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Application of compound in preparation of medicines for treating acute gout

A technology for acute gout and a compound, which is applied to the application field of the compound in the preparation of a drug for treating acute gout, can solve the problems of granulocytopenia, aplastic anemia and the like, and achieves the effect of strong prevention and treatment activity and outstanding substantive characteristics.

Active Publication Date: 2013-11-27
SHANGHAI STEPPHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although they have fast anti-inflammatory and analgesic effects, their toxic and side effects are also quite obvious. For example, the effective dose of colchicine is similar to the dose that produces diarrhea and other gastrointestinal symptoms. Absolutely contraindicated in the case of bleeding, and the administration of phenylbutazone for as short as 3 weeks can also cause severe neutropenia or aplastic anemia

Method used

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  • Application of compound in preparation of medicines for treating acute gout
  • Application of compound in preparation of medicines for treating acute gout
  • Application of compound in preparation of medicines for treating acute gout

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Embodiment 1: the preparation of the compound Aphanamgrandiol A tablet involved in the present invention:

[0018] Take 5 grams of compound Aphanamgrandiol A, add 195 grams of dextrin, mix well, and make 1000 tablets by conventional compression.

Embodiment 2

[0019] Embodiment 2: the preparation of compound Aphanamgrandiol A capsules involved in the present invention:

[0020] Get 5 grams of compound Aphanamgrandiol A, add 195 grams of starch, mix well, pack into capsules and make 1000 capsules.

[0021] The following pharmacodynamic experiments will further illustrate its drug activity.

experiment example 1

[0022] Experimental example 1: Aphanamgrandiol A anti-acute gout inflammation experiment:

[0023] 1: method

[0024] ① Solution preparation

[0025] Add 5g of uric acid and 1000ml of distilled water to boil, add 5% NaOH solution to adjust the pH to 7.4, stir, cool and crystallize to make sodium urate crystals (MSU). The prepared MSU 10 mg was autoclaved, added 10 ml of serum-free DMEM culture solution, and ground to form a 1 mg / ml DMEM solution. During the experiment, this solution was added with DMEM culture medium to form MSU solutions with different concentrations of DMEM.

[0026] Aphanamgrandiol A2.5mg, dissolved in dimethyl sulfoxide (DMSO), the final concentration of DMSO <0.02%, plus serum-free DMEM medium, prepared to a concentration of 2.5ug / ml, 25ug / ml, 250ug / ml.

[0027] Positive drug indomethacin 2.0mg, the method is the same as Aphanamgrandiol A, the preparation concentration is 20ug / ml.

[0028] ② In vitro culture of vascular endothelial cells

[0029] HUV...

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Abstract

The invention provides a novel use of Aphanamgrandiol A in medical science, and in particular relates to an application of Aphanamgrandiol A in preparation of medicines for treating acute gout. Experimental research results show that the Aphanamgrandiol A has the protective effect on an acute gout model of urate-caused injury of human vascular endothelial cells and inhibits expression of ICAM-1 (Intercellular Adhesion Molecule 1), so that the Aphanamgrandiol A can be used to prepare medicines for treating acute gouty inflammation. The application of the Aphanamgrandiol A in preparation of medicines for treating acute gout provided by the invention is disclosed for the first time. As the framework type of the Aphanamgrandiol A is a novel framework type, and the activity of the Aphanamgrandiol A to prevent and treat acute gout is unexpectedly strong, the probability of giving any indication by other compounds does not exist. The Aphanamgrandiol A has remarkable substantive characteristics and meanwhile has a remarkable progress for preventing and treating acute gout.

Description

technical field [0001] The present invention relates to a new application of compound Aphanamgrandiol A, in particular to the application of Aphanamgrandiol A in the preparation of medicines for treating acute gout. Background technique [0002] Gout, also known as gouty arthritis, is a disease caused by the disorder of purine metabolism in the body. It is manifested by excessive uric acid in the blood, and it is easy to cause urate (MSU) to crystallize in joints and other tissues. The acute attack of gout is due to the local neutrophil infiltration and inflammatory response caused by MSU deposited in the joints. [0003] Western medicine selects three kinds of medicines for use in the acute attack stage of gout: colchicine, non-steroidal anti-inflammatory drugs and corticosteroids. The mechanism of action of colchicine is to bind to the tubulin of neutrophils, thereby hindering the activity of granulocytes and inhibiting granulocyte infiltration. Non-steroidal anti-inflam...

Claims

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Application Information

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IPC IPC(8): A61K31/366A61P19/06
Inventor 张延
Owner SHANGHAI STEPPHARM CO LTD
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