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Application of benzyl-containing flavonoid lignan in preparation of medicament for treating hepatitis B

A technology of flavonoid lignans and uses is applied in the application field of benzyl flavonoid lignans for preparing medicines for treating hepatitis B, can solve the problem that there is no anti-hepatitis B virus medicine for hepatitis B virus infectious diseases, etc., and achieves a clear industrialization prospect. , the preparation method is simple and feasible, and the source of raw materials is easy to obtain the effect

Inactive Publication Date: 2010-12-15
DALI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Through the inventor's detailed literature review, so far, there is no report about the formula (1) compound that the present invention relates to treating hepatitis B virus infectious diseases and preparing anti-hepatitis B virus drugs

Method used

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  • Application of benzyl-containing flavonoid lignan in preparation of medicament for treating hepatitis B
  • Application of benzyl-containing flavonoid lignan in preparation of medicament for treating hepatitis B
  • Application of benzyl-containing flavonoid lignan in preparation of medicament for treating hepatitis B

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1: Compound (±)-2-[2,3-dihydro-3-(3-benzyloxy-4-hydroxyphenyl)-2-hydroxymethyl-1,4-benzodioxane Preparation of Cyclo-6]-2,3-dihydro-3,5,7-trihydroxy-4H-1-benzopyran-4-one

[0026] The present invention has prepared the flavonoid lignan compound shown in formula (1) with de novo synthesis method, in addition to this method, can also directly carry out oxidative coupling reaction with the coniferyl alcohol substituted by commercially available pacitaxel and benzyloxy group, The compound of formula (1) is generated in one step. The instruments and reagents used include: Shimadzu UV-240 ultraviolet spectrophotometer for UV spectrum measurement; H NMR spectrum 1 H-NMR is measured by INOVA type superconducting nuclear magnetic resonance spectrometer (VARIAN INOVA-400MHz) (tetramethylsilyl ether TMS is the internal standard); (100-200, 200-300 and 300-400 mesh) and silica gel GF254 (10-40 mesh) for thin layer chromatography are all produced by Qingdao Ocean Chemical...

Embodiment 2

[0039] Example 2: Inhibitory Effect of Compound (1) on Hepatitis B e Antigen (HBeAg) Secreted by HepG2.2.15 Cells

[0040] 2.1 Cell culture:

[0041] HepG2.2.15 cells were cultured in DMEM medium containing 10% inactivated fetal bovine serum, 100 U / ml penicillin and 100 U / ml streptomycin, 100 μg / ml G418 at 37°C, 5% CO 2 , cultured in an incubator with 100% relative humidity.

[0042] 2.2 The inhibitory effect of the compound of formula (1) on HepG2.2.15 cell growth was measured by MTT method:

[0043] Take the HepG2.2.15 cells in the logarithmic growth phase, and dilute the cells to 1×10 with medium 5 cells / ml, seeded in 96-well cell culture plate, 100 μl per well, at 37°C, 5% CO 2 After 24 hours in an incubator with 100% relative humidity, add compound (1) diluted with medium, the concentration is 1000 μg / ml, 200 μg / ml, 40 μg / ml and 8 μg / ml, 200 μg / ml in each well microliter, each concentration was set up in triplicate, placed at 37°C, 5% CO 2 , cultivated in an incuba...

Embodiment 3

[0050] Example 3: Inhibition of the replication of hepatitis B virus deoxyribonucleic acid (HBV DNA) secreted by the compound of formula (1) to HepG2.2.15 cells

[0051] 3.1 Cell culture: the method is the same as in Example 2.

[0052] 3.2 The inhibitory effect of the flavonoid lignan compound represented by formula (1) on the growth of HepG2.2.15 cells was determined by MTT method: the method is the same as that in Example 2.

[0053] 3.3 The flavonoid lignan compounds shown in the assay formula (1) inhibit the replication of hepatitis B virus deoxyribonucleic acid (HBV DNA): get the HepG2.2.15 cells in the logarithmic growth phase, and use the culture medium to dilute the cells to 1 ×10 5 cells / ml, seeded in 96-well cell culture plate, 100 μl per well, at 37°C, 5% CO 2 After cultivating in an incubator with 100% relative humidity for 24 hours, add the flavonoid lignan compound shown in the formula (1) diluted with the culture medium, the concentrations are respectively ...

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Abstract

The invention relates to application of benzyl-containing flavonoid lignan in preparation of a medicament for treating hepatitis B, in particular to application of flavonoid lignan and pharmaceutically-acceptable salt thereof in preparation of the medicament for eliminating hepatitis B e antigen, inhibiting hepatitis B virus desoxyribonucleic acid (HBV DNA) replication and treating viral hepatitis B. The flavonoid lignan can inhibit the activity of hepatitis B virus e antigen (HBeAg); the inhibition intensity of the flavonoid lignan under low concentration of 20 micrograms per milliliter is much higher than that of a positive control front-line medicament lamivudine and an interferon; and the compound with the concentration of 20 micrograms per milliliter displays an inhabitation ratio over 50 percent on the HBV DNA, so that the application of the flavonoid lignan in preparation of the medicament for eliminating the hepatitis B e antigen and the medicament for inhibiting the HBV DNA replication and treating hepatitis B viral diseases can be anticipated.

Description

technical field [0001] The present invention relates to the technical field of medicine, specifically, the present invention relates to flavonoid lignans represented by formula (1) or pharmaceutically acceptable salts thereof for the preparation of drugs for clearing hepatitis B e antigen, inhibiting HBV DNA replication, and treating viral hepatitis B The use of flavonoid lignans has been found through pharmacodynamic tests to have a strong inhibitory effect on the activity of hepatitis B e antigen, and its inhibitory strength is much higher than that of positive control first-line drugs lamivudine and -interference at a low concentration of 20 μg / ml. At the same time, at 20 micrograms per milliliter, the compound also shows an inhibition rate greater than 50% to HBV DNA, so it can be expected to be developed as a drug for reducing hepatitis B e antigen, inhibiting HBV DNA replication or treating hepatitis B virus infection. Background technique [0002] Hepatitis B (HBV) is...

Claims

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Application Information

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IPC IPC(8): A61K31/357A61P31/20
Inventor 彭芳姜皞蒋凌云冯玉冰李峰巫秀美赵昱郝小江
Owner DALI UNIV
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