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Application of flavanonol lignanoid in preparing antiviral hepatitis B medicine

A technology of flavonoid lignans and dihydrogen, applied in antiviral agents, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve the problems of no reported anti-HBV activity of flavonoid lignans and achieve industrialization prospects The effects of clarity, convenient source, and easy-to-obtain raw material source

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

[0018] 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, among which there is no record of any flavonoid lignans having anti-HBV activity, especially the natural products of silybin and its derivatives, almost no one in China

Method used

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  • Application of flavanonol lignanoid in preparing antiviral hepatitis B medicine
  • Application of flavanonol lignanoid in preparing antiviral hepatitis B medicine
  • Application of flavanonol lignanoid in preparing antiviral hepatitis B medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1: Formula (1) compound (±)-2-[2,3-dihydro-3-(3,5-dimethoxy4-hydroxyphenyl)-2-hydroxymethyl-1,4 benzodiox Preparation of Hexacyclo-5]-2,3-dihydro-3,5,7-trihydroxy-4H-1-benzopyran-4-one

[0033] Instruments and reagents:

[0034] 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 Sephadex LH-20 from Amersham Pharmacia Biotech AB in Swe...

Embodiment 2

[0053] Example 2: Inhibitory effect of compound (1) on hepatitis B e antigen (HBeAg) secreted by HepG2.2.15 cells.

[0054] 2.1 Cell culture:

[0055] 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.

[0056] 2.2 The inhibitory effect of compound (1) on the growth of HepG2.2.15 cells was determined by MTT method:

[0057] 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 ...

Embodiment 3

[0064] 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

[0065] 3.1 Cell culture: the method is the same as in Example 2.

[0066] 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.

[0067] 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 20 microgr...

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Abstract

The invention relates to application of flavanonol lignanoid in preparing an antiviral hepatitis B medicine, in particular to application of angle flavanolignan or pharmaceutically acceptable salts thereof in preparing a medicine which can be used for eliminating hepatitis B e antigen HBeAg, inhibiting HBV DNA replication and treating hepatitis B virus infection diseases. The flavanolignan has a certain HBeVg activity inhibition, the HBeAg elimination intensity of the flavanolignan is higher than that of a positive control first-line medicine as lamivudine in light concentration and is equivalent to that of alpha-interferon of 1000 unit / ml, and meanwhile, under the concentration of 20 microgram / ml, the flavanolignan displays an inhibition ratio which is larger than 45 percent for HBV DNA. The pharmacodynamics result indicates the application of the flavanolignan or the pharmaceutically acceptable salts thereof in preparing the medicine as expected for eliminating hepatitis B e antigen, inhibiting HBV DNA replication and treating hepatitis B virus infection diseases.

Description

technical field [0001] The present invention relates to the technical field of medicine, in particular, the present invention relates to a flavonoid lignan compound with an angular structure represented by formula (1) or a pharmaceutically acceptable salt thereof, which is used for the preparation of anti-hepatitis B e antigen and inhibition of hepatitis B virus Deoxyribonucleic acid HBV DNA replication, the use of drugs for the treatment of hepatitis B virus, the flavonoid lignans have been found to have a certain inhibitory activity of hepatitis B virus core antigen HBeAg through pharmacodynamic tests, and its HBeAg removal strength is at a low concentration of 20 μg / ml The lower stool is higher than that of the positive control first-line drug lamivudine, and is equivalent to 10000 units / ml of α-interferon; at the same time, the compound shows an inhibition rate of greater than 45% on HBV DNA at 20 μg / ml. The above pharmacodynamic results show that the flavonoid lignan or i...

Claims

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Application Information

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IPC IPC(8): A61K31/357A61P31/20
Inventor 董晓东敖雷何正春伍义行罗尔夫·希尔根菲尔德巫秀美赵昱谭仁祥
Owner DALI UNIV
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