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Method for preparing dicaffeoylquinic acid methyl compound and composition thereof

A technology of caffeoylquinic acid methyl ester and caffeoylquinic acid, which is applied in the field of anti-influenza and anti-hepatitis compositions, and achieves the effects of mild reaction conditions, significant anti-influenza virus activity, and good yield

Inactive Publication Date: 2010-07-14
THE FIFTH MEDICAL CENT OF CHINESE PLA GENERAL HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, what is the material basis of mountain silver flower's anti-virus? What is the relationship between the content of active ingredients and the efficacy? These issues need to be further clarified

Method used

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  • Method for preparing dicaffeoylquinic acid methyl compound and composition thereof
  • Method for preparing dicaffeoylquinic acid methyl compound and composition thereof
  • Method for preparing dicaffeoylquinic acid methyl compound and composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Preparation of dicaffeoylquinic acid methyl ester compound:

[0022] The dicaffeoylquinic acid methyl ester compound is prepared according to the following steps (taking Lonicera macranthoides Hand.-Mazz. dry medicinal materials in the mountain silver flower as an example):

[0023] Take 10kg of dried medicinal material, decoct twice with 10 times the amount of water, each time for 1 hour, combine the decoction, concentrate under reduced pressure to 0.5g crude drug / mL, and add it to the D101 macroporous adsorption resin (sample amount and resin volume The ratio is 1:2~4), first elute with 3 times column volume of water, and discard the water. Then use 5 times column volume of 10% ethanol to elute, and discard the 10% ethanol eluate. After elution with 5 times the column volume of 30-40% ethanol, collect the eluent, dry, add water to dissolve the residue to a concentration of 0.5-1g crude drug / ml, add dilute hydrochloric acid to adjust the pH to 1-4, and extract with et...

Embodiment 2

[0033] Tablet preparation of dicaffeoylquinic acid methyl ester compound composition:

[0034] prescription:

[0035] Crude drug (prepared in embodiment 1

[0036] Dicaffeoylquinic acid methyl esters) 15g

[0037] PVPK 30 1.5g

[0038] Microcrystalline Cellulose 4.5g

[0039] Low-substituted hydroxypropyl cellulose 0.45g

[0040] Sodium carboxymethyl starch 0.45g

[0041] Magnesium Stearate Appropriate amount

[0042]

[0043] Makes 100 pieces

[0044] Mix the above-mentioned pharmaceutical composition with auxiliary materials, add an appropriate amount of distilled water, stir and mix well, probe ultrasonically (4000r / min) for 5 minutes, and high-pressure milk (pressure 1000bar) for 10 laps to obtain a suspension; vacuum-dry and pass through an 80-mesh sieve , granulated with 70% ethanol, dried, added an appropriate amount of magnesium stearate and mixed evenly, and made into 100 tab...

Embodiment 3

[0046] Anti-influenza A virus effect of drugs

[0047] Test drug: caffeoylquinic acid methyl ester component (dicaffeoylquinic acid methyl ester compound prepared in Example 1, batch number: 20091106)

[0048] Experimental material: DMEM (Gibco company), cell maintenance medium except containing 1% fetal bovine serum (FBS, American Gibco product), other components are the same as DMEM culture medium. Hep2 cells, MDCK cells, influenza virus standard strain (A / PR8 / 34), influenza A virus (FluA, H1N1), provided by the Institute of Infectious Diseases of the PLA. 96-well cell culture plate, produced by Calif, USA.

[0049] Cytotoxicity test: Hep2 cells or MDCK cells were seeded in 96-well cell culture plates and placed in CO at 37°C 2 Cultivate in the incubator for 2 days. After the cells grow into a single layer, remove the culture medium, add 0.1ml maintenance solution half-diluted test drug solution, and set 0.1mL maintenance solution as a blank control. Continue to place in ...

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Abstract

The invention relates to a method for preparing a dicaffeoylquinic acid methyl compound and an anti-influenza and antihepatitic medicine composition thereof. The method for preparing a dicaffeoylquinic acid methyl compound has the following steps of: extracting from woodbine, separating and modifying to obtain the dicaffeoylquinic acid methyl compound; and preparing the anti-influenza and antihepatitic medicine composition thereof. A great amount of anti-influenza and antihepatitic medicine composition containing dicaffeoylquinic acid methyl compound used as effective ingredients can be produced from plants with low dicaffeoylquinic acid methyl compound content by the invention.

Description

technical field [0001] The invention relates to the field of traditional Chinese medicine chemistry, in particular to a method for extracting, separating and synthesizing medicinal components of a dicaffeoylquinic acid methyl ester compound from honeysuckle plants and an anti-influenza and anti-hepatitis composition. Background technique [0002] Viral infectious diseases are one of the ten major diseases, which seriously threaten people's health. Influenza virus is the main pathogen that causes acute viral respiratory infectious diseases, and has the characteristics of high infectivity, rapid transmission, and easy occurrence of epidemics. Because the virus can only grow in living cells, the subtype of influenza virus mutates quickly, and the research and production of vaccines are slow, making it difficult for chemical drugs and influenza virus vaccines to exert their optimal therapeutic and preventive effects, and it is currently impossible to predict effectively The tim...

Claims

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Application Information

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IPC IPC(8): C07C69/757C07C67/08A61K31/216A61P1/16A61P31/16A61P31/20
Inventor 肖小河袁海龙张甜甜赵艳玲
Owner THE FIFTH MEDICAL CENT OF CHINESE PLA GENERAL HOSPITAL
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