Application of luteolin 7-O-glucoside in preparing anti-HBV drug

A technology of luteolin and glucoside, which is applied in antiviral agents, pharmaceutical formulas, medical preparations containing active ingredients, etc., and can solve problems such as no reports of anti-hepatitis B virus activity.

Inactive Publication Date: 2019-03-26
FUDAN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] So far, there is no report of its anti-HBV activity

Method used

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  • Application of luteolin 7-O-glucoside in preparing anti-HBV drug
  • Application of luteolin 7-O-glucoside in preparing anti-HBV drug
  • Application of luteolin 7-O-glucoside in preparing anti-HBV drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1: Compound Luteolin-7-O-glucoside on cytotoxicity and proliferation inhibition experiments

[0021] Determination of the toxicity of the compound luteolin-7-O-glucoside to HepG2.2.15 cells: HepG2.2.15 cells digested with trypsin were inoculated into 96-well plate cells at a density of 5000 cells / well, at 37°C, 5% CO 2 After culturing for 24 hours, discard the liquid, add 100 μl DMEM medium again, and dilute the drug into 4 serial concentrations (respectively: 4 μg / ml, 8 μg / ml, 16 μg / ml, 20 μg / ml), and each dilution has 5 pairs wells, and a normal cell control group was set at the same time. After 48 hours of drug action, the cytotoxicity was detected, and the medium of the same compound concentration was changed once at the same time. After 3 days (the total action time was 5 days), the inhibitory efficiency of the compound on cell growth was detected. The results showed that the compound had no effect on HepG2.2.15 cells. The maximum non-toxic concentration c...

Embodiment 2

[0022] Example 2: Anti-hepatitis B virus effect experiment of compound luteolin-7-O-glucoside

[0023] Determination of the inhibitory effect of the compound luteolin-7-O-glucoside on the hepatitis B virus antigen secreted by HepG2.2.15 cells: ELISA kits were used to detect the levels of hepatitis B virus surface antigen and e antigen in the supernatant collected from the cells, and the operation Proceed according to the instructions of the kit, and finally read the OD value at a wavelength of 450nm with a microplate reader, and compare the inhibitory effect of the reaction compound on the intracellular antigen according to the percentage of the control group;

[0024] Determination of the inhibitory effect of the compound luteolin-7-O-glucoside on the replication of hepatitis B virus particles in HepG2.2.15 cells: after the compound acts on HepG2.2.15 cells for 72 hours, the cells are harvested and broken, digested with DNase, protease After K digestion, phenol-chloroform ext...

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Abstract

The invention belongs to the field of chemicals and relates to an application of luteolin 7-O-glucoside (the molecular formula is C21H20O11, CAS: 5373-11-5) in preparing an anti-HBV drug. The compoundis free of obvious toxic and side effects and anti-proliferative effect to HepG2.2.15 cells which express and secrete hepatitis B virus. The concentration of the maximum non-toxic effect reaches 16 [mu]g / ml. Hatched in 48 hours at the concentration, the inhibiting rates of the compound on a hepatitis b surface antigen HBsAg and an e antigen HBeAg secreted by the HepG2.2.15 cells can separately reach 77.4% and 73.3%, the copy inhibiting effect of hepatitis B virus in the HepG2.2.15 cells reaches 45%, and the transcription inhibiting effect to hepatitis B virus in the HepG2.2.15 cells can reachabout 50%. The formula is as shown in the description.

Description

technical field [0001] The invention belongs to the field of chemical medicines, and relates to the new application of luteolin 7-O-glucoside, in particular to the application of luteolin 7-O-glucoside in the preparation of anti-hepatitis B virus drugs. Background technique [0002] Data show that hepatitis B is a worldwide disease caused by hepatitis B virus (Hepatitis B virus, HBV), which seriously threatens human health. According to statistics, more than half of the population in China has been infected with HBV, among which there are at least 120 million hepatitis B surface antigen (HBsAg) carriers, and there are more than 350 million chronic hepatitis B patients worldwide. In the 1980s, the most effective vaccine to control the spread of hepatitis B was developed so far—the vaccine prepared by recombinant hepatitis B virus surface antigen (HBsAg). In recent years, HB vaccination has been basically popularized among newborns, and the HBV infection rate has declined sign...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61P31/20
CPCA61K31/7048
Inventor 赵超黄丹枫谢幼华崔晓娴杨晓
Owner FUDAN UNIV
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