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Uses of flavonoid compounds in preparation of anti-hepatitis virus medicines

A flavonoid, anti-hepatitis B technology, applied in the field of medicine, can solve problems such as lack of research on anti-HBV medicinal substances

Inactive Publication Date: 2016-06-08
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

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

Method used

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  • Uses of flavonoid compounds in preparation of anti-hepatitis virus medicines
  • Uses of flavonoid compounds in preparation of anti-hepatitis virus medicines
  • Uses of flavonoid compounds in preparation of anti-hepatitis virus medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Example 1 Extraction, separation, preparation of flavonoids

[0017] Take 15 kg of dried roots of Sesame sageum, crush them, and reflux extract them with 95% ethanol for 3 times (50 L×3), each time for 2 hours, combine the extracts and concentrate to obtain 1.05 kg of extract, add water (4 L) 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 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 SephadexLH-20 gel column chromatography and other means to purify, isolate and ...

Embodiment 2

[0020] Embodiment 2 in vitro anti-HBV experiment

[0021] 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% CO2 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 medicines and relates to uses of flavonoid compounds in preparation of anti-hepatitis virus medicines. The flavonoid compounds which are 5,7,8-trihydroxy-4'-methoxyflavone (1) and potengriffioside A (2) are extracted and separated from helicteres angustifolia. Tests prove that the flavonoid compounds have anti-hepatitis virus activity. Pharmacological test results with a lamivudine positive control show that the flavonoid compounds have obvious anti-hepatitis virus functions, wherein the IC50 value for HBsAg of the 5,7,8-trihydroxy-4'-methoxyflavone (1) is 49.3 mug / mL, the IC50 value for HBeAg of the 5,7,8-trihydroxy-4'-methoxyflavone (1) is 68.4 mug / mL, the IC50 value for HBsAg of the potengriffioside A (2) is 14.6 mug / mL, the IC50 value for HBeAg of the potengriffioside A (2) is 41.5 mug / mL, the above mentioned IC50 values are obviously higher than those of the lamivudine positive control. The flavonoid compounds can be adopted as active components and used for preparing the anti-hepatitis virus medicines.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to the use of flavonoids 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 250,000 people died from he...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61K31/7048A61P31/20
Inventor 陈道峰殷翔史训龙朱海燕卢燕
Owner FUDAN UNIV
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