Application of flavanolignan to preparation of medicament for treating viral hepatitis B

A technology of flavonoid lignans and uses, which is applied in the application field of flavonoid lignans for preparing medicines for treating viral hepatitis B, can solve the problems such as no reports on the anti-HBV activity of flavonoid lignans, and achieve a clear industrialization prospect. , Synthetic convenience, the effect of inhibiting HBV DNA replication

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

[0016] 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 flavanolignan to preparation of medicament for treating viral hepatitis B
  • Application of flavanolignan to preparation of medicament for treating viral hepatitis B
  • Application of flavanolignan to preparation of medicament for treating viral hepatitis B

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1: Formula (1) (±)-2-[2,3-dihydro-3-(4-hydroxyphenyl)-2-hydroxymethyl-1,4 benzodioxane-5]-2,3 -Preparation of dihydro-3,5,7-trihydroxyl-4H-1-benzopyran-4-one

[0031] Instruments and reagents:

[0032] 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; reverse-phase silica g...

Embodiment 2

[0051] Example 2: Inhibitory Effect of Compound (1) on Hepatitis B Surface Antigen (HBsAg) Secreted by HepG2.2.15 Cells

[0052] 2.1 Cell culture:

[0053] 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.

[0054] 2.2 The inhibitory effect of the compound of formula (1) on HepG2.2.15 cell growth was measured by MTT method:

[0055] 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

[0063] Example 3: Inhibition of the replication of hepatitis B virus deoxyribonucleic acid (HBV DNA) secreted by the compound of formula (1) to HepG2.2.15 cells

[0064] 3.1 Cell culture:

[0065] Method is with embodiment 2.

[0066] 3.2 The inhibitory effect of the flavonoid lignan compound shown in formula (1) on the growth of HepG2.2.15 cells was determined by MTT method:

[0067] Method is with embodiment 2.

[0068] 3.3 Flavonoid lignan compounds shown in the assay formula (1) inhibit the replication of hepatitis B virus deoxyribonucleic acid (HBV DNA):

[0069] 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 an incubator with 100% relative humidity for 24 hours, add the flavonoid lignan compound shown in the formula (1) diluted with the medium, the concentration is respectively 20 micrograms / ml, 4 micrograms / m...

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PUM

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Abstract

The invention relates to application of flavanolignan to preparation of a medicament for treating viral hepatitis B, in particular to application of angular flavanolignan or a pharmaceutical salt thereof to preparation of a medicament for reducing the surface antigen HBsAg of hepatitis B virus, inhibiting HBV DNA duplication and treating hepatitis B virus infection diseases. The flavanolignan can inhibit the HBsAg activity obviously, and the strength of clearing the HBsAg at the lower concentration exceeds five and half times that of positive control medicaments (alpha-interferon); and simultaneously, the compound shows the inhibition rate of over 45 percent on HBV DNA at 20 micrograms / milliliter of concentration. The pharmacodynamic result indicates that the flavanolignan or the pharmaceutical salt thereof can be used for preparing the medicament for clearing the surface antigen of the hepatitis B virus, inhibiting the HBV DNA duplication or treating the hepatitis B virus infection diseases expectably.

Description

technical field [0001] The present invention relates to the technical field of medicine, in particular, the present invention relates to a kind of horn-type flavonoid lignan or its pharmaceutically acceptable salt, which is used for preparing medicines for reducing HBsAg surface antigen of hepatitis B virus, inhibiting HBV DNA replication or treating hepatitis B virus infection The purposes of disease drug, this flavonoid lignan has extremely significant HBsAg inhibitory activity, and its clearing HBsAg strength surpasses positive control drug (10000 units / ml α-interferon) 5 times under lower concentration (20 microgram / ml) At the same time, the compound showed an inhibition rate greater than 45% on HBV DNA at a concentration of 20 μg / ml. The above pharmacodynamic results show that the flavonoid lignan or its pharmaceutically acceptable salt can be expected to be used in the preparation of drugs for clearing hepatitis B virus surface antigen, inhibiting HBV DNA replication, or...

Claims

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Application Information

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IPC IPC(8): A61K31/357A61P31/20
Inventor 杨继武吴迪瑶肖怀杨雷香陈智巫秀美赵昱郝小江
Owner DALI UNIV
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