Application of flavone lignan to preparing medicaments for treating virus B hepatitis

A technology for viral hepatitis and flavonoid lignan, applied in the field of medicine, can solve problems such as few documents, and achieve the effects of simple preparation steps, huge social and economic benefits, and high yield

Inactive Publication Date: 2012-03-28
DALI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Although the flavonoid lignan compounds represented by silibinin have the above-mentioned antioxidant effects, there are relatively few literatures on their antiviral treatment

Method used

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  • Application of flavone lignan to preparing medicaments for treating virus B hepatitis
  • Application of flavone lignan to preparing medicaments for treating virus B hepatitis
  • Application of flavone lignan to preparing medicaments for treating virus B hepatitis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1: Formula (1) compound (±)-2-[2,3-dihydro-3-(3,5-dimethoxy-4-hydroxyphenyl)-2-hydroxymethyl-1,4-benzo Preparation of dioxane-6]-2,3-dihydro-3,5,7-trihydroxy-4H-1-benzopyran-4-one

[0023] Instruments and reagents: UV spectra were measured with a Shimadzu UV-240 UV spectrophotometer; H NMR spectra 1 H-NMR is measured by INOVA type superconducting nuclear magnetic resonance spectrometer (VARIAN INOVA-400MHz) (tetramethylsilyl ether TMS is the internal standard); electrospray mass spectrometry ESI-MS is measured by Bruker Esquire 3000+ mass spectrometer, column chromatography Silica gel (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 Sep...

Embodiment 2

[0036] Example 2: Inhibitory Effect of Compound (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 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 ...

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Abstract

The invention relates to application of flavone lignan to preparing medicaments for treating virus B hepatitis, in particular to (+ / -)-2-[2,3-dihydro-3-(3,5-dimethoxy-4-hydroxyphenyl)-2-methylol-1,4-benzodioxane-6]-2,3-dihydro-3,5,7-trihydroxy-4H-1-benzopyran-4-ketone or application of medicinal salts thereof to preparing medicaments for treating the virus B hepatitis or preparing medicaments forreducing virus B hepatitis surface antigens (HBsAg). Because the flavone lignan has high-efficiency activity for suppressing the HBsAg, the flavone lignan can be expected to be applied to preparing medicaments for treating the virus B hepatitis.

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 and pharmaceutical compositions thereof in the preparation and treatment of hepatitis B virus infection diseases and anti-hepatitis B virus drugs use. The flavonoid lignan is found through pharmacodynamic tests to have a strong inhibitory effect on the activity of hepatitis B surface antigen HBsAg, and can be expected to be developed into an anti-hepatitis B virus drug. Background technique [0002] Hepatitis B virus (hepatitis B for short) is an infectious disease caused by hepatitis B virus HBV, which is a member of the hepadnaviridae family of hepadnaviridae. HBV is a peculiar virus that is less contagious in other animals and can only replicate in humans or the primate chimpanzee. The virus is transmitted through blood and body fluids and has a ch...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/357A61P31/20A61P1/16
Inventor 刘蜻蜻赵军王成军李海波廖晓辉巫秀美赵昱曾苏
Owner DALI UNIV
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