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Application of aminobenzoyl silybin for preparing virus hepatitis B medicine

A technology of aminobenzoyl and silybin, which is applied in the field of medicine, can solve problems such as not being effectively developed, and achieve the effects of convenient source of raw materials, large-scale production of energy saving and emission reduction, and convenient synthesis

Inactive Publication Date: 2010-09-15
DALI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] Flavonoid lignans have not been effectively developed for the treatment of DNA virus infection, especially their new application in anti-hepatitis B virus (including inhibition of HBsAg or HBeAg, inhibition of HBV DNA replication). Active compounds in the field of viruses, that is, modifying the structure of flavonoid lignans to have anti-DNA virus activity is a new field

Method used

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  • Application of aminobenzoyl silybin for preparing virus hepatitis B medicine
  • Application of aminobenzoyl silybin for preparing virus hepatitis B medicine
  • Application of aminobenzoyl silybin for preparing virus hepatitis B medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1: Formula (1) compound (±)-p-aminobenzoic acid [3-(4-hydroxyl-3-methoxyphenyl)-6-(2,3-dihydro-3,5,7-trihydroxyl-4 Preparation of -oxy-1-benzopyran-2)-2,3-dihydro-1,4-benzodioxane-2]methyl ester

[0028] 1.1 Instruments and reagents:

[0029] The ultraviolet spectrum was measured with a Shimadzu UV-240 ultraviolet spectrophotometer; the hydrogen nuclear magnetic resonance 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 Factory; the reagents used are all analytically pure; thin-layer preparative chromatography (PTLC ) uses the aluminum foil silica gel plate of Merck Company; Sephadex LH-20 used for column chromatography adopts the product of Amersham Pharmacia Biotech AB Company of Sweden; Reve...

Embodiment 2

[0036] Example 2: Inhibitory Effect of Compound of Formula (1) on Hepatitis B Surface Antigen (HBsAg) Secreted by HepG2.2.15 Cells

[0037] 2.1 Cell culture:

[0038] 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.

[0039] 2.2 The inhibitory effect of the compound of formula (1) on HepG2.2.15 cell growth was measured by MTT method:

[0040] 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 cultivating in the incubator of 100% relative humidity for 24 hours, add the compound (1) diluted with the medium, the concentration is respectively 1000 μg / ml, 200 μg / ml, 40 μg / ml and 8 μg / ml, 200 μg / ml in each hole microliter, each concentration was set up in triplicat...

Embodiment 3

[0049] Example 3: Inhibitory effect of compound of formula (1) on hepatitis B e antigen (HBeAg) secreted by HepG2.2.15 cells

[0050] 3.1 Cell culture: the method is the same as in Example 2.

[0051] 3.2 Determination of the inhibitory effect of the compound of formula (1) on the growth of HepG2.2.15 cells by MTT method: the method is the same as in Example 2.

[0052] 3.3 Determination of the inhibitory effect of the compound on hepatitis B e antigen (HBeAg): take the HepG2.2.15 cells in the logarithmic growth phase, and dilute the cells to 1 × 10 with the medium 5 / ml, seeded in 96-well cell culture plate, 100ml per well, at 37°C, 5% CO 2 After culturing in an incubator with 100% relative humidity for 24 hours, add samples diluted with culture medium at concentrations of 100 μg / ml, 20 μg / ml and 4 μg / ml, 200 μl per well, and set three concentrations for each Multiple wells were placed at 37°C, 5% CO 2 , cultivated in an incubator with 100% relative humidity, change the ...

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Abstract

The invention relates to the application of aminobenzoyl silybin for preparing a virus hepatitis B medicine, in particular to the application of 23-bit p-aminobenzoyl substituted silybin ester or pharmaceutically acceptable salts thereof for preparing a medicine for eliminating hepatitis B virus surface antigen and hepatitis B e-antigen and inhibiting HBV DNA reproduction. The aminobenzoyl silybin has obvious activity for inhibiting HBsAg and HBeAg, the intensities for eliminating the HBsAg and the HBeAg are respectively of 73.9 percent and 95.3 percent when the concentration is 100 milligram / milliliter and are respectively higher than that of a positive control medicine alpha-interferon by 4.6 times and 5.6 times, and meanwhile, under the same concentration, the inhabitation ratio of the aminobenzoyl silybin for the HBV DNA is larger than 96 percent. The invention indicates the application of flavanolignan or the pharmaceutically acceptable salt which can be used for preparing a non-nucleoside medicine for eliminating the HBsAg and the HBeAg, inhibiting HBV DNA reproduction, treating hepatitis B virus infection diseases.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular, the invention relates to a silybin ester substituted with 23 p-aminobenzoyl groups or a pharmaceutically acceptable salt thereof for preparing HBsAg and HBeAg for lowering hepatitis B virus surface antigen and hepatitis B e antigen , Inhibition of HBV DNA replication, or use of drugs for treating hepatitis B virus infection. This flavonoid lignan has a very significant activity of inhibiting HBsAg and HBeAg, and its intensity of removing HBsAg and HBeAg is respectively 73.9% and 95.3% at a concentration of 100 micrograms per milliliter, surpassing the positive control drug (α of 10000 units / ml) respectively. -Interferon) 4.6 times and 5.6 times; What's more exciting is: at this concentration, it shows an inhibition rate greater than 96% to HBV DNA, which is 19% higher than that of the positive control drug lamivudine and higher than that of α- Interferon 2.5 times. The above pharm...

Claims

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Application Information

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IPC IPC(8): A61K31/357A61P31/20
Inventor 杜一民白玉高鹏飞伍义行窦辉巫秀美赵昱郝小江
Owner DALI UNIV
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