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New use of ellagic acid compounds in the preparation of drugs for the treatment of hyperuricemia

A technology for hyperuricemia and compounds, applied in the field of chemical medicine, can solve the problem of few types of ellagic acid derivatives, and achieve the effects of no toxic and side effects, lowering serum uric acid level and high safety

Active Publication Date: 2017-08-25
SUZHOU HEYAN BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are few reports on the research on ellagic acid derivatives. The literature reports that ellagic acid derivatives have certain xanthine oxidase inhibitory activity. The results show that ellagic acid and ellagic acid‐4‐O‐β‐D ‐Xylopyranosides inhibit xanthine oxidase IC 50 The values ​​are 9.3, 4.7μmol / L, respectively
However, the literature reports that there are few kinds of ellagic acid derivatives extracted, and only ellagic acid and ellagic acid xylopyranoside are isolated.

Method used

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  • New use of ellagic acid compounds in the preparation of drugs for the treatment of hyperuricemia
  • New use of ellagic acid compounds in the preparation of drugs for the treatment of hyperuricemia
  • New use of ellagic acid compounds in the preparation of drugs for the treatment of hyperuricemia

Examples

Experimental program
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Effect test

Embodiment 1

[0036] Example 1 The extraction and characterization of compound 2-5 of the present invention

[0037] Take 5kg of the Herba Myrobalan medicinal material, crush it, and reflux extract it with 50L of 95% ethanol for 3 times, each time for 3 hours, combine the extracts, concentrate under reduced pressure at 40°C, extract the extract with n-hexane, remove the lipids, and use Sephadex LH-20 was used for column chromatography, and 0%, 5%, 10%, 20%, 30%, 50%, and 100% ethanol were used for gradient elution and each eluted fraction was collected, and 5%, 10% , 20%, 30%, and 50% of the eluted components were concentrated under reduced pressure to remove the solvent, and then used reversed-phase C18 chromatographic columns for column chromatography, using 0%, 5%, 25%, 50%, 100% containing 2% Elute with methanol in acetic acid, collect the eluate, concentrate under reduced pressure to remove the solvent, and obtain four compounds 2-5, which are detected by HPLC-ESI-MS and NMR. The detec...

Embodiment 2

[0050] Example 2 Extraction and characterization of compounds 5 and 6 of the present invention

[0051] Take 2kg of Myrobalan medicinal material, grind it, and extract it with 20L of 95% ethanol for 3 times, each time for 3 hours, combine the extracts, concentrate under reduced pressure at 40°C, extract the extract with n-hexane, remove lipids, and use Sephadex LH ‐20 for column chromatography, respectively with 5%, 15%, 25%, 35%, 60%, 100% ethanol for gradient elution and collect each eluted fraction, 5%, 15% eluted fraction After concentrating under reduced pressure to remove the solvent, use reversed-phase C18 column chromatography to carry out purification respectively, use 5%, 15%, 25%, 50, 100% methanol containing 2% acetic acid to carry out elution, collect eluate, reduce Concentrated under pressure to remove the solvent, two compounds 5 and 6 can be obtained, detected by HPLC-ESI-MS and NMR, the detection and characterization data of compounds 5 and 6 are as follows: ...

Embodiment 3

[0059] Example 3 Extraction and Characterization of Compounds 7,8,9 of the present invention

[0060] Take 3 kg of Chinese tallow tree medicinal material, crush it, and reflux extract it with 30 L of 95% ethanol for 3 times, each time for 3 hours, combine the extracts, concentrate under reduced pressure at 40 ° C, and use petroleum ether, ethyl acetate and n-butanol for the extract respectively. After extraction, the ethyl acetate extraction part was concentrated under reduced pressure to remove the solvent, and then separated by silica gel column chromatography, using chloroform-methanol gradient elution (V 氯仿 :V 甲醇 =98:2—70:30), the obtained part was recrystallized and purified to obtain compounds 7, 8, and 9. Detected by HPLC-ESI-MS and NMR, the detection and characterization data of compounds 7, 8, and 9 are as follows:

[0061] Compound 7: 3,3’,4’‐trimethoxyellagic acid C 17 h 12 o 8 [M‐H ‐ ]:343.2

[0062] 1 H‐NMR (DMSO‐d 6 ,300MHz)δ:7.55(1H),7.64(1H),4.05(3H),4...

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Abstract

The present invention discloses uses of an ellagic acid derivatives and a pharmaceutically acceptable salt in hyperuricemia treatment. According to the present invention, the ellagic acid compound provides a strong in vitro inhibition effect on xanthine oxidase, can significantly reduce the serum uric acid level in the hyperuricemia mice, and can be used as the potential xanthine oxidase inhibitor and the uric acid lowering drug for treatment of hyperuricemia and gout or gout complications caused by hyperuricemia.

Description

technical field [0001] The invention belongs to the field of chemical medicine, and specifically relates to the application of an ellagic acid derivative and a pharmaceutically acceptable salt thereof in the preparation of a medicine for treating hyperuricemia, and a medicine for treating hyperuricemia and gout combination. Background technique [0002] In recent years, with the improvement of people's living standards and changes in dietary structure, the intake of sugar, fat, and protein has increased significantly, and the incidence of hyperuricemia and gout has increased day by day, which has become a common disease. [0003] It is generally believed that when the blood uric acid is 416 μmol / L, it is hyperuricemia, and about 5%‐12% of patients with hyperuricemia will develop gout. The clinical features are: recurrent gouty acute arthritis, tophi deposition, characteristic chronic arthritis and joint deformities, often involving the kidneys to cause chronic interstitial ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/366A61K31/7048A61P19/06A61P19/02A61P29/00A61P13/12A61P13/04A61P9/00
Inventor 夏增华
Owner SUZHOU HEYAN BIOTECH
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