Application of methoxybenzene benzoyl silibinin in preparing medicine for treating viral hepatitis B

A technology of methoxybenzoyl and silibinin ester, which is applied in the application field of methoxybenzoyl silibinin for preparing a drug for treating viral hepatitis B, and can solve the problem of no reported flavonoid lignan compounds Anti-HBV activity and other issues, to achieve the effect of clear industrialization prospects, large-scale production of energy saving and emission reduction, and low pollution

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

[0011] Zuo Guoying et al. (Zuo Guoying, Liu Shuling, Xu Guili, World Chinese Journal of Digestion, 2006, Vol. 14, No. 13, pp. 1241-1246) reviewed the research progress of the anti-HBV activity of medicinal plant ingredients in vitro in the past 20 years. Natural products, there is no record of any flavonoid lignans having anti-HBV activity, especially silibinin natural products and their derivatives, which are almost unknown in China, and only the team of inventors conducted research on them. Structural modifications and anti-HBV activity studies that have not been noticed before

Method used

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  • Application of methoxybenzene benzoyl silibinin in preparing medicine for treating viral hepatitis B
  • Application of methoxybenzene benzoyl silibinin in preparing medicine for treating viral hepatitis B
  • Application of methoxybenzene benzoyl silibinin in preparing medicine for treating viral hepatitis B

Examples

Experimental program
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Effect test

Embodiment 1

[0023] Example 1: Formula (1) compound (±)-4-methoxybenzoic acid [3-(4-hydroxy-3-methoxyphenyl)-6-(2,3-dihydro-3,5,7-tri Preparation of Hydroxy-4-oxo-benzopyran-2)-2,3-dihydro-1,4-benzodioxane-2]-methyl ester

[0024] 1.1 Instruments and reagents:

[0025] 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; all reagents used are analytically pure, and the boiling range of petroleum ether is 60 -90°C; thin-layer preparative chromatography (PTLC) uses aluminum foil silica gel plates from Merck; column chromatography uses dextran gel Sephadex LH-20 from Amersham Pharmacia Biot...

Embodiment 2

[0029] Example 2: Inhibition of the replication of hepatitis B virus deoxyribonucleic acid (HBV DNA) secreted by the compound of formula (1) to HepG2.2.15 cells

[0030] 2.1 Cell culture:

[0031] 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.

[0032] 2.2 The inhibitory effect of the compound of formula (1) on HepG2.2.15 cell growth was measured by MTT method:

[0033] 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 , add compound (1) diluted with culture medium after 24 hours in the incubator of 100% relative humidity, the concentration is respectively 1000 microgram / ml, 200 microgram / ml, 40 microgram / ml, 8 microgram / ml, every well microliter, each concentra...

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Abstract

The invention relates to an application of methoxybenzene benzoyl silibinin in preparing medicine for treating viral hepatitis B, in particular relates to an application of a silibinin esterified favonolignan compound substituted by 23-site 4-metoxybenzene benzoyl, or pharmaceutically acceptable salt thereof in preparing medicines for inhibiting HBV DNA replication, and treating hepatitis B virus infection diseases, wherein the favonolignan compound has exact inhibition activity to the hepatitis B virus, the inhibition activity thereof at 100 microgramme/mL to the HBV DNA replication of the hepatitis B virus is better than that of the alpha-interferon at the highest concentration of 10000 uint/mL, namely 47% higher than that of the inhibition activity of the alpha-interferon. The pharmacodynamics results show that the favonolignan compound or the pharmaceutically acceptable salt thereof can be expected to be used for preparing the medicine for inhibiting non-nucleoside HBV DNA replication or treating the hepatitis B virus infection diseases.

Description

technical field [0001] The present invention relates to the technical field of medicine, in particular, the present invention relates to a 23-position 4-methoxybenzoyl substituted silybin ester flavonoid lignan or a pharmaceutically acceptable salt thereof represented by formula (1) It is used for preparing medicines for inhibiting the replication of hepatitis B virus deoxyribose nucleic acid HBV DNA and treating hepatitis B virus. The flavonoid lignans have definite activity of inhibiting the activity of hepatitis B virus HBV DNA at high doses (100 micrograms / ml) The replication inhibitory activity to hepatitis B virus HBV DNA is higher than that of alpha-interferon at the highest concentration of 10,000 units / ml (47% higher), which belongs to the effective non-nucleoside inhibitory natural product of hepatitis B virus. The above pharmacodynamic results It shows that the flavonoid lignan or its pharmaceutically acceptable salt can be expected to be used in the preparation of ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/357A61P31/20
Inventor 李春艳金钱星刘卫红伍义行张礼和巫秀美赵昱钱金栿
Owner DALI UNIV
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