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Application of lignan of biphenyl cyclooctene series in preparing anti-hepatitis B virus medicament

A technology of biphenyl cyclooctene lignan and biphenyl cyclooctene, which is applied in new medicinal fields and can solve the problems that patients cannot be cured.

Inactive Publication Date: 2009-03-04
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Clinically, α-interferon and nucleoside drug lamivudine, which have been officially approved by the FDA, can only achieve therapeutic effects to a certain extent, and most patients cannot achieve the purpose of cure. After stopping the treatment, " The "rebound" phenomenon is the most difficult problem for medical workers, so the development of new anti-HBV drugs with high efficiency, low toxicity and no "rebound" poses a challenge to medicinal chemists

Method used

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  • Application of lignan of biphenyl cyclooctene series in preparing anti-hepatitis B virus medicament
  • Application of lignan of biphenyl cyclooctene series in preparing anti-hepatitis B virus medicament
  • Application of lignan of biphenyl cyclooctene series in preparing anti-hepatitis B virus medicament

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1 Preparation of Heqing Schisandra biphenyl cyclooctene lignans

[0030] Take 8kg of dried fruit of Heqing Schisandra (S.wilsoniana), a medicinal plant in Yunnan Province, and soak in 95% ethanol. After concentration, the extract is extracted with ether to obtain a total of 400 grams (extraction rate 5%). Take 200 grams of dry method for loading Perform silica gel column chromatography, eluting with a petroleum ether-acetone gradient, and eluting with a petroleum ether-acetone gradient. In the fraction of oil ether-acetone (30:1), crude crystals were obtained, which were recrystallized in oil ether-acetone (30:1) solvent to obtain Schisandrin A (1); oil ether-acetone (20:1) The fractions were subjected to MCI column (methanol-water (4:1)) to remove the pigment, repeated silica gel column chromatography with petroleum ether-acetone (20:1-15:1), and then applied the preparative TLC method (petroleum ether-ethyl acetate) Ester (10:1)) was purified to obtain gomisin O(2...

Embodiment 2

[0031] Example 2 In vitro anti-HBV experiment

[0032] The 2.2.15 cell line of Hep G2 (Key Laboratory of Medical Molecular Virology of the Ministry of Education / Ministry of Health, Shanghai) is applied to 10×10 per well 5 Cells were inoculated in a 24-well plate, the medium was DMEM, the growth medium contained 10% fetal bovine serum, 380μg / ml G418, 0.03% glutamine, penicillin and streptomycin 100μg / ml each, in 5% CO 2 Incubate in an incubator at 37°C. After 48 hours, change to a dimethyl sulfoxide-assisted drug-containing culture medium. Set 3 to 5 concentrations for each drug and set 4 parallel holes for each concentration. Continue to culture for 9 days (Change the medium every 3 days), collect the supernatant and detect the HBsAg and HBeAg content by ELISA. Under the same conditions, the drug-free culture supernatant was used as the control group. At the same time, the above cell lines were used to determine the cytotoxicity of the drugs by MTT method. The positive control is ...

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Abstract

The invention belongs to the traditional Chinese medicine pharmaceutical field and relates to a new use of a dibenzocyclooctadiene lignan in the preparation of anti-HBV drugs. The invention extracts the dibenzocyclooctadiene lignan from S.wilsoniana of Schisandra plant and confirms the anti-HBV activity thereof through a test. The result of the pharmacological test comparison of the dibenzocyclooctadiene lignan with the active controlled lamivudine proves that the dibenzocyclooctadiene lignan has significant anti-HBV role, low effective concentration and smaller cell toxicity, and the dibenzocyclooctadiene lignan can be used as an active ingredient for preparing the drugs for the treatment of hepatitis B.

Description

Technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to a new medicinal use of biphenylcyclooctene lignans in Heqing Schisandra. In particular, it relates to a new use of biphenylcyclooctene lignans in Heqing Schisandra chinensis in preparing anti-hepatitis B virus drugs. Background technique [0002] Hepatitis B virus (HBV) infection is one of the major diseases affecting human health worldwide. There are approximately 300 million people in the world who are chronic HBV carriers, and my country accounts for about half of them. Because HBV infection can lead to chronic hepatitis, liver cirrhosis and primary liver cancer, it has become one of the nine major diseases affecting human life. Since chronic HBV infected persons have a relative risk of liver cancer of 217 compared with non-carriers, approximately 2 million people die from liver cirrhosis and liver cancer caused by hepatitis B each year in the world. my country is...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/085A61K31/215A61P1/16A61P31/12
Inventor 陈道峰马文辉周佩黄海
Owner FUDAN UNIV
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