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Application of steroid saponin terpenoids and derivatives thereof in preparing medicine for treating purine metabolic disturbance diseases

A technology for steroidal saponins and abnormal metabolism, which can be used in steroids, bone diseases, drug combinations, etc., and can solve problems such as steroidal saponins that have not yet been found.

Inactive Publication Date: 2009-09-16
成都军区昆明总医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, steroidal saponins have not been found to inhibit xanthine oxidase or treat purine metabolism disorders.

Method used

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  • Application of steroid saponin terpenoids and derivatives thereof in preparing medicine for treating purine metabolic disturbance diseases
  • Application of steroid saponin terpenoids and derivatives thereof in preparing medicine for treating purine metabolic disturbance diseases
  • Application of steroid saponin terpenoids and derivatives thereof in preparing medicine for treating purine metabolic disturbance diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] The preparation method of salicin:

[0027] Taking the whole plant of Salix poplar grown in southern China as the raw material, the whole plant is dried in the shade and crushed, sieved, divided into coarse and fine powders, and loaded according to the fine powder, percolated with 10 times the amount of 30% ethanol, and the flow rate is controlled to 300ml / min. The leachate was filtered, concentrated to p=1.1, filtered with a 200-mesh filter cloth, and spray-dried to collect powder. The dry powder was degreased with petroleum ether and then air-dried. N-butanol was used as the solvent, the extraction temperature was 70°C, and the solvent dosage was 16 times the liquid-solid ratio for 4 hours. The obtained n-butanol extract was passed through a silica gel column, eluted with petroleum ether-ethyl acetate as a gradient of 100:0→10:90 to collect specific fractions, and then treated with a macroporous adsorption resin and chromatographed on a silica gel column for multiple ...

Embodiment 2

[0029] Fluorescence method to evaluate the effect of saponin Riparsaponin on xanthine oxidase in vitro, see figure 2 .

[0030] In this example, a 96-well fluorescence detection plate was used, and a positive control group, allopurinol, a negative control group, DMSO, and a test sample group were set up, and the total reaction system was 150 ul. The sample group to be tested has six concentrations, five parallel wells for each concentration, so that the final concentration is 3ug / ml, 6ug / ml, 12ug / ml, 25ug / ml, 50ug / ml, 100ug / ml, 1ul / well; positive; The control is 6 concentrations of allopurinol, the final concentration is 0.3, 0.6, 1.2, 2.4, 4.8, 9.6ug / ml, 1ul / well; the negative control DMSO, 1ul / well; use a fluorescence chemiluminescence detector at the excitation wave Measure the fluorescence value of each well at the emission wave of 380nm / 440nm, obtain the mean value, and calculate the inhibition rate and IC 50 value.

[0031] It can be seen from Table 2 that the saponi...

Embodiment 3

[0037] The effect of Riparsaponin on hypoxanthine-guanine phosphoribosyltransferase (HGPRT) was evaluated.

[0038] The ratio of HGPRT and β-actin PCR products was used to represent the HGPRT mRNA level. Compared with the control group, the HGPRT mRNA expression in the test sample group increased with the increase of the drug concentration, wherein the drug concentration was 12 μg / ml, 25 μg / ml. ml, the group rank of 50μg / ml was significantly different from the blank group (p image 3 .

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Abstract

The invention relates to an application of steroid saponin terpenoids and derivatives thereof in preparing medicine for treating purine metabolic disturbance diseases; the steroid saponin terpenoids and derivatives thereof have the above structural general formula and the application thereof in preparing medicine for lowering level of blood uric acid and treating purine metabolic disturbance diseases has the effect of inhibiting xanthine oxidase, facilitating excretion of ethacrynic acid and resisting inflammation; the steroid saponin terpenoids and derivatives thereof can be prepared into multiple preparation formulations which are applicable to diseases related to uric acid increase, can treat or prevent gout, purine metabolic disturbance diseases and complicating diseases thereof such as uric acid stone, mixed calcium / uric acid stone, hyperuricemic nephropathy, urate nephropathy, acute and chronic gouty arthritis and the like.

Description

Technical field: [0001] The invention relates to medicinal compounds in the technical field of medicine, in particular to the use of salicylic saponin, a newly discovered steroidal saponin compound in Salix salivarius, for preparing medicines for lowering blood uric acid and treating diseases with abnormal purine metabolism. Background technique: [0002] Salix Homonoia riparia Lour. is a plant of the Euphorbiaceae family, and its roots are used to treat swelling and pain. A new steroidal saponin Riparsaponin has been isolated and identified from the whole plant. 's report. [0003] Disorders of abnormal purine metabolism can be defined as plasma or serum urate concentrations greater than 420umol / L or 7.0mg / dL. The cause can be a congenital factor or the result of an acquired disease, classified as primary or secondary. Another classification is based on the source of disorders of abnormal purine metabolism: increased urate production, decreased uric acid excretion, and mi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J53/00A61K31/704A61P43/00A61P19/06A61P13/12
Inventor 赵晶赵雪倩
Owner 成都军区昆明总医院
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