Application of cassia ketoside in preparation of xanthine oxidase inhibitor

A technology of xanthine oxidase and cassia ketone glycosides is applied in the application field of cassia ketone glycosides in the preparation of xanthine oxidase inhibitors, and can solve the problem that no ketoside glycosides inhibit the activity of xanthine oxidase and resist hyperuric acid Research reports on blood effects, etc., to achieve the effect of clear mechanism of action and less toxic and side effects

Inactive Publication Date: 2015-06-24
QINGDAO UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] However, there is no research report on the inhibitory effect of cassia keton

Method used

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  • Application of cassia ketoside in preparation of xanthine oxidase inhibitor
  • Application of cassia ketoside in preparation of xanthine oxidase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] The half inhibitory concentration IC 50 determination

[0020] HPLC determination method: Diamonsil ODS chromatographic column (250 mm × 4.6 mm, 5 mu m); mobile phase: 100 mmol / L sodium dihydrogen phosphate solution (pH=3.5); detection wavelength: 290 nm; flow rate: 1.0 mL / min.

[0021] Determination system: different concentrations of test product solutions (0.07 mol / L phosphate buffer containing 0.25% DMSO) 200 mu L added 0.07 mol / L phosphate buffer 140 mu L, xanthine oxidase solution 120 mu L (0.02 unit / mL, 0.07 mol / L phosphate buffer), keep warm at 25°C for 15 min, add xanthine solution 240 mu L (300 mu mol / L, 0.07 mol / L phosphate buffer), incubate at 25°C for 15 min, add 1 mol / L hydrochloric acid 100 mu L terminates the reaction. For blank control determination, the test solution was replaced with 0.07 mol / L phosphate buffer containing 1% DMSO. The amount of uric acid produced was determined by HPLC, and the concentration of each group was paralleled...

Embodiment 2

[0023] Determination of the inhibitory effect of cassiazone glycosides on xanthine oxidase

[0024] HPLC determination method: Diamonsil ODS chromatographic column (250 mm × 4.6 mm, 5 mu m); mobile phase: 100 mmol / L sodium dihydrogen phosphate solution (pH=3.5); detection wavelength: 290 nm; flow rate: 1.0 mL / min.

[0025] Determination system: different concentrations of test product solutions (0.07 mol / L phosphate buffer containing 0.25% DMSO) 200 mu L, add 0.07 mol / L phosphate buffer 140 mu L, add xanthine solution 240 mu L (100 mu mol / L, 50 mu mol / L, 37.5 mu mol / L, 25 mu mol / L, 0.07 mol / L phosphate buffer), xanthine oxidase solution 120 mu L (0.05 unit / mL, 0.07 mol / L phosphate buffer), keep warm at 25°C for 1 min, add 1 mol / L hydrochloric acid 100 mu L terminates the reaction. The amount of uric acid produced was determined by HPLC, and the concentration of each group was parallelized three times. The type of inhibition was determined by the Lineweaver-B...

Embodiment 3

[0027] Effects of cassiatone glycosides on serum uric acid levels in experimental hyperuricemia model mice

[0028] The mice were randomly divided into 6 groups, 20 in each group, which were normal control group (normal saline 10 mL / Kg), model control group (oxonate potassium 250 mg / Kg), high-dose cassiazone glycoside group (oxygen Potassium oxonate 250 mg / Kg+cassarone 40 mg / Kg), middle-dose group (potassium oxonate 250 mg / Kg+cassarone 20 mg / Kg), low-dose group (Potassium oxonate 250 mg / Kg+cassine glycoside 10 mg / Kg), allopurinol control group (potassium oxonate 250 mg / Kg+allopurine 5 mg / Kg). Every day at 9:00 AM, the model control group and each administration group were administered intragastrically with oxonate potassium, and 1 hour later, each administration group was administered by intragastric administration, and the administration cycle was 7 days. The normal control group and the model control group were administered intragastrically equal volume of saline. After 1 ...

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Abstract

The invention provides an application of cassia ketoside in preparation of a xanthine oxidase inhibitor. In vitro tests prove that cassia ketoside has an obvious inhibitory effect on the activity of xanthine oxidase; a test by an experimental hyperuricemia mouse model proves that the cassia ketoside greatly reduces the level of serum uric acid in the model mouse; therefore, the cassia ketoside can be used for preparing the xanthine oxidase inhibitor and used for preparing products for inhibiting the activity of the xanthine oxidase to treat hyperuricemia.

Description

technical field [0001] The invention belongs to the field of medicine and relates to the application of cassiazone glycosides in the preparation of xanthine oxidase inhibitors. Background technique [0002] Hyperuricemia is a group of heterogeneous diseases caused by purine metabolic disorders or (and) decreased uric acid excretion. It is an important biochemical basis for gout. It is a disease that seriously affects public health. Epidemiological surveys from China, the United States, the United Kingdom and other countries have shown that the incidence of hyperuricemia is rising rapidly, and it has been listed by the World Health Organization as one of the top ten chronic human diseases in the 20th century. Hyperuricemia not only seriously affects the patient's quality of life, but even threatens the life of the patient, seriously threatens the state of public health, and brings a heavy economic burden to the society. [0003] Xanthine oxidase, as the key enzyme of uric a...

Claims

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Application Information

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IPC IPC(8): A61K31/704A61P19/06
Inventor 王威刘坤韩立春刘小红高华
Owner QINGDAO UNIV
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