Application of flavonoid quercetin dimmer as medicament for treating viral hepatitis B

A technology of viral hepatitis and quercetin, which is applied in the field of medicine, can solve the problems of no reported anti-HBV activity of quercetin dimer flavonoids, achieve clear industrialization prospects, simple and easy preparation methods, and easy source of raw materials The effect

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

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. As a natural product, there is no record of any quercetin dimer flavonoids having anti-HBV activity, and only the inventor team prepared a new synthesis method and studied its anti-HBV activity.

Method used

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  • Application of flavonoid quercetin dimmer as medicament for treating viral hepatitis B
  • Application of flavonoid quercetin dimmer as medicament for treating viral hepatitis B
  • Application of flavonoid quercetin dimmer as medicament for treating viral hepatitis B

Examples

Experimental program
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Effect test

Embodiment 1

[0025] Example 1: The preparation of formula (1) compound

[0026] 1.1 Instruments and reagents:

[0027] 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 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 of Fuji Silysia Chemical Company of Japan; MCI is the product of Mitsubishi, Japan Chemical company p...

Embodiment 2

[0031] Example 2: Inhibitory Effect of Compound (1) on Hepatitis B Surface Antigen (HBsAg) Secreted by HepG2.2.15 Cells

[0032] 2.1 Cell culture:

[0033] 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.

[0034] 2.2 The inhibitory effect of the compound of formula (1) on HepG2.2.15 cell growth was measured by MTT method:

[0035] 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 compound (1) diluted with medium, the concentration is 1000, 200, 40 and 8 μg / ml respectively, 200 μl per well, and three concentrations are set for each Duplicate wells, placed at 37°C, 5% CO 2 , cultivated...

Embodiment 3

[0044] Example 3: Inhibitory Effect of Compound (1) on Hepatitis B e Antigen (HBeAg) Secreted by HepG2.2.15 Cells

[0045] 3.1 Cell culture: the method is the same as in Example 2.

[0046] 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.

[0047] 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 100 μg / ml, 20 μg / ml and 4 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 medi...

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Abstract

The invention relates to the application of flavonoid quercetin dimmer as the medicament for treating viral hepatitis B, in particular to the application of flavonoid quercetin dimmer or pharmaceutically acceptable salt thereof to the preparation of the medicament for eliminating HBsAg and HBeAg and inhibiting HBV DNA replication. The flavonoid quercetin dimmer or pharmaceutically acceptable salt thereof has obvious HBsAg and HBeAg inhibiting activity, and at the concentration of 100mcg / ml, the flavonoid quercetin dimmer pharmaceutically acceptable salt thereof has the HBsAg eliminating strength of 65.7% and the HBeAg eliminating strength of 44.8% which are respectively 4.1 times and 2.7 times higher than the positive control medicament of Alpha-interferon and has the HBV DNA inhibiting ratio of 44.8% which is 117% of the HBV DNA inhibiting ratio of the Alpha-interferon at the highest test concentration. Therefore, the flavonoid quercetin dimmer or pharmaceutically acceptable salt thereof can be expectedly used for preparing the non-nucleoside medicament for eliminating HBsAg and HBeAg, inhibiting HBV DNA replication and treating viral hepatitis B.

Description

technical field [0001] The present invention relates to the technical field of medicine, in particular, the present invention relates to a quercetin dimer flavone or a pharmaceutically acceptable salt thereof, which is used to prepare and reduce hepatitis B virus surface antigen HBsAg and hepatitis B e antigen HBeAg, inhibit HBV DNA replication, and treat Use of medicines for hepatitis B virus infection. This dimer flavonoid has quite significant activity of inhibiting HBsAg and HBeAg, and its intensity of removing HBsAg and HBeAg is respectively 65.7% and 44.8% under the concentration of 100 micrograms / milliliter, surpasses positive control drug (10000 units / milliliter α- interferon) 4.1 times and 2.7 times; at the same time, it showed 44.8% inhibition rate to HBV DNA at this concentration, and it was 117% of the inhibition rate of α-interferon at the highest test concentration. The above pharmacodynamic results show that the quercetin dimer flavone or its pharmaceutically a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/357A61P31/20A61P1/16
Inventor 王国富施树云郭美仙伍义行张水利巫秀美赵昱谭仁祥
Owner DALI UNIV
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