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Application of B/E ring substituted silybin for preparing medicament for treating virus hepatitis B

A technology for viral hepatitis and milk thistle, applied in the field of medicine, can solve the problems of not being effectively developed, few documents, etc., and achieve the effects of being conducive to large-scale production, convenient source, energy saving and emission reduction, and large-scale production.

Inactive Publication Date: 2012-12-05
DALI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] Although the flavonoid lignan compounds represented by silibinin have the above-mentioned antioxidant effects, there are relatively few literatures on their antiviral treatment
Flavonoid lignans have not been effectively developed for the treatment of DNA-like virus infection, especially for anti-hepatitis B virus (including inhibition of HBsAg or HBeAg, inhibition of HBV DNA replication). Active compounds in the field of viruses, that is, structural modification of flavonoid lignans to have anti-DNA virus activity is a new field

Method used

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  • Application of B/E ring substituted silybin for preparing medicament for treating virus hepatitis B
  • Application of B/E ring substituted silybin for preparing medicament for treating virus hepatitis B
  • Application of B/E ring substituted silybin for preparing medicament for treating virus hepatitis B

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1: Compound (±)-2-[2,3-dihydro-3-(4-hydroxy-3,5-dimethoxyphenyl)-2-hydroxymethyl-8-ethoxy- Preparation of 1,4-benzodioxane-6-]-2,3-dihydro-3,5,7-trihydroxy-4H-1-benzopyran-4-one

[0032] 1.1 Instruments and reagents:

[0033] 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 produced by Qingdao Ocean Chemical Factory; all reagents used are 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; Reversed-phase silica gel RP-...

Embodiment 2

[0046] Example 2: Inhibitory Effect of Compound (1) on Hepatitis B Surface Antigen (HBsAg) Secreted by HepG2.2.15 Cells

[0047] 2.1 Cell culture:

[0048] 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.

[0049] 2.2 The inhibitory effect of the compound of formula (1) on HepG2.2.15 cell growth was measured by MTT method:

[0050] 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 ...

Embodiment 3

[0059] Example 3: Inhibitory Effect of Compound (1) on Hepatitis B e Antigen (HBeAg) Secreted by HepG2.2.15 Cells

[0060] 3.1 Cell culture: the method is the same as in Example 2.

[0061] 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.

[0062] 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 culture med...

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Abstract

The invention relates to application of a B / E ring substituted silybin for preparing a medicament for treating virus hepatitis B, in particular to the application of a B ring ethoxy and E ring methoxy substituted silybin ester or medicinal salts thereof for preparing the medicament for eliminating hepatitis B virus surface antigens and hepatitis B e antigen and inhibiting HBV and DNA replication. The medicament has accurate activity of inhibiting HBsAg and HbeAg, and respective intensity of 18.5% and 23.0% in eliminating HBsAg and HbeAg at the concentration of 100 microgram / ml, which exceeds the positive control medicament of an alpha-interferon; and meanwhile, 23.3% inhibition ratio on HBV and DNA is displayed at the concentration of 100 microgram / ml; and therefore, flavonoid lignans or a medicinal salt thereof are proved to have the efficacy of inhibiting HbsAg, HbeAg, HBV and DNA. The application is predictably used for preparing the non-nucleoside medicament for eliminating HBsAg and HbeAg, inhibiting HBV and DNA replication and treating hepatitis B virus infectious diseases.

Description

technical field [0001] The present invention relates to the technical field of medicine, specifically, the present invention relates to a kind of silybin ester substituted by B ring ethoxy group and E ring methoxy group or its pharmaceutically acceptable salt is used for preparing and reducing hepatitis B virus surface antigen HBsAg and Use of hepatitis B e antigen HBeAg, inhibiting HBV DNA replication, and treating hepatitis B virus infection diseases. This flavonoid lignan has the definite activity of inhibiting HBsAg and HBeAg, and its intensity of removing HBsAg and HBeAg is respectively 18.5% and 23.0% at 100 micrograms / ml concentration, all exceeds positive control drug (10000 units / ml alpha-interference At the same time, it showed a 23.3% inhibitory rate to HBV DNA at this concentration. The above shows that the flavonoid lignan or its pharmaceutically acceptable salt has the effect of inhibiting HBsAg, HBeAg and HBV DNA; it can be expected to be used to prepare non-nu...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/357A61P31/20A61P1/16C07D407/04
Inventor 窦辉熊轶施贵荣汪峰张荣平巫秀美赵昱戴志明
Owner DALI UNIV
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