Application of angle flavonoids lignan to preparation of medicaments for treating viral hepatitis B

A flavonoid lignan and horn-shaped technology, which is applied in the field of medicine, can solve problems such as not being effectively developed, and achieve the effects of large-scale production, huge social and economic benefits, and low pollution

Inactive Publication Date: 2011-01-26
DALI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Flavonoid lignans have not been effectively developed for the treatment of DNA-like virus infection, especially their new application in anti-hepatitis B virus (especially inhibiting HBV DNA replication). Compounds, that is, flavonoid lignans structurally modified to have anti-DNA virus activity is a new field

Method used

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  • Application of angle flavonoids lignan to preparation of medicaments for treating viral hepatitis B
  • Application of angle flavonoids lignan to preparation of medicaments for treating viral hepatitis B
  • Application of angle flavonoids lignan to preparation of medicaments for treating viral hepatitis B

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1: Formula (1) compound (±)-2-[2,3-dihydro-3-(3-methoxy-4-hydroxyphenyl)-2-hydroxymethyl-1,4 benzodioxane -5] Preparation of -2,3-dihydro-3,5,7-trihydroxy-4H-1-benzopyran-4-one

[0025] Instruments and reagents:

[0026] 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 SephadexLH-20 from Amersham Pharmacia Biotech AB in Sweden; rev...

Embodiment 2

[0045] 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

[0046] 2.1 Cell culture:

[0047] 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.

[0048] 2.2 The inhibitory effect of compound (1) on the growth of HepG2.2.15 cells was determined by MTT method:

[0049] 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 concentration ...

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PUM

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Abstract

The invention relates to application of an angle flavonoids lignan to preparation of medicaments for treating viral hepatitis B, in particular to application of the angle flavonoids lignan or medicinal salts thereof to preparation of medicaments for inhibiting hepatisis B virus (HBV) DNA replication and treating HBV infection diseases. The flavonoids lignan can exactly inhibit HBV DNA activity; the inhibition activity of the flavonoids lignan with high dosage (20 microgram / ml) to the HBV DNA replication is 189 percent higher than that of alpha-interferon with the maximum concentration of 10,000 unit / ml; and the flavonoids lignan belongs to a strong-effect non-nucleosides inhibition HBV natural product. The pharmacological results show that the angle flavonoids lignan or the medicinal salts thereof can be expected to be used for preparing the medicaments for inhibiting hepatisis B virus (HBV) DNA replication and treating the HBV infection diseases.

Description

technical field [0001] The present invention relates to the technical field of medicine, in particular, the present invention relates to an angular flavonoid lignan represented by formula (1) or a pharmaceutically acceptable salt thereof for preparing and inhibiting hepatitis B virus deoxyribonucleic acid HBV DNA replication, treatment The use of hepatitis B drugs. The flavonoid lignans have definite inhibition of hepatitis B virus HBV DNA activity, and its replication inhibitory activity to hepatitis B virus HBV DNA at high doses (20 micrograms / ml) is higher than that of alpha-interferon at the highest concentration of 10,000 units / ml The activity is 189% higher, and it is a potent non-nucleoside natural product for inhibiting hepatitis B virus. The above pharmacodynamic results show that the flavonoid lignan or its pharmaceutically acceptable salt can be expected to be used for the preparation of inhibitors of HBV DNA replication and the treatment of hepatitis B The use of ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/357A61P31/20
Inventor 徐路蒋翔锐刘光明王晓雨郑筱祥巫秀美赵昱曾苏
Owner DALI UNIV
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