Application of effective component of geranium wilfordii to treatment or prevention of viral hepatitis

A viral hepatitis and active ingredient technology, applied in the field of compounds and pharmaceutical compositions for the treatment or prevention of viral hepatitis, can solve the problems of drug resistance, huge medical expenses, side effects of drugs, easy rebound, no direct effect on HBeAg and HBsAg clearance, etc. , to achieve the effects of excellent clinical safety, good druggability, and excellent pharmacokinetic properties

Active Publication Date: 2022-08-02
北京中以海德医学研究有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Although these reverse transcriptase inhibitors can effectively reduce the level of HBV DNA and enable patients to control the level of hepatitis B virus, they have no direct effect on the clearance of HBeAg and HBsAg because their target is the process of reverse transcription of RNA into DNA
Therefore, the probability of HBeAg and HBsAg seroconversion in nucleoside analog monotherapy is extremely low, and it cannot really cure hepatitis B, and it is easy to rebound after stopping the drug. Patients need to take drugs for a long time or even life
[0007] Although the above-mentioned reverse transcriptase inhibitors can enable patients to control the level of hepatitis B virus, the resulting drug resistance, huge medical expenses, and serious side effects of drugs should not be underestimated.
The point is that there is still no drug that can completely clear the virus and achieve a functional cure for hepatitis B

Method used

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  • Application of effective component of geranium wilfordii to treatment or prevention of viral hepatitis
  • Application of effective component of geranium wilfordii to treatment or prevention of viral hepatitis
  • Application of effective component of geranium wilfordii to treatment or prevention of viral hepatitis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065] Evaluation of the in vitro anti-HBV activity of Geranolin (HD037) using HepG2-NTCP cells

[0066] The compound preparation method is as follows:

[0067] Taking the preparation of 20mM concentration as an example, the volume of solvent DMSO (μl) = sample mass (mg) × purity ÷ molecular weight ÷ 20 × 10 6

[0068] Control compounds include ETV (batch number: P1214012; 99.0% purity), purchased from Shanghai Titan Technology Co., Ltd. The positive control compound RG7834 (batch number: ET25747-14-P1; 99.5% purity) was purchased from Shanghai WuXi AppTec New Drug Development Co., Ltd. The stock concentrations of the above control compounds were all 20 mM and stored at -20°C.

[0069] Table 1: Main reagents and cellular viruses

[0070]

[0071] Experimental program

[0072] Plating cells and compound treatment

[0073] On day 0, HepG2-NTCP was plated into 48-well plates (7.5 × 10 4 cells / well).

[0074] On day 1, change to medium containing 2% DMSO.

[0075] On...

Embodiment 2

[0101] Geranium polysaccharide (HDHB001-01) extraction and application of HepG2.2.15 cells to evaluate the in vitro anti-HBV activity of Geranium polysaccharide

[0102] The extraction method of geranium polysaccharide, taking the initial 50 grams of geranium powder as an example: take about 50 g of geranium powder, accurately weigh, add fourteen times of water to reflux for extraction for 2 hours, filter, and collect the extract. After adding ethanol to 60% for precipitation, enrichment on macroporous resin, collecting water and 5% ethanol eluate, filtering, and evaporating to dryness to obtain polysaccharide.

[0103] Using HepG2.2.15 cells to evaluate the in vitro anti-HBV activity of geranium polysaccharides: Weigh an appropriate amount of extracted geranium polysaccharides, use H 2 Dissolve O to 10 mg / mL (adjustable), then use H 2 O respectively prepare the drug solution of corresponding concentration;

[0104] Drug precipitation treatment method: 37 ℃ water bath ultras...

Embodiment 3

[0108] Geranium polyphenols (HDHB001-02) extraction and application of HepG2.2.15 cells to evaluate the in vitro anti-HBV activity of Geranium polyphenols

[0109] The extraction method of geranium polyphenols, taking the initial 1 kg of geranium whole grass as an example: 1 kg of dried geranium whole grass is extracted with 10L volume fraction of 75% ethanol water for 3 times, 2 hours each time, and recovered under reduced pressure Remove the ethanol and apply it to a macroporous resin column. Elute four to five volumes with water, 15% ethanol, 35% ethanol and 75% ethanol respectively, and collect the eluate to recover the solvent to obtain solid polyphenol.

[0110] Using HepG2.2.15 cells to evaluate the in vitro anti-HBV activity of geranium polyphenols: Weigh an appropriate amount of extracted geranium polyphenols, use H 2 Dissolve O to 10 mg / mL (adjustable), then use H 2 O respectively prepare the drug solution of corresponding concentration;

[0111] Drug precipitatio...

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Abstract

The invention provides application of an effective component of geranium wilfordii in preparation of a medicine for treating or preventing viral hepatitis, the effective component of geranium wilfordii is selected from at least one of polysaccharide, polyphenol, non-polysaccharide, non-polyphenol and geraniin, and preferably, the viral hepatitis is hepatitis B.

Description

technical field [0001] The present application relates to the technical field of antiviral drugs, in particular, to a compound, a pharmaceutical composition and its application for treating or preventing viral hepatitis. Background technique [0002] Human hepatitis B virus (HBV) infection is a major public health problem worldwide. After acute hepatitis B virus infection, about 8% still develop chronic hepatitis B infection, and persistent HBV infection will lead to liver cirrhosis and even liver cancer. HBV transmission is mainly through vertical and horizontal transmission. Vertical transmission refers to mother-to-child transmission; horizontal transmission is mainly through blood. [0003] The treatment of hepatitis B is also a long-term process. The goal of treatment is to maximize the inhibition or elimination of HBV, reduce liver cell inflammation and necrosis and liver fibrosis, delay and prevent disease progression, reduce and prevent liver decompensation, liver ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/185A61P1/16A61P31/20
CPCA61K36/185A61P1/16A61P31/20Y02A50/30
Inventor 李瑛颖陈明键仇思念
Owner 北京中以海德医学研究有限公司
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