Uses of 1,3-benzodioxole compound in preparation of anti-hepatitis B virus drugs

A kind of technology of benzodioxol and compound, applied in the field of preparation of anti-hepatitis B virus drugs

Inactive Publication Date: 2016-04-27
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The compound 2-(3',4'-dihydroxyphenyl)-1,3-benzodioxol-5-aldehyde in the present invention is isolated from this genus for the first time, and modern pharmacological studies have shown that the compound has Antitumor, antibacterial and antioxidative effects, but there is no report about its anti-HBV activity

Method used

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  • Uses of 1,3-benzodioxole compound in preparation of anti-hepatitis B virus drugs
  • Uses of 1,3-benzodioxole compound in preparation of anti-hepatitis B virus drugs
  • Uses of 1,3-benzodioxole compound in preparation of anti-hepatitis B virus drugs

Examples

Experimental program
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Embodiment 1

[0013] Example 1 Preparation of 2-(3',4'-dihydroxyphenyl)-1,3-benzodioxol-5-aldehyde

[0014] Take 25kg of dry roots of Sesame chinensis, crush them, and reflux extract with 95% ethanol for 3 times (50L×3), each time for 2h, combine the extracts and concentrate to obtain 0.95kg of extract, add water (4L) to suspend, and add an equal volume of petroleum Extracted 5 times with ether, ethyl acetate and n-butanol, combined the extracts and concentrated to dryness to obtain 200 g of ethyl acetate extract. The ethyl acetate extraction part was separated by silica gel (200-300 mesh) column chromatography, and sequentially eluted with dichloromethane-methanol (50:1-0:1) gradient to obtain 11 fractions (Fr.1-11) , wherein the fraction Fr.3 (32g) was subjected to silica gel column chromatography (dichloromethane-methanol, 30:1, 20:1, 10:1, 5:1, 3:1, 1:1), MPLC (methanol - water, 20:80-80:20 gradient elution) and semi-preparative HPLC and other means to purify, isolate and obtain compou...

Embodiment 2

[0016] Embodiment 2 in vitro anti-HBV experiment

[0017] 2.2.15 cell line of HepG2 (Ministry of Education / Ministry of Health Key Laboratory of Medical Molecular Virology, Shanghai), with 10×10 cells per well 5 Cells were inoculated in a 24-well plate, the medium was DMEM, the growth medium contained 10% fetal bovine serum, 380 μg / ml G418, 0.03% glutamine, 100 μg / ml each of penicillin and streptomycin, in 5% CO 2 Cultivate in an incubator at 37°C. After 48 hours, replace with a drug-containing culture solution aided by dimethyl sulfoxide. Set 3 to 5 concentrations for each drug, and set 4 parallel wells for each concentration, and continue to cultivate for 9 days. (Change the medium once every 3 days), collect the supernatant and detect the content of HBsAg and HBeAg by ELISA. Under the same conditions, the culture supernatant without drugs was used as the control group. At the same time, the above cell lines were used to measure the cytotoxicity of the drug by MTT method. ...

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Abstract

The present invention belongs to the field of medicine, and relates to uses of a 1,3-benzodioxole compound in preparation of anti-hepatitis B virus drugs. According to the present invention, a 1,3-benzodioxole compound 2-(3',4'-dihydroxyphenyl)-1,3-benzodioxole-5-aldehyde is extracted and separated from a Helicteres plant H.angustifolia, and the experiment results verify that the obtained compound has anti-hepatitis B virus activity; and compared with the results of the positive control lamivudine pharmacological experiments, the experiment results of the compound of the present invention show that the compound has characteristics of significant anti-hepatitis B virus activity, low effective concentration and low cytotoxicity, wherein the IC50 value on HBsAg is 11.7 [mu]g / ml and the IC50 value on HBeAg is 93.0 [mu]g / ml, the IC50 value on HBsAg and the IC50 value on HBeAg of the compound are significantly higher than the IC50 value on HBsAg and the IC50 value on HBeAg of the positive control lamivudine, and the compound of the present invention can be used as the active ingredient so as to be used for anti-hepatitis B virus drug production.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to a 1,3-benzodioxol compound 2-(3',4'-dihydroxyphenyl)-1,3-benzene isolated from the medicinal plant sesame Use of dioxol-5-aldehyde in the preparation of anti-hepatitis B virus medicine. Background technique [0002] According to relevant statistics, there are about 300 million people in the world who are chronic hepatitis B virus (HBV) carriers, and my country accounts for about half of them. Hepatitis B virus infection has become one of the major diseases affecting human health globally. Since HBV infection can lead to chronic hepatitis, cirrhosis and primary liver cancer, it has become one of the nine major diseases affecting human life. Since the relative risk rate of liver cancer among chronic HBV-infected persons compared with non-carriers is 217, about 2 million people die from liver cirrhosis and liver cancer caused by hepatitis B every year in the world. 250,000 people died from c...

Claims

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Application Information

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IPC IPC(8): A61K31/357A61P31/20A61P1/16C07D317/46A61K36/185
Inventor 陈道峰殷翔史训龙朱海燕卢燕
Owner FUDAN UNIV
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