Use of trans-3,4,5-trihydroxy-diphenyl and derivant for resisting hepatitis B virus

A technology of trihydroxystilbene and hepatitis B virus, which can be applied in the directions of active ingredients of hydroxyl compounds, antiviral agents, drug combinations, etc., and can solve the problems of drug resistance, no effect, obvious toxic and side effects, etc.

Inactive Publication Date: 2005-03-30
RADIOLOGY INST ACAD OF MILITARY MEDICINE SCI PLA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Some of these drugs have obvious anti-HBV effect, but the effect of most drugs is not good, or the toxicity and side effects are obvious, or there is no obvious effect characteristic, especially the virus starts to replicate after stopping the drug or drug resistance appears after long-term medication

Method used

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  • Use of trans-3,4,5-trihydroxy-diphenyl and derivant for resisting hepatitis B virus

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Embodiment 1: the extraction process of compound A

[0015] Polygonum cuspidatum 1.0kg, pulverized and leached three times with 50% methanol aqueous solution at room temperature, each time for 3 days. The filtrates were combined and filtered and then vacuum-dried to obtain 100 g of alcohol extract, which was then extracted three times with ethyl acetate (500 ml / time). The organic phases were combined and vacuum-dried to obtain 30.0 g of a paste. The paste was subjected to silica gel column chromatography with gradient elution, and the eluent was chloroform:methanol (50:1-10:1). Obtain 10 fractions, fraction 5 (3.0g) further use C 18 Column HPLC separation afforded the monomer (100 mg). Compared with the spectrum of the standard substance, it was determined to be trans-3,4',5-trihydroxystilbene.

Embodiment 2

[0016] Example 2: Compound A inhibits the secretion of HBsAg and HBeAg by L2.2.15 cells

[0017] 1 Materials and methods

[0018] 1.1 Test drugs

[0019] Drug name: trans-3,4',5-trihydroxystilbene (compound A) (molecular weight 501.48).

[0020] Drug properties: light yellow powder.

[0021] Purity: more than 95%.

[0022] Preparation method: Weigh 2mg of dry powder and add 0.2ml of DMSO to dissolve completely, then add 3.79ml of 2% DMEM to filter and sterilize.

[0023] 1.2 Cell lines and reagents

[0024] The L2.2.15 cells are preserved in this laboratory, using DMEM medium (GIBCO), supplemented with 10% fetal bovine serum, 100U / ml penicillin, 100U / ml streptomycin, G418 100μg / ml (GIBCO), 0.03% glutamine Amide, pH adjusted to 6.84 with 0.238% Hepes, Tezolan (MTT) (Sigma), Dimethylsulfoxide (DMSO).

[0025] 1.3 Drug handling

[0026] Disperse L2.2.15 cells into a single cell suspension with 0.06% trypsin, press 3×10 4 Cells / well concentration were inoculated in 96-well...

Embodiment 3

[0065] Embodiment 3: the effect of compound A anti-duck hepatitis B virus in vivo

[0066] 1 Materials and methods

[0067] 1.1 Test drugs

[0068] Compound name: trans 3,4',5-trihydroxystilbene.

[0069] Preparation: the concentration is 1.2mg / ml. Preparation method: Weigh 109mg of Compound A, add 3ml of DMSO to dissolve, and then add 67ml of water.

[0070] 1.2 Positive drugs

[0071] Drug name: Lamivudine (3TC).

[0072] Production unit: Glaxo UK.

[0073] Drug lot number: HK-42075.

[0074] 1.3 Instruments and reagents

[0075] NC membrane, purchased from Amersham Company. The DHBV plasmid was extracted by our technicians. The gap translation kit was purchased from Promega. α- 32 p-dCTP was purchased from Beijing Yahui Company. SephadexG-50, purchased from Pharmacia Company. 96-well hybridization spotter: product of Bio-Rad, USA. Geiger counter: product of S.E.International Company in the United States.

[0076] 1.4 Experimental animals

[0077] Male 1-day-...

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Abstract

An application of trans-3,4',5-trihydroxybistyrene in treating the infection of hepatitis B virus and the composite medicine containing trans-3,4',5-trihydroxybistyrene and its derivatives are disclosed.

Description

technical field [0001] The present invention relates to the new application of trans-3,4',5-trihydroxystilbene in the preparation of medicines for treating hepatitis B virus infection Background technique [0002] According to reports, there are 350 million chronic hepatitis B virus (HBV) carriers in the world, accounting for 5% of the world's population. The HBV carrier rate in Asia and Africa is 8%-15%, and 50%-70% of HBV carriers have active virus replication, which is chronic hepatitis B. The 5-year follow-up study shows that the incidence of liver cirrhosis in chronic hepatitis B patients is 2%-20%, 20%-23% develops from compensated liver cirrhosis to decompensated liver cirrhosis, and 6%-15% develops into liver cancer . According to the survey, about 25%-40% of chronic hepatitis B patients in China will eventually die of liver cirrhosis or liver cancer. Over the past two decades, people have been looking for drugs for the treatment and / or prevention of HBV infection...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/045A61K31/05A61P1/16A61P31/12
Inventor 吕秋军郭绍明温利青陈媛媛张敏任建平
Owner RADIOLOGY INST ACAD OF MILITARY MEDICINE SCI PLA
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