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Application of substituted isosilybin in preparing medicament for treating virus hepatitis B

A technology for the use of isosilibinin, which is applied in the field of replacing isosilibinin for the preparation of drugs for the treatment of viral hepatitis B, achieves clear industrialization prospects, simple and easy preparation methods, and the effect of inhibiting HBV DNA replication

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

[0013] Flavonoid lignans have not been effectively developed for the treatment of DNA-like virus infection, especially for anti-hepatitis B virus (including inhibiting hepatitis B e antigen HBeAg or inhibiting HBV DNA replication). The active compounds in the field of hepatitis B virus, that is, the structural modification of flavonoid lignans to have anti-DNA virus activity is a new field

Method used

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  • Application of substituted isosilybin in preparing medicament for treating virus hepatitis B
  • Application of substituted isosilybin in preparing medicament for treating virus hepatitis B
  • Application of substituted isosilybin in preparing medicament for treating virus hepatitis B

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1: Compound (±)-2-[2,3-dihydro-2-(3-benzyloxy-4-hydroxyphenyl)-3-hydroxymethyl-1,4-benzodioxane Preparation of cyclo-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 was measured by INOVA superconducting nuclear magnetic resonance spectrometer (VARIAN INOVA-400MHz) (tetramethylsilyl ether TMS was used as 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 Biotech AB in Sweden; rev...

Embodiment 2

[0043] Example 2: Inhibitory Effect of Compound (1) on Hepatitis B e Antigen (HBeAg) Secreted by HepG2.2.15 Cells

[0044] 2.1 Cell culture:

[0045] 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.

[0046] 2.2 The inhibitory effect of compound (1) on the growth of HepG2.2.15 cells was determined by MTT method:

[0047] 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 incubator w...

Embodiment 3

[0054] 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

[0055] 3.1 Cell culture: the method is the same as in Example 2.

[0056] 3.2 The inhibitory effect of the flavonoid lignan compound represented by formula (1) on the growth of HepG2.2.15 cells was determined by MTT method: the method is the same as that in Example 2.

[0057] 3.3 The flavonoid lignan compounds shown in the assay formula (1) inhibit the replication of hepatitis B virus deoxyribonucleic acid (HBV DNA): get the HepG2.2.15 cells in the logarithmic growth phase, and use the culture medium to dilute the cells to 1 ×10 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 100 microg...

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Abstract

The invention relates to application of substituted isosilybin in preparing a medicament for treating virus hepatitis B, in particular to application of E-ring substituted isosilybin or medicinal salt thereof in preparing a medicament for clearing hepatitis B e antigen, inhibiting HBV DNA replication and treating hepatitis B virus infected diseases. The E-ring substituted isosilybin has strong effect of inhibiting HBeAg activity, and the strength of the E-ring substituted isosilybin at the concentration of 100 micrograms per milliliter for clearing the HBeAg is 3.5 times that of a positive control front-line medicament (10,000 units per milliliter of alpha-interferon); and moreover, the compound at the concentration of 100 micrograms per milliliter has strong inhibiting rate (97.7 percent) on the HBV DNA. Pharmacodynamical results show that the E-ring substituted isosilybin or the medicinal salt thereof can be expected to be used for preparing the medicament for treating the hepatitis B virus infected diseases.

Description

technical field [0001] The present invention relates to the technical field of medicine, in particular, the present invention relates to an E-ring substituted isosilibinin derivative represented by formula (1) or a pharmaceutically acceptable salt thereof for preparing anti-hepatitis B e antigen and inhibiting hepatitis B Viral deoxyribonucleic acid HBV DNA replication, the use of drugs for the treatment of hepatitis B virus, the E-ring substituted isosilibinin derivatives have been found through pharmacodynamic tests to have a strong ability to inhibit the activity of hepatitis B virus core antigen HBeAg, and it can clear HBeAg The strength is 3.5 times that of the positive control first-line drug (10000 units / ml of α-interferon) at a concentration of 100 micrograms / ml; more importantly: the compound shows extremely high levels of HBV DNA at a concentration of 100 micrograms / ml. Potent 97.7% inhibition rate. The above pharmacodynamic results show that the E-ring substituted ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/357A61P31/20
Inventor 李辉邹宏斌丁云胡明辉赵荣华巫秀美赵昱钱金栿
Owner DALI UNIV
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