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Application of syringin in preparation of medicine for treating acute gout

A technology for acute gout and syringin is applied in the application field of syringin in the preparation of medicines for treating acute gout, and can solve the problems of granulocytopenia, aplastic anemia and the like

Inactive Publication Date: 2012-05-30
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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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 syringin in preparation of medicine for treating acute gout
  • Application of syringin in preparation of medicine for treating acute gout
  • Application of syringin in preparation of medicine for treating acute gout

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1 syringin preparation

[0040] Weigh 2 kg of Acanthopanax senticosus dry powder, reflux extraction with 70% ethanol for 3 times, the solid-liquid ratio is (1:8; 1:6; 1:5), 1h / time, the filtrates are combined, the ethanol is recovered, and the concentrated solution is added 8 times Amount of water was stirred to form a suspension, extracted three times with an equal amount of petroleum ether, and the aqueous layer was extracted four times with an equal volume of ethyl acetate. The ethyl acetate layers were combined, concentrated and dried under reduced pressure to obtain an extract. The extract was separated on a silica gel column and eluted sequentially with chloroform-methanol gradient with increasing polarity. When the ratio of chloroform-methanol was 100:4, crude crystals were eluted, and then recrystallized by methanol to obtain syringin crystals.

Embodiment 2

[0041] Example 2 Syringin protects HUVEC activity

[0042] 0.20 mg of syringin was dissolved in dimethyl sulfoxide (DMSO), the final concentration of DMSO was <0.02%, and serum-free DMEM culture solution was added to prepare a concentration of 20 μg / mL.

[0043] HUVEC were cultured in culture flasks, and when they grew to 70% to 80% confluence, they were digested with 0.25% trypsin, centrifuged, washed three times with 10% calf serum DMEM culture solution, and adjusted to 10% calf serum DMEM culture solution. 4×10 4 / mL cell suspension, implanted into a 96-well plate (200 μL per well), cultured for 24 hours, and gently sucked out the original culture solution, and performed the following experiments. Each group has 8 wells, and the specific grouping and liquid addition are as follows: control group (200 μL DMEM culture solution), model group (100 μg / mL MSU solution), syringin group (100 μg / mL MSU solution + 20 μg / ml syringin), add After liquid, continue to put 37 ℃, 5% CO 2...

Embodiment 3

[0044] Example 3 Syringin inhibits ICAM-1 expression

[0045] Digest the HUVEC in the logarithmic growth phase with 0.25% trypsin, gently pipette to make a cell suspension, and adjust the cell density to 5×10 9 / L, inoculated in cell culture flasks. After the cells were congested (about 24 hours), the supernatant was discarded and divided into the following groups: control group, model group (100 μg / mL MSU solution), syringin group (100 μg / mL MSU solution + 20 μg / mL syringin), and continue After culturing for 24 hours, the cells were collected with PBS, centrifuged to remove the supernatant, and CD54 monoclonal antibody was added. After 30 min, the cells were washed with PBS, and the cells were resuspended. The percentage of positive cells was detected by flow cytometry (n=10000).

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Abstract

The invention provides a new application of syringin in medical science, in particular to application of syringin in the preparation of a medicine for treating acute gout. Syringin is extracted and separated from acanthopanax roots and other plants, and the extraction method comprises the following steps of: refluxing and extracting dry acanthopanax root powder with ethanol, recovering the ethanol, adding water to the concentrated solution, stirring to obtain a mixed suspension, extracting with petroleum ether, extracting the water layer with acetic ether, merging the acetic ether layer, concentrating under reduced pressure to obtain an extract, separating by using a silica gel column, carrying out gradient elution by using chloroform and methanol in sequence to obtain a coarse crystal, and recrystallizing with methanol to obtain a syringin crystal. Experimental researches show that syringin can protect an acute gout model due to human vascuoar endothelial cell damages caused by urateand inhibit the expression of ICAM-1 (Intercellular Adhesion Molecule-1); thus, syringin can be used for preparing a medicine for treating acute gout.

Description

[0001] 1. Technical field: The present invention relates to the new application of Chinese medicine extract syringin in medicine, in particular to the application of syringin in the preparation of medicine for treating acute gout. 2. Background technology: [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. NSAIDs, ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/7034A61P19/06
Inventor 尹莲杨研华王明艳
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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