Application of substituted benzoyl silybin in preparing medicament for treating virus hepatitis B

A technology of silybin ester and nitrobenzoyl, which is applied in the field of medicine, can solve the problems of less literature and no effective development, and achieve the effect of convenient source, convenient source of raw materials, and less pollution

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

[0010] 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 their new application in anti-hepatitis B virus (especially inhibiting HBV DNA replication). Compounds, that is, structural modification of flavonoid lignans to have anti-DNA viroid activity is a new field

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1: The compound of formula (1) (±)-3-amino-5-nitrobenzoic acid [3-(4-hydroxy-3-methoxyphenyl)-6-(2,3-dihydro-3,5, Preparation of 7-trihydroxy-4-oxo-benzopyran-2)-2,3-dihydro-1,4-benzodioxane-2]-methyl ester

[0023] 1.1 Instruments and reagents:

[0024] UV spectrum was measured with Shimadzu UV-240 UV spectrophotometer; proton nuclear magnetic resonance spectrum 1 H-NMR was measured by INOVA superconducting nuclear magnetic resonance spectrometer (VARIAN INOVA-400MHz) (tetramethylsilyl ether TMS as internal standard); ESI-MS was measured by BrukerEsquire 3000+ mass spectrometer, and silica gel was used for column chromatography (100-200, 200-300 and 300-400 mesh) and thin layer chromatography silica gel GF254 (10-40 mesh) are produced by Qingdao Ocean Chemical Plant; the reagents used are all analytical pure, of which the boiling range of petroleum ether is 60-90℃; Thin-layer preparative chromatography (PTLC) uses Merck's aluminum foil silica gel plate; Sephadex L...

Embodiment 2

[0028] Example 2: The inhibitory effect of the compound of formula (1) on the replication of hepatitis B virus deoxyribonucleic acid (HBV DNA) secreted by HepG2.2.15 cells

[0029] 2.1 Cell culture:

[0030] HepG2.2.15 cells were cultured in DMEM medium containing 10% inactivated fetal bovine serum, 100U / ml penicillin and 100U / ml streptomycin, 100μg / ml G418, and placed at 37°C, 5% CO 2 , Cultivate in an incubator with 100% relative humidity.

[0031] 2.2 Determine the inhibitory effect of compound (1) on the growth of HepG2.2.15 cells by MTT method:

[0032] Take HepG2.2.15 cells in logarithmic growth phase and dilute the cells to 1×10 with medium 5 Pcs / ml, seeded on 96-well cell culture plate, 100 microliters per well, at 37℃, 5% CO 2 After culturing in a 100% relative humidity incubator for 24 hours, add the compound (1) diluted with the medium at the concentration of 1000 μg / ml, 200 μg / ml, 40 μg / ml and 8 μg / ml, 200 per well Microliters, each concentration has three replicate well...

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Abstract

The invention relates to application of substituted benzoyl silybin in preparing a medicament for treating virus hepatitis B, in particular to application of 3-amino-5-nitrobenzoyl substituted silybin ester type flavonolignan or medicinal salt thereof in preparing a medicament for inhibiting HBV DNA replication and treating hepatitis B virus infected diseases. The flavonolignan has the effect of definitely inhibiting HBV DNA activity, the activity of the flavonolignan in high dosage (100 micrograms per milliliter) for inhibiting the HBV DNA replication is 55 percent higher than the inhibiting activity of alpha-interferon at highest concentration of 10,000 units per milliliter, and the flavonolignan belongs to an effectual non-nucleoside natural product for inhibiting the hepatitis B virus. Pharmacodynamical results show that the flavonolignan or the medicinal salt thereof can be expected to be used for preparing the medicament for inhibiting HBV DNA replication and treating the hepatitis B virus infected diseases.

Description

Technical field [0001] The present invention relates to the technical field of medicine. Specifically, the present invention relates to a 3-amino-5-nitrobenzoyl substituted silybin ester type flavonolignan represented by formula (1) or its medicinal use The salt is used to prepare drugs for inhibiting hepatitis B virus deoxyribonucleic acid HBV DNA replication and treating hepatitis B virus. The flavonolignan has the exact inhibitory activity of hepatitis B virus HBV DNA, and its inhibitory activity against hepatitis B virus HBV DNA at high doses (100 μg / ml) is higher than that of α-interferon at the highest concentration of 10000 units / ml. It is 55% higher, which is a markedly effective non-nucleoside natural product that inhibits hepatitis B virus. The above pharmacodynamic results show that the flavone lignan or its pharmaceutically acceptable salt can be expected to be used for preparation to inhibit HBV DNA replication and treat hepatitis B virus infection Use of disease d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/357A61P31/20
Inventor 刘光明邱立鹏朱建华王晓雨王彦广巫秀美赵昱曾苏
Owner DALI UNIV
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