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Application of lignan compound 4-keto pinoresinol in preparing anti-hepatitis B virus medicine

A technology of ketorosinol and compound is applied in the field of lignan compound 4-ketorosinol to prepare anti-hepatitis B virus medicines, which can solve the problem that 4-ketorosinol has not yet reported anti-HBV activity and anti-HBV. Problems such as lack of research on medicinal substances

Inactive Publication Date: 2016-06-15
FUDAN UNIV
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  • Application Information

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Problems solved by technology

Our research shows that the crude extract of Sesame sesame has good anti-HBV activity, but there is a lack of research on its anti-HBV medicinal substances, and the 4-ketopinoresin involved in the present invention has not yet seen anti-HBV activity reports

Method used

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  • Application of lignan compound 4-keto pinoresinol in preparing anti-hepatitis B virus medicine
  • Application of lignan compound 4-keto pinoresinol in preparing anti-hepatitis B virus medicine
  • Application of lignan compound 4-keto pinoresinol in preparing anti-hepatitis B virus medicine

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Experimental program
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Effect test

Embodiment 14

[0012] The extraction and separation of embodiment 14-ketopinoresin

[0013] Take 15kg of dried aboveground part of Sesame, crush it, and reflux extract it with 95% ethanol for 3 times (50L×3), each time for 2h, combine the extracts and concentrate to obtain 1.05kg of extract, add water (4L) to suspend, and mix with equal volume Petroleum ether, ethyl acetate and n-butanol were extracted 5 times, and the extracts were combined and concentrated to dryness to obtain 160 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 (30g) 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, and the compound 4-ketopi...

Embodiment 2

[0015] Embodiment 2 in vitro anti-HBV experiment

[0016] 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 invention belongs to the field of medicine, and relates to application of lignan compounds in preparing an anti-hepatitis B virus medicine. According to the invention, the lignan compound 4-keto pinoresinol is extracted and isolated from Helicteres H.angustifolia, and upon tests, the lignan compound 4-keto pinoresinol is proved to have an anti-hepatitis B virus activity; by comparing the compound with lamivudine, which is taken as positive control, through a pharmacological test, a result shows that the compound is significant in anti-hepatitis B virus effect, and IC50 value to HBsAg is 36.6[micron]g / ml and IC50 value to HBeAg is 126.4[micro]g / ml, significantly greater than the positive control, namely the lamivudine; therefore, the compound disclosed by the invention can be used for preparing the anti-hepatitis B virus medicine as an active ingredient.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to the use of a lignan compound 4-ketopinoresin isolated from the medicinal plant Sesame chinensis 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 every year in the world, and my country is a high-incidence area of ​​hepatitis B. About 250,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/34A61P31/20
Inventor 陈道峰殷翔史训龙朱海燕卢燕
Owner FUDAN UNIV
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