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Application of galloyl-glucoside derivative and pharmaceutical composition for treating hyperuricemia

A technology of galloyl glucoside and hyperuricemia, applied in the field of application of galloyl glucoside derivatives and pharmaceutical compositions for the treatment of hyperuricemia, can solve the problem of no further animal experiment data, inhibitory effect not obvious

Active Publication Date: 2015-09-30
SUZHOU HEYAN BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Some scholars [Liu Youhao, Zhao Lichao, Lu Jiaxin, et al. Separation, purification and kinetics of active components of eucalyptus leaf extract that inhibit xanthine oxidase [J]. Guangdong Agricultural Science, 2014, 41(14). 100-105.] The inhibitory effect of pentagalloyl glucose extracted from eucalyptus leaves on xanthine oxidase activity was studied. The IC50 is 31.75 μg / mL, which has a certain inhibitory effect, but the inhibitory effect is not significant, and there is no further animal experiment data for this study

Method used

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  • Application of galloyl-glucoside derivative and pharmaceutical composition for treating hyperuricemia
  • Application of galloyl-glucoside derivative and pharmaceutical composition for treating hyperuricemia
  • Application of galloyl-glucoside derivative and pharmaceutical composition for treating hyperuricemia

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Experimental program
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Effect test

Embodiment 1

[0057] Embodiment 1: Extraction and characterization of compound (1)-(3) of the present invention

[0058] Take 10kg of the medicinal material of myrobalan, pulverize it, and extract it twice with water in a slightly boiling state, each time for 40 minutes. Concentrate the extract in vacuo to 3L, extract the concentrate with n-butanol, concentrate and dry the extract under reduced pressure, use Diaion HP-20 macroporous adsorption resin for n-butanol extraction for column chromatography separation, water, 30% ethanol, 60% ethanol and 95% ethanol were used as eluents for elution. The eluent eluted with water and 30% ethanol is separated by column chromatography on reversed-phase C18 silica gel, and eluted with 5%-35% ethanol as the eluent to obtain compounds 1, 2 and 3 of the present invention respectively. , with HPLC-ESI-MS and NMR detection characterization data as follows:

[0059] Compound (1): 3-O-galloyl-β-D-glucopyranose C 13 h 16 o 10 M-H - :331.21

[0060] 1 H-...

Embodiment 2

[0068] Embodiment 2: Extraction and characterization of compound (4)-(6) of the present invention

[0069] Take 5 kg of dried leaves of Potassium officinalis, crush them, and use 60% ethanol to ultrasonically extract twice at 60°C for 40 minutes each time. Concentrate the extract to 2L in vacuo, extract the concentrate with ether, ethyl acetate and n-butanol respectively, concentrate and dry the extract under reduced pressure, and separate the extracted part of ethyl acetate by column chromatography with Diaion HP-20 macroporous adsorption resin , and eluted with water, 30% ethanol, 70% ethanol, and 95% ethanol as eluents. Take 30% and 70% ethanol eluted parts and use reverse phase C18 silica gel for column chromatography separation, use 20-70% ethanol as the eluent for elution to obtain the compounds (4) and (5) of the present invention respectively And (6), detect characterization data with HPLC-ESI-MS and NMR as follows:

[0070] Compound (4): 1,2,6-tri-O-galloyl-β-D-gluc...

Embodiment 3

[0079] Embodiment 3: Synthesis and characterization of compound (7)-(9) of the present invention

[0080] Compound (7)-(9) of the present invention adopts such as figure 1 Synthetic by the synthetic route shown.

[0081] The specific operation is as follows:

[0082] 1: Synthesis of 1,2-O-isopropylidene-D-glucofuranose

[0083] Using iodine (11g) as a catalyst, add 40.0g of anhydrous D-glucose to 2000ml of acetone, stir, raise the temperature to 56±1°C, continue the reaction for 2 hours, cool, and add 2% (w / w) sulfur to the reaction solution Sodium sulfite solution 2000ml, the reaction solution changed from yellow to colorless, extracted 3 times with 1000ml chloroform respectively, combined the extracts, then washed the extracts with water, dried over anhydrous sodium sulfate, evaporated the chloroform under reduced pressure to obtain the crude product, and dissolved in benzene: Recrystallization from petroleum ether (1:1, V / V) gave 41 g of colorless needle-like crystals of...

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Abstract

The invention relates to a galloyl-glucoside derivative, application of a pharmaceutically acceptable salt of the galloyl-glucoside derivative to preparation of a medicine for treating hyperuricemia or gout, and a pharmaceutical composition for treating hyperuricemia or gout. The structural general formula of the galloyl-glucoside derivative is as shown in the description, wherein R1-R5 are independently selected from H or galloyl. The galloyl-glucoside derivative and the pharmaceutically acceptable salt of the galloyl-glucoside derivative have a remarkable inhibiting effect on xanthine oxidase and can remarkably reduce the uric acid level in blood serum.

Description

technical field [0001] The invention relates to the application of galloyl glucoside derivatives and pharmaceutically acceptable salts thereof in the preparation of medicines for treating hyperuricemia and a pharmaceutical composition for treating hyperuricemia. Background technique [0002] Gout is a group of metabolic diseases in which blood uric acid increases due to purine metabolism disorder and (or) uric acid excretion disorder. The main clinical manifestations are hyperuricemia, recurrent gouty acute arthritis, gouty chronic arthritis and tophi, gouty nephropathy, and renal uric acid stones. At present, there are more than 75 million gout patients in my country, and it is increasing at a rate of 0.97% per year. Gout has become the second largest metabolic disease after diabetes, and seriously endangers people's life and health. [0003] At present, the control of uric acid in the blood is achieved through two ways: one is to inhibit the production of uric acid. Xant...

Claims

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Application Information

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IPC IPC(8): A61K31/7024A61P19/06
Inventor 夏增华
Owner SUZHOU HEYAN BIOTECH
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