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Daucane type sesquiterpenes and preparation method and application thereof

A technology of carotane and sesquiterpene, which is applied in the field of preparation of anti-HBV drugs, new carotane-type sesquiterpene compounds and its preparation, 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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  • Daucane type sesquiterpenes and preparation method and application thereof
  • Daucane type sesquiterpenes and preparation method and application thereof
  • Daucane type sesquiterpenes and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0022] Example 1 Preparation of Heqing Schisandrin A-C

[0023] Heqing schisandra fruit 8kg, soaked in 95% ethanol, extracted with diethyl ether after the extract was concentrated, totally obtained 400 grams (extraction rate 5%), got 200 grams dry loading and carried out silica gel column chromatography, washed with petroleum ether-acetone gradient take off. Petroleum ether-acetone (20:1) fraction, the pigment was removed by MCI column (methanol-water (4:1)), eluted by petroleum ether-acetone (20:1) repeatedly on silica gel column, and then prepared by TLC method (petroleum ether-ethyl acetate (10:1)), to obtain Heqing zizi ethylene (2); the flow fraction of petroleum ether-acetone (10:1), through the MCI column (methanol-water (4:1) ) to remove the pigment, and repeatedly eluted with a silica gel column through petroleum ether-acetone (10:1), and then through the preparative TLC method (petroleum ether-ethyl acetate (6:1)), to obtain Heqing zizi allyl (3); Petroleum ether-a...

Embodiment 2

[0024] Example 2 In vitro anti-HBV experiment

[0025] Apply the 2.2.15 cell line of Hep G2 (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 M...

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Abstract

The invention belongs to the traditional Chinese medicine pharmaceutical field and relates to a dancane sesquiterpene, a preparation method thereof and a new use in the preparation of anti-HBV drugs. The invention extracts the dancane sesquiterpene from S.wilsoniana of Schisandra plant and confirms the anti-HBV activity thereof. The result of the pharmacological test comparison of the compound with the active controlled lamivudine proves that the compound has significant anti-HBV role, low effective concentration and smaller cell toxicity, and the dancane sesquiterpene compound 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 carotane-type sesquiterpene compound, a preparation method thereof and an application in 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 ​​he...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/047A61K31/215A61K36/57A61P31/12A61P1/16
Inventor 陈道峰马文辉周佩黄海
Owner FUDAN UNIV
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