Medicine with dicaffeoylquinic acid from Artemisia selengensis for treating gout

a technology of dicaffeoylquinic acid and gout, which is applied in the field of botanical medicine, can solve the problems of gouty arthritis, uric acid level increase, and series of inflammatory reactions, and achieves the effects of simple operation, improved treatment effect and low cos

Pending Publication Date: 2021-08-05
HUAZHONG AGRI UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The dicaffeoylquinic acid compounds, particularly 1,4-dicaffeoylquinic acid, show superior xanthine oxidase inhibition and anti-inflammatory effects, offering a safer and more effective treatment for hyperuricemia and gout with fewer side effects compared to conventional medications.

Problems solved by technology

The increase of XOD activity will cause an increase in uric acid level, leading to hyperuricemia.
When too much uric acid in the body is deposited in the form of crystals in the synovial membrane and interstitial fluid of the joint, it will cause a series of inflammatory reactions and cause gouty arthritis.

Method used

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  • Medicine with dicaffeoylquinic acid from Artemisia selengensis for treating gout

Examples

Experimental program
Comparison scheme
Effect test

embodiment 1

[0016] Extraction and Identification of Dicaffeoylquinic Acid

[0017]Artemisia selengensis leaves were dried in an oven at 60° C. for 20 h, and pulverized through a 60-mesh sieve to obtain powder of the Artemisia selengensis leaves.

[0018]The powder of the Artemisia selengensis leaves was extracted with 50% (by volume) ethanol, and a ratio of material to liquid was 1:15. The mixture was stirred for 1 hour at room temperature, extracted twice and filtered wherein the filtrate was combined. After removing ethanol by rotary evaporation, a concrete of the Artemisia selengensis leaves was obtained.

[0019]The concrete was extracted with petroleum ether and ethyl acetate in sequence to obtain an extract of the Artemisia selengensis leaves. The ethyl acetate extract layer was rotary evaporated to remove ethyl acetate, and lyophilized to obtain powder of the ethyl acetate fraction of the Artemisia selengensis leaves.

[0020]The ethyl acetate fraction of the above-mentioned Artemisia selengensis le...

embodiment 2

[0023] Inhibition of XOD Enzyme Activity by Dicaffeoylquinic Acid

[0024]Twenty μL of the above identified five monomeric compound solutions from the Artemisia selengensis leaves and positive control (allopurinol) were pipetted into enzyme labels before adding 100 μL of XOD enzyme solution (0.02 U / mL), and vibrating in a 37° C. microplate reader for 10 s to incubate for 2 min. Forty μL of xanthine solution (1 mmol / L) was added with a spray gun to measure absorbance every 20 s for 15 times. Change of absorbance in the reaction system at 295 nm within 5 min was K1, and the change in PBS control was K0.

The inhibition rate(%)of the samples on XOD enzyme activity=(1 −K1 / K0)×100%.

[0025]As can be seen from Table 2, among the five compounds, 1,4-diCQA has the lowest IC50 value and is lower than that of the allopurinol (positive drug). This indicates that 1,4-diCQA in the Artemisia selengensis leaves has a good ability to inhibit XOD enzyme activity, and it can be applied to product developmen...

embodiment 3

[0026] Effect of Dicaffeoylquinic Acid on Relieving Gout Inflammation

[0027]THP-1 suspension cells were inoculated into a 24-well plate. When the density reached 80%, a phorbol ester (PMA) solution with a final concentration of 100 ng / mL was added. After 12 hours of PMA treatment, THP-1 cells differentiated into adherent macrophages. Culture medium was aspirated before washing the cells with PBS, completely replacing the culture medium to culture for 12 h before carrying out a dosing treatment. One hundred μmol / L of the above identified monomer compounds were pre-incubated for 12 h, then lipopolysaccharide with a final concentration of 1 μg / mL was added and acted for 2 h, and finally a sodium urate solution with a final concentration of 200 μg / mL was added and acted for 4 h. The control group did not add drugs, and did not stimulate the cells with lipopolysaccharide and sodium urate. The model group was pre-incubated without drugs, and cells were stimulated with lipopolysaccharide an...

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Abstract

1,4-dicaffeoylquinic acid is used as a xanthine oxidase inhibitor and in preparation of a medicament for treating gout. The present invention is the first to isolate and identify five dicaffeoylquinic acid compounds from Artemisia selengensis leaves. The compound not only has an ability of inhibiting xanthine oxidase activity, but also has the function of anti-gout inflammation, which can be better used for treating gout. The dicaffeoylquinic acid is derived from natural plants and has the advantages of being safe and non-toxic, and having fewer side effects.

Description

CROSS REFERENCE OF RELATED APPLICATION[0001]This is a continuation application of U.S. patent application Ser. No. 16 / 566,886, filed on Sep. 11, 2019; and claims the priority of Chinese Patent Application CN 201910496409.X, filed to the China National Intellectual Property Administration (CNIPA) on Jun. 10, 2019, the entire content of which are incorporated hereby by reference.BACKGROUND OF THE PRESENT INVENTIONField of Invention[0002]The present invention relates to a pharmaceutical use of dicaffeoylquinic acid, and more particularly to a medicine for treating hyperuricemia and gout, and belongs to a field of botanical medicine.Description of Related Arts[0003]Gout is a disease in which uric acid is deposited in tissues due to an increase in blood uric acid or a decrease in renal excretion of uric acid caused by a disorder of sputum metabolism. Hyperuricemia is the biochemical basis of gout, and gout has become a common disease that threatens human health such as hypertension, diab...

Claims

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Application Information

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Patent Type & AuthorityApplications(United States)
IPC IPC(8): A61K31/216
CPCA61K31/216A61K2236/333A61P19/06C07C67/48C07C2601/14
InventorXU, XIAOYUNCAO, WEIWEIWU, TINGPAN, SIYI
OwnerHUAZHONG AGRI UNIV