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Eneyne glucoside ester compounds and drug composition and application thereof

A compound and composition technology, applied in the direction of drug combination, sugar derivatives, sugar derivatives, etc., can solve the problem of less research on anti-HBV activity, no compound, no compound drug composition, drug application report of hepatitis B virus, etc. question

Inactive Publication Date: 2015-12-02
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 choleresis, and there are few studies on their anti-HBV activity. In 2014, Zhao Yong et al. isolated a series of sesquiterpene and chlorogenic acid derivatives from Artemisia annua. Compounds, triterpenes, flavonoids, lignin and phenolic acids have certain in vitro anti-HBV activity (ZhaoY., et al. Fitoterapia.2014, 95, 187-193.; ZhaoY., et al. J. Ethnopharmacol. .)
[0004] So far, there is no compound 3S,8S-dihydroxy-9-decene-4,6-diyne 1-O-(6'-O-caffeoyl)-β-D-glucopyranoside (3S ,8S-dihydroxydec-9-en-4,6-yne1-O-(6'-O-caffeoyl)-β-D-glucopyranoside, 1) and 3S,8S-dihydroxy-9-decene-4,6 -Diyne 1-O-(2'-O-caffeoyl)-β-D-glucopyranoside (3S,8S-dihydroxydec-9-en-4,6-yne1-O-(2'-O- caffeoyl)-β-D-glucopyranoside, 2), there is no report on the pharmaceutical composition of compound 1 or / and 2 as an active ingredient, and there is no compound 1 or / and 2 pharmaceutical composition in the preparation or treatment of B virus Reports on the Application of Drugs for Chronic Hepatitis

Method used

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  • Eneyne glucoside ester compounds and drug composition and application thereof
  • Eneyne glucoside ester compounds and drug composition and application thereof
  • Eneyne glucoside ester compounds and drug composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Preparation of Compounds 1 and 2:

[0055] Extraction and separation of compounds 1 and 2:

[0056] Take the dried whole herb of Artemisia capillaris or Artemisia scoparia, crush it, and reflux extract it twice with 90% ethanol for 3 hours each time, combine the ethanol extracts, recover the ethanol under reduced pressure to obtain the extract. The extract is dissolved and adsorbed on silica gel with 80% ethanol, placed at room temperature to evaporate the solvent, ground and sieved, and subjected to silica gel column chromatography, with chloroform-methanol-water (9:1:0, 9:1:0.1, 8: 2:0.2, 6:4:0.4) gradient elution, to obtain 5 components A-E, component D was prepared by MCICHP-20Pgel column medium pressure, acetonitrile-water (20:80 to 80:20) gradient elution, to obtain 5 fractions D-1 to D-5. D-4 was subjected to silica gel column chromatography and eluted with ethyl acetate-methanol-water 8:2:0.2 to obtain two fractions D-4-1 and D-4-2. D-4-2 via Rp-C 18 The col...

Embodiment 2

[0083] Compound Combination Pharmaceutical Form - Tablet:

[0084] Compound 1 or / and 2 of the present invention is used as the preparation of the drug combination tablet of active ingredient: use compound 1 or / and 2 as drug active ingredient, use the excipient described in Table 3 as the adjuvant component of preparation combination drug tablet, Tablet samples containing 5 to 60 mg of the pharmaceutical ingredients of compound 1 or / and 2 were made according to the ratio. Table 3 shows the formula ratio of common tablets:

[0085] Table 3 The raw material and adjuvant formula of compound 1 or / and 2 combination medicine tablet of the present invention

[0086]

[0087] The method of preparing a certain amount of compound 1 or / and 2 with excipients and auxiliary materials into tablet preparations of different doses is to uniformly mix several excipients and auxiliary materials with the raw material drug, and add 1% hydroxymethylcellulose sodium solution in an appropriate amoun...

Embodiment 3

[0089] Compound Combination Pharmaceutical Form - Capsules:

[0090] Preparation of pharmaceutical combination capsule preparations containing compound 1 or / and 2 as active ingredients: use compound 1 or / and 2 samples as pharmaceutical active ingredients, use several excipients in the table as excipients for preparing combination drug capsules, according to the proportion Proportioning is made into capsule preparations containing 5-50 mg of the pharmaceutical ingredients of Compound 1 or / and 2 in each capsule, and Table 4 provides the formula ratio of common capsule preparations:

[0091] Table 4 The bulk drug and adjuvant formula of the compound drug capsule preparation

[0092]

[0093] The method for preparing a certain amount of compound 1 or / and 2 samples and excipients and auxiliary materials into capsule preparations is: mix several excipients and auxiliary materials with compound 1 or / and 2 evenly, add 1% hydroxymethyl cellulose Appropriate amount of sodium solutio...

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Abstract

The invention provides two eneyne glucoside ester compounds of 3S,8S-dihtdroxydec-9-en-4,6-yne 1-O-(6'-O-caffeyl)-beta-D-glucopyranoside,1 and 3S,8S-dihtdroxydec-9-en-4,6-yne 1-O-(2'-O-caffeyl)-beta-D-glucopyranoside,2 shown in the structural formula I, a drug composition composed of therapeutically effective amount of the compound 1 or / and the compound 2 and a pharmaceutical carrier or an excipient, a preparation method of the compound 1 or / and the compound 2 and the drug composition thereof, and application of the compound 1 or / and the compound 2 and the drug composition for preparing drugs for treating human diseases particularly the viral hepatitis type B.

Description

Technical field: [0001] The invention belongs to the technical field of medicines. Specifically, it relates to two new enyne glycoside ester compounds 1 and 2, a pharmaceutical composition for treating viral hepatitis B with compounds 1 and / or 2 as active ingredients, their preparation methods, and their use in pharmaceuticals application, especially in the preparation of anti-hepatitis B drugs. Background technique: [0002] Hepatitis B caused by hepatitis B virus (HBV) is a serious infectious disease that affects human health. In particular, chronic hepatitis B (chronichepatitisB, CHB) can be carried for a long time, and is the main cause of liver cirrhosis and liver cancer. According to World Health Organization (WHO) statistics, there are 2 billion HBV carriers in the world, of which about 350 million are CHB patients; as a high-incidence area, China has about 120 million HBV carriers, and more than 30 million CHB patients (Lin Yonghuan. Hepatitis B Prevention and Tre...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H15/10C07H1/08A61K31/7028A61P31/20A61P1/16
Inventor 陈纪军耿长安黄晓燕马云保赵勇张雪梅
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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