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Uses of coumarin compound in preparation of anti-hepatitis B virus drugs

A technology of coumarin and compounds, applied in the field of medicine, can solve the problems of lack of research on medicinal substances

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

AI Technical Summary

Problems solved by technology

Studies have shown that the wild sesame extract has anti-HBV activity, but there is a lack of research on its anti-HBV medicinal substances. So far, there has been no relevant information about 6,7,9α-trihydroxy-3,8,11α related to the present invention. -A report on the anti-HBV activity of trimethylcyclohexane-[d,e]-coumarin

Method used

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  • Uses of coumarin compound in preparation of anti-hepatitis B virus drugs
  • Uses of coumarin compound in preparation of anti-hepatitis B virus drugs
  • Uses of coumarin compound in preparation of anti-hepatitis B virus drugs

Examples

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Embodiment 1

[0013] Example 1 Preparation of 6,7,9α-trihydroxy-3,8,11α-trimethylcyclohexane-[d,e]-coumarin

[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 of purification, isolated t...

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 it 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 coumarin compound in preparation of anti-hepatitis B virus drugs. According to the present invention, a coumarin compound 6,7,9[alpha]-trihydroxy-3,8,11[alpha]trimethylcyclohexane block-[d,e]-coumarin is extracted and separated from a Helicteres plant H.angustifolia, and the anti-hepatitis B virus activity of the compound is confirmed; and compared to the pharmacological experiment results of the positive control lamivudine, the pharmacological experiment results of the compound prove that the compound has significant anti-hepatitis B virus effect, wherein the IC50 on HBsAg is 11.8 [mu]g / ml, the IC50 on HBeAg is 34.2 [mu]g / ml, the IC50 on HBsAg and the IC50 on HBeAg of the compound are significantly higher than the IC50 on HBsAg and the IC50 on HBeAg of the positive control lamivudine, and the compound can be used as the active ingredient so as to be used for preparing the anti-hepatitis B virus drugs.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to the use of coumarin compounds in the preparation of anti-hepatitis B virus drugs, in particular to a coumarin compound 6,7,9α-trihydroxy- Use of 3,8,11α-trimethylcyclohexane-[d,e]-coumarin in the preparation of anti-hepatitis B virus drugs. 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 of liver cirrhosis and liver cancer caused by hepatitis B...

Claims

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Application Information

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IPC IPC(8): A61K31/37C07D311/92A61P31/20
Inventor 陈道峰殷翔史训龙朱海燕卢燕
Owner FUDAN UNIV
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