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New use of polyhydroxy galloyl-beta-D-glucose derivatives

A technology of galloyl and glucose, applied in the field of medicine, to achieve the effect of wide source, low cost and good anti-helicobacter pylori activity

Inactive Publication Date: 2011-04-20
CHIA TAI TIANQING PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003]Polyhydroxygalloyl-β-D-glucose derivatives are a class of known compounds with a wide range of sources, and their various biological activities have been reported successively, such as scavenging free Base, antioxidant activity, anti-SARS virus infection activity, anti-HCV NS3 protease activity, apoptosis-inducing activity, angiotensin transferase inhibitor activity, cell cycle inhibitor activity, as tyrosine kinase inhibitor activity, etc. But so far, there are no reports of its activity against Helicobacter pylori in the world

Method used

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  • New use of polyhydroxy galloyl-beta-D-glucose derivatives

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065] Embodiment 2 prepares compound 1 and 5 by gallnut

[0066] After crushing 500 g of Galla chinensis, 2000 ml of 50% ethanol-water solution was cold soaked at room temperature to extract three times, soaked for 24 hours each time, and the extracted filtrate was concentrated under reduced pressure to evaporate ethanol to obtain 260 g of crude extract. The crude extract was extracted sequentially with petroleum ether (500ml×4), chloroform (500ml×4), ethyl acetate (500ml×4), and n-butanol (500ml×4), and divided into several parts. The ethyl acetate parts were combined, concentrated and evaporated to dryness, and applied to a gel column (Sephadex LH-20) in batches, followed by water, methanol: water = 2: 8, methanol: water = 4: 6, methanol: water = 6: 4 , methanol: water = 8: 2, methanol, acetone for gradient elution, and detection by thin layer chromatography to obtain 6 components.

Embodiment 2

[0067] The 6 components were subjected to polyamide column decompression column chromatography, followed by ethyl acetate, ethyl acetate: methanol = 10: 1, ethyl acetate: methanol: water = 10: 1: 0.5, ethanol: water = 6:4, ethanol: water = 8: 2, ethanol, acetone: water = 6: 4, acetone: water 8: 2, acetone for gradient elution, and use thin layer chromatography to track the eluate, combined with gel column (Sephadex LH-20) chromatography, followed by gradient elution with water, methanol:water 2:8, methanol:water 4:6, methanol:water 6:4, methanol:water 8:2, methanol, acetone, the same The eluates were combined, concentrated and dried to obtain pure compounds 1 and 5.

[0068] Example 3 Preparation of compound 3 by Rhodiola angustifolia

[0069] 3kg of Rhodiola angustifolia was crushed, soaked and extracted with 10000ml 80% ethanol three times, soaked for one week each time, the crude extract was concentrated under reduced pressure, and after the ethanol was evaporated, 300g of...

Embodiment 3

[0070] Embodiment 4 prepares compound 4 by chebula

[0071] After 2 kg of chebula fruit is pulverized, use 5000 mL of 80% ethanol-water solution, extract by cold soaking at room temperature three times, and soak for one week each time. The extracted filtrate is concentrated under reduced pressure and evaporated to ethanol to obtain 552 g of crude extract. With petroleum ether (600ml × 4), chloroform (600ml × 4), ethyl acetate (600ml × 4), n-butanol (600ml × 4) the crude extract is extracted into multiple parts, and the organic solvent is evaporated to dryness to obtain Petroleum ether fraction 25g, chloroform fraction 30g, ethyl acetate fraction 53g, n-butanol fraction 234g. The n-butanol fraction was applied to polyamide column in batches (20 g per batch). Gradient elution was performed sequentially with chloroform:methanol:formic acid 100:10:1, chloroform:methanol:formic acid 100:15:1, chloroform:methanol:formic acid 60:40:1, methanol:formic acid 50:50:1, and thin The elua...

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Abstract

The invention relates to a usage of polyhydroxy galloyl-Beta-D-glucose derivatives or the medicinal salts in anti-helicobacter pylori, and the invention also relates to a usage of drugs which contain at least one extract of polyhydroxy galloyl-Beta-D-glucose derivative used for the prevention and / or treatment of diseases which are caused by helicobacter pylori.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to the new application of polyhydroxy galloyl-β-D-glucose derivatives, in particular to polyhydroxy galloyl-β-D-glucose derivatives or an extract containing at least one of the derivatives in Use in anti-Helicobacter pylori. Background technique [0002] In 1983, Australian scholars Warren and Marshall first isolated Helicobacter pylori (Hp) from gastric mucosa. A large number of studies have shown that: Helicobacter pylori infection is related to many diseases that seriously endanger human health, such as chronic active gastritis, gastric ulcer, duodenal ulcer, gastric mucosa-associated lymphoid tissue (MALT) malignant lymphoma and gastric cancer wait. According to data, more than 50% of the population in the world is infected with Helicobacter pylori, especially in developing countries, where the adult infection rate reaches 60-80%. In 1994, the International Agency for Research...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/7024A61P1/04
Inventor 李洋张喜全李新祝
Owner CHIA TAI TIANQING PHARMA GRP CO LTD
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