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Preparation method of 3,5-cynarin methyl ester and medicament composition thereof

A technology of caffeoylquinic acid methyl ester and methyl esterification, which is applied to the preparation of carboxylic acid esters, the preparation of organic compounds, chemical instruments and methods, etc., can solve the problem of uncertain covalent closed-loop HBV DNA clearance, side effects, and easy Rebound and other problems, to achieve significant anti-influenza virus activity, strong inhibitory effect, and good anti-influenza virus effect

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

AI Technical Summary

Problems solved by technology

Although nucleoside drugs and interferon-based drugs have certain antiviral effects, their scavenging effects on covalently closed-loop HBV DNA are still uncertain, and they are prone to rebound after drug withdrawal, and virus mutations occur to varying degrees after drug use
Interferon is clinically effective only 30-50%, and has the same side effects as nucleosides

Method used

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  • Preparation method of 3,5-cynarin methyl ester and medicament composition thereof
  • Preparation method of 3,5-cynarin methyl ester and medicament composition thereof
  • Preparation method of 3,5-cynarin methyl ester and medicament composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Embodiment 1: 3, the preparation of 5-DCQAME

[0046] Take 20kg of dried flower buds of Lonicerae pilosula, put them in a round bottom flask, add 12 times the weight of distilled water to reflux for extraction, decoct for 1.5 hours for the first time, filter, add 10 times the amount of distilled water to reflux and extract for 1.5 hours, filter, Add 10 times the amount of distilled water to the filter residue, reflux and extract for 1 hour, combine the three extracts, concentrate and dry the extract under reduced pressure, and obtain a light yellow extract; dissolve the prepared light yellow extract in water, and apply the pretreated D101 type macroporous adsorption resin, combined with HPLC chromatographic analysis, to collect the part containing isochlorogenic acid; the elution conditions of the macroporous adsorption resin: the macroporous resin is treated with 5% NaOH, 10% acetic acid and 95% ethanol respectively before use, When the resin is washed with distilled w...

Embodiment 2

[0049] Example 2: Preparation of capsules of 3,5-dicaffeoylquinic acid methyl ester compound

[0050] prescription:

[0051] 3,5-DCQAME 15g

[0052] PVPK 30 1.5g

[0053] Microcrystalline Cellulose 4.5g

[0054] Low-substituted hydroxypropyl cellulose 0.45g

[0055] Sodium carboxymethyl starch 0.45g

[0056] Magnesium Stearate Appropriate amount

[0057]

[0058] 100 capsules

[0059] 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, packed into capsules, made into 100 capsules, and obtained.

experiment example 3

[0060] Experimental example 3: Anti-hepatitis virus effect of 3,5-DCQAME

[0061] Test drug: 3,5-DCQAME (by the compound prepared in Example 1, batch number: 20091115)

[0062] Reagents: DMEM (produced by Gibco, USA); fetal bovine serum (produced by Gibco, USA); G-418 (produced by Sigma, USA); HbeAg, HbsAg stationary phase radioimmunoassay kit (produced by China Isotope Corporation, North Immunoreagent Research Institute);

[0063] 2.2.15 Cell: In order to transfect the whole genome of HBV (Aayw subunit), human hepatoblastoma cell line that can secrete HbeAg, HbsAg, and HBV-DNA particles (constructed by Mount sinai Medical Center in the United States, Institute of Pharmaceutical Biotechnology, Chinese Academy of Medical Sciences Virus chamber subculture).

[0064] Experimental method: Inoculate 24-well culture plate with 100,000 2.2.15 cells per milliliter, 1ml per well, 37℃5%CO 2 Incubate for 24 hours, add 2-fold dilution of the test solution below the non-toxic concentrati...

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Abstract

The invention relates to a preparation method of 3,5-cynarin methyl ester shown in a formula (1) as well as a medicament composition for preventing influenza and hepatitis. The preparation method comprises the following steps of: preparing 3,5-cynarin methyl ester as well as a medicament composition for preventing influenza and hepatitis by means of semisynthesis by using an extract of one or more of plants such as the composite family, Caprifoliaceae and the like as an intermediate. According to the preparation method of the 3,5-cynarin methyl ester, the 3,5-cynarin methyl ester with high purity can be massively produced from the plants with extremely-low content of the 3,5-cynarin methyl ester.

Description

technical field [0001] The present invention relates to the field of traditional Chinese medicine chemistry, specifically, the present invention relates to the extracts of one or more plants in Compositae, Lonicera and other plants as intermediates, and adopts a semi-synthetic method to obtain 3,5-dicaffeoyl A preparation method of quinic acid methyl ester (3,5-DCQAME), and a pharmaceutical composition of 3,5-DCQAME for anti-influenza and anti-hepatitis. Background technique [0002] Influenza (Influenza), referred to as influenza, is an acute respiratory infectious disease caused by influenza virus. It is mainly spread by air droplets. Influenza viruses belong to the Orthomyxoviridae family, which are enveloped RNA viruses and are divided into three types: A, B, and C. Among them, type A is prone to mutation, and the influenza epidemic caused by it is the most extensive and severe, and it is one of the infectious diseases that are monitored internationally. Once influenz...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C69/757C07C67/08A61K31/216A61P31/16A61P31/20
Inventor 袁海龙肖小河张甜甜
Owner THE FIFTH MEDICAL CENT OF CHINESE PLA GENERAL HOSPITAL
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