1-O-ethyl-6-O-caffeoyl-beta-D-glucopyranose,1 and pharmaceutical composition and application thereof

A technology of caffeoyl and composition, applied in the direction of preparation of sugar derivatives, sugar derivatives, sugar derivatives, etc., can solve the problem of unclear anti-HBV active substances, no reports of pharmaceutical compositions, and no pharmaceutical composition B virus Hepatitis drug application reports and other issues

Active Publication Date: 2014-05-14
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the reports on the activity of these compounds in the existing literature mainly focus on protecting the liver and promoting gallbladder, and their anti-HBV active substances are still unclear.
[0005] So far, there is no report of compound 1-O-ethyl-6-O-caffeoyl-β-D-glucopyranoside (1) in the prior art, and there is no report of its pharmaceutical composition as an active ingredient, nor There is no report on the application of its pharmaceutical composition in the preparation or treatment of hepatitis B drugs

Method used

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  • 1-O-ethyl-6-O-caffeoyl-beta-D-glucopyranose,1 and pharmaceutical composition and application thereof
  • 1-O-ethyl-6-O-caffeoyl-beta-D-glucopyranose,1 and pharmaceutical composition and application thereof
  • 1-O-ethyl-6-O-caffeoyl-beta-D-glucopyranose,1 and pharmaceutical composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Preparation of 1-O-ethyl-6-O-caffeoyl-β-D-glucopyranoside (1):

[0055] Extraction and separation of 1-O-ethyl-6-O-caffeoyl-β-D-glucopyranoside (1):

[0056] Collect the whole herb of Artemisia capillaris (10kg), whose scientific name is identified as Artemisia capillarisThunb., reflux extraction with 90% ethanol twice for 3 hours each time, combine the ethanol extracts, and recover the ethanol under reduced pressure until there is no alcohol smell. The extract was suspended in an aqueous solution, and extracted with ethyl acetate. The ethyl acetate part was dissolved and adsorbed on silica gel with methanol-chloroform, and the solvent was evaporated at room temperature. After being ground, it was subjected to silica gel column chromatography and eluted with methanol-chloroform (0:100-60:40) to obtain 7 components (A-G). Component F was prepared by medium pressure on MCI CHP-20P gel column, eluted with methanol-water (30:70-100:0), and 4 fractions F-1~F-4.F-3 were obt...

Embodiment 2

[0070] According to the method of Example 1, 1-O-ethyl-6-O-caffeoyl-β-D-glucopyranoside (1) was first prepared, after dissolving with a small amount of DMSO, water for injection was added as usual, finely filtered, Potting and sterilizing to make injection solution.

Embodiment 3

[0072] According to the method of Example 1, 1-O-ethyl-6-O-caffeoyl-β-D-glucopyranoside (1) was first prepared, and after dissolving with a small amount of DMSO, it was dissolved in sterile water for injection , stir to dissolve, filter with a sterile suction filter funnel, then aseptic fine filter, pack in ampoules, lyophilize at low temperature, and aseptically melt seal to obtain a powder injection.

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PUM

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Abstract

The invention provides a 1-O-ethyl-6-O-caffeoyl-beta-D-glucopyranose,1 represented by a structural formula (I), an effective quantity of compound 1 for treatment, a pharmaceutical composition consisting of an officinal carrier or an excipient, a preparation method of the compound and other pharmaceutical compositions and application of the compound and the compositions in preparation of pharmaceuticals for treating human diseases, especially hepatitis B virus hepatitis. (img file='DDA0000472127250000011. TIF' wi='847' he='573' / ).

Description

Technical field: [0001] The invention belongs to the technical field of medicines. Specifically, it relates to a new glucosyl caffeate compound, a pharmaceutical composition for treating viral hepatitis B using it as an active ingredient, their preparation method, and their application in pharmacy, especially in the preparation of anti-hepatitis B Drug application in viral hepatitis. Background technique: [0002] Hepatitis B, referred to as hepatitis B, is an infectious disease caused by hepatitis B virus (HBV), which is generally transmitted through blood and body fluids and is in a chronic carrier state. Its infectivity is 50-100 times stronger than AIDS, and the risk of liver cirrhosis and hepatocellular carcinoma in healthy people after infection increases by 1000 times, and eventually leads to death. According to the statistics of the World Health Organization (WHO), there are 2 billion HBV carriers in the world, including 350 million patients with chronic hepatitis ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H15/04C07H1/08A61K31/7028A61P31/20
Inventor 陈纪军赵勇耿长安马云保黄晓燕张雪梅
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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