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Application of flavone lignan (+/-) Scutellaprostin A in preparing medicaments for treating viral hepatitis type B

A technology of flavonoid lignans and uses, which is applied in the field of use of flavonoid lignans (±) Scutellaprostin A for preparing medicines for the treatment of viral hepatitis B, can solve problems such as few documents, new uses have not been effectively developed, etc., and achieves convenient sources. , is conducive to large-scale production, the preparation method is simple and easy to implement

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

[0015] Although the flavonoid lignan compounds represented by silibinin have the above-mentioned antioxidant effects, there are relatively few literatures on their antiviral treatment
The new application of flavonoid lignans in the treatment of DNA virus infection, especially its anti-hepatitis B virus (including inhibition of HBsAg or HBeAg, inhibition of HBV DNA replication) has not been effectively developed

Method used

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  • Application of flavone lignan (+/-) Scutellaprostin A in preparing medicaments for treating viral hepatitis type B
  • Application of flavone lignan (+/-) Scutellaprostin A in preparing medicaments for treating viral hepatitis type B
  • Application of flavone lignan (+/-) Scutellaprostin A in preparing medicaments for treating viral hepatitis type B

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1: Formula (1) (±)-trans-6-hydroxy-2-hydroxymethyl-3-(3-methoxy-4-hydroxyphenyl)-9-phenyl-2,3-dihydro-[1 , 4] Preparation instruments and reagents of dioxane [2,3-h] benzopyran-7-one:

[0033] The ultraviolet spectrum was measured with a Shimadzu UV-240 ultraviolet spectrophotometer; the hydrogen nuclear magnetic resonance spectrum 1H-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 produced by Qingdao Ocean Chemical Factory; all reagents used are analytically pure, thin-layer preparative chromatography (PTLC ) uses the aluminum foil silica gel plate of Merck Company; Sephadex LH-20 used for column chromatography adopts the product of Amersham Pharmacia Biotech AB Company of Sweden; Reversed-phase silica gel RP-18 adopts the Chromatorex product o...

Embodiment 2

[0040] Example 2: Inhibitory Effect of Compound (1) on Hepatitis B Surface Antigen (HBsAg) Secreted by HepG2.2.15 Cells

[0041] 2.1 Cell culture:

[0042] 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.

[0043] 2.2 The inhibitory effect of the compound of formula (1) on HepG2.2.15 cell growth was measured by MTT method:

[0044] 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

[0053] Example 3: Inhibitory Effect of Compound (1) on Hepatitis B e Antigen (HBeAg) Secreted by HepG2.2.15 Cells

[0054] 3.1 Cell culture: the method is the same as in Example 2.

[0055] 3.2 Determination of the inhibitory effect of the compound of formula (1) on the growth of HepG2.2.15 cells by MTT method: the method is the same as in Example 2.

[0056] 3.3 Determination of the inhibitory effect of the compound on hepatitis B e antigen (HBeAg): take the HepG2.2.15 cells in the logarithmic growth phase, and dilute the cells to 1 × 10 with the medium 5 / ml, seeded in 96-well cell culture plate, 100ml per well, at 37°C, 5% CO 2 After culturing in an incubator with 100% relative humidity for 24 hours, add samples diluted with culture medium at concentrations of 20 μg / ml, 4 μg / ml and 0.8 μg / ml, 200 μl per well, and set three concentrations for each Multiple wells were placed at 37°C, 5% CO 2 , cultivated in an incubator with 100% relative humidity, change the culture med...

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Abstract

The invention relates to application of flavone lignan (+ / -) Scutellaprostin A in preparing medicaments for treating viral hepatitis type B, in particular to a compound with the formula (1) or pharmaceutically-acceptable salts thereof for preparing medicaments for clearing HBsAg and HBeAg and suppressing HBV (Hepatitis B Virus) DNA replication. In the invention, the intensities of the compound for clearing the HBsAg and the HBeAg under the concentration of 20 micrograms / milliliter respectively reach 81.8 percent and 81.9 percent, which are respectively 5.1 times and 4.8 times as high as the corresponding activity of alpha-interferon used as a positive contrast medicament; and what is more exciting, when the compound has the concentration, the compound performs a suppression ratio higher than 81 percent, and the value is also higher than that of both lamivudine and alpha-interferon. Accordingly, the flavone lignan or the pharmaceutically-acceptable salts can be expectably used for preparing nucleoside medicaments for clearing the HBsAg and the HBeAg, suppressing the HBV DNA replication and treating HBV infected diseases.

Description

technical field [0001] The present invention relates to the technical field of medicine, in particular, the present invention relates to a kind of flavonoid lignan (±) Scutellaprostin A or pharmaceutically acceptable salt thereof of A cyclodioxane coupling type, which is used to prepare and reduce hepatitis B virus surface antigen HBsAg and hepatitis B Application of e antigen HBeAg, inhibiting HBV DNA replication, and treating hepatitis B virus infection diseases. This flavonoid lignan has extremely significant inhibition of HBsAg and HBeAg activity, and its intensity of removing HBsAg and HBeAg is as high as 81.8% and 81.9% respectively at the concentration of 20 micrograms / ml. Interferon) 5.1 times and 4.8 times the corresponding activity; more exciting is: at this concentration, it showed an inhibition rate greater than 81% to HBV DNA, higher than the positive control lamivudine, and is α-interference 2.1 times of the inhibitory rate of prime corresponding to HBV DNA. Th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/357A61P31/20
Inventor 申元英贾婕王建超杨雷香莫建霞巫秀美赵昱戴志明
Owner DALI UNIV
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