative humidity is 60% to 70%.

[0070] The isolated rat kidney perfusion model was prepared according to the method reported by Wang and Lepsy, and the perfusion fluid was K-H solution (mmol / L, NaCl118.0, KCl4.7, NaHCO 3 25,KH 2 PO 4 1.2, MgSO 4 2.34, CaCl 2 1.28, glucose5.55) as the basis, plus 65g / L bovine serum albumin component V and 0.153% compound amino acid injection (17AA, added before use). After preparation, filter with a membrane filter (0.45 μm pore size), and adjust the pH to 7.4. 1h before use and during the perfusion process, continue to fill with 95% O 2 +5%CO 2 mixed compositi...

Embodiment 2

[0083] Influence of 1,3,6,7-tetrahydroxybenzophenone derivatives shown in embodiment 2 formula I on xanthine oxidase

[0084] Xanthine oxidase (EC1.1.3.22) was prepared with PBS to an appropriate concentration for later use. Tetraacetoxybifen was prepared in PBS to a series of concentrations (1.2mmol / L, 0.12mmol / L, 0.012mmol / L) for later use.

[0085] After incubating the tetraacetoxydiphenhydrazine solution 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 to obtain a series of concentrations of tetraacetoxydiphenylpyrrolidone The inhibition rate of piroxin solution to xanthine oxidase is shown in Table 2.

[0086] The impact of table 2 tetraacetoxy benzophenone on xanthine oxidase ( n=9)

[0087]

[0088] It can be seen from Table 2 that the inhibitory rates of tetraacetoxybenzophenone at serial concentrations (1.2mmol / L, 0.12mmol / L, 0.012mmol / L) on xanthine oxidase a...

Embodiment 3

[0094] Example 3 Study on the Dose-Effect Relationship of 1,3,6,7-tetrahydroxybenzopyrrole Derivatives in Lowering Uric Acid Shown in Formula I

[0095] Select 60 healthy male Kunming mice, weighing 18-22 g, provided by the Experimental Animal Center of Kunming Medical University [Experimental animal production license number: SCXK (Dian) 2005-2008]. Breeding conditions: Room temperature is 22±2°C, relative humidity is 60% to 70%.

[0096] Animals were randomly divided into 6 groups, 10 in each group, respectively normal control group (0.5%CMC-Na10ml / kg), hyperuricemia model group (oxonate potassium 250mg / kg), tetraacetoxydiphenylpyrrole Ketone low-dose group (potassium oxonate 250mg / kg+tetraacetoxybifen 1.52mg / kg), medium-dose group tetraacetoxybifen (potassium oxonate 250mg / kg+tetraacetoxy phenpyrazone 3.11mg / kg), tetraacetoxy benzopyrone high-dose group (oxonate potassium 250mg / kg + tetraacetoxy benzopyrone 6.47mg / kg) and positive drug control group (oxonate potassium Pot...

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Abstract

The invention relates to the medicine field, and particularly relates to an application of 1,3,6,7-tetrahydroxy diphenylpyrrone derivative in preparing a drug for preventing hyperuricemia and / or gout. The invention provides the application of 1,3,6,7-tetrahydroxy diphenylpyrrone derivative shown as the formula I in preparing the drug for reducing a uric acid level. The application provided by the invention reduces the uric acid level through a dual effect of inhibiting activity of xanthine oxidase and promoting excretion of uric acid, has a relatively good curative effect for the hyperuricemia and / or gout, and provides a novel selection for clinically treating the hyperuricemia and / or gout. The formula I is shown in the description.

Description

technical field [0001] The invention relates to the field of medicine, in particular to the use of a 1,3,6,7-tetrahydroxybenzopyrazone derivative in the preparation of drugs for the prevention and treatment of hyperuricemia and / or gout. Background technique [0002] With the improvement of people's living standards and changes in eating habits, the incidence of hyperuricemia and gout in my country has been increasing year by year in recent years. Hyperuricemia is a disease in which blood uric acid exceeds the normal value due to purine metabolism disorder and / or uric acid excretion disorder, and it does not show any symptoms clinically. When the human body is in the condition of hyperuricemia for a long time, uric acid is precipitated in the joints, soft tissues, cartilage and kidneys in the form of sodium salt, causing human organ and tissue lesions, leading to gout, and causing serious complications, including gouty Arthritis, gouty nephropathy, gouty kidney stones, gouty...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61P19/06A23L1/30A23L33/10
Inventor 宋立明张翼张伟杨兆祥
Owner KPC PHARM INC
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