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Anti-HBV infection host HNF factor inhibitor and application thereof

A kind of use, anti-hepatitis B technology, applied in the specific inhibitor of host cell hepatic nuclear factor HNF, clinical treatment of hepatitis B virus infection disease, antiviral drug field, can solve the problems such as no literature reports, achieve the effect of enhancing the inhibitory effect

Inactive Publication Date: 2017-06-20
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] Baicalin is a flavonoid compound extracted from the dry root of Scutellaria baicalensis Georigi, a plant of the Labiatae family. The origin of Scutellaria baicalensis is also found; among them, baicalin is one of the main active ingredients of Scutellaria baicalensis, and it is also the main quality control index component of Scutellaria baicalensis and its preparations. According to pharmacological research reports, baicalin has antibacterial, antiviral, anti-inflammatory and anti-tumor properties. , immune regulation, blood pressure reduction, sedation, choleretic, liver protection, anti-oxidation and antispasmodic effects. In vitro experiments show that baicalin has a certain inhibitory effect on HBV replication. In clinical practice, baicalin is also used as an adjuvant drug for hepatitis B treatment. Good curative effect, but the exact mechanism of action of baicalin against HBV has not been reported in the literature, and there is no evidence that the baicalin compounds represented by baicalin have the effect of inhibiting the infection of hepatitis B virus HBV drug-resistant mutant strains

Method used

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  • Anti-HBV infection host HNF factor inhibitor and application thereof
  • Anti-HBV infection host HNF factor inhibitor and application thereof
  • Anti-HBV infection host HNF factor inhibitor and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Baicalin (baicalin) inhibits liver nuclear factor HNF, down-regulates HBV-RNA level, reduces HBV virus surface antigen level and virus particle level test

[0049] After the HepG2 2.2.15 cells grow into a single layer, discard the culture medium, wash the cells once with EDTA solution, add 5 mL of digestive solution (EDTA solution: 0.5% trypsin = 5:1) to each bottle (25cm2 culture flask), and place at 37 ℃ incubator for 5-10 minutes, remove the digestive juice, add an appropriate amount of cell culture medium to each bottle, gently blow down and disperse the adherent cells with a pipette, divide the bottles for passage, and culture at 37°C, 5% CO2, 48 The medium was changed after 1 hour, and the cells were subcultured every 5 days on average. HepG2 2.2.15 cells were digested and prepared into 2×10 5 / mL cell suspension, inoculated in 48-well cell culture plates with 250 μL / well, after culturing for 48 hours to grow into a single layer of cells, add baicalin-containing ...

Embodiment 2

[0056] In vitro anti-HBV wild-type strain test of the combination of baicalin BA and entecavir ETV

[0057] HepG2 2.2.15 cells in 2×10 5 / mL density, 250μL / well was inoculated in a 48-well cell culture plate, and after culturing for 48 hours to grow into a monolayer of cells, a mixture of ETV and BA prepared with culture medium was added, respectively ETV3nM+BA 50μM, ETV0.75nM +BA 50 μM and ETV 0.19 nM +BA 50 μM. At the same time, ETV 3nM, 0.75nM and 0.19nM were used as ETV intervention control alone, and culture medium without drug was set as control. The culture was continued for another 9 days, during which the medium was changed every 3 days, and the cell supernatant was collected after 9 days of sample intervention, and the levels of HBsAg, HBeAg and HBV DNA were detected;

[0058] The detection of HBV antigen in the supernatant of HepG2 2.2.15 cells showed that the inhibitory effect of ETV on HBV antigen was weak when used alone, and the inhibitory effect was improved t...

Embodiment 3

[0060] Anti-HBV rtM204V+rtL180M mutant activity detection of entecavir baicalin combination in vitro

[0061] HepG2 cells were treated with 2×10 5 / mL cell density, 250 μL / hole was inoculated in a 48-well cell culture plate, cultivated for 24 hours, when about 80% confluence, transfected mutant plasmid rtM204V+rtL180M, then added the mixed solution of ETV and BA prepared with culture medium, They were ETV 48nM+BA 50μM, ETV 12nM+BA 50μM, ETV 3nM+BA 50μM and ETV 0.75nM+BA50μM. At the same time, the ETV concentration was 48nM, 12nM, 3nM and 0.75nM respectively. Drug culture solution control; after 6 days of sample intervention (during which the medium was changed once every other day), the cell supernatant was collected, and ELISA kits were used to detect HBsAg and HBeAg, and fluorescent quantitative PCR was used to detect HBV DNA levels;

[0062] The detection of HBV antigen in the supernatant of the HBV rtM204V+rtL180M drug-resistant mutant cell model showed that the inhibitor...

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Abstract

The invention belongs to the technical field of biological medicine, relates to a drug for clinical treatment of HBV infection diseases, and provides application of the natural active material baicalin capable of specifically inhibiting the host nuclear transcription factor HNF (hepatocyte nuclear factor) to preparation of anti-HBV drugs, and application of a pharmaceutical composition composed of a baicalin compound and a nucleoside compound to preparation of drugs for clinical treatment of HBV infection diseases. Experiments prove that baicalin inhibits the replication activity of HBV by interfering with the nuclear transcription factor, and has a remarkable wild type and lamivudine-resistant mutant strain HBV replication inhibiting effect; after being combined with nucleoside analogs, baicalin can effectively improve the HBV drug-resistant mutant strain intervening effect and reduce the toxic and side effects of nucleoside drugs, and can be used for preparing drugs for clinical treatment of HBV infection diseases.

Description

technical field [0001] The invention belongs to the technical field of biomedicine and relates to antiviral drugs in natural active substances, in particular to a host HNF factor inhibitor against HBV infection, in particular to baicalin or nucleoside, a specific inhibitor of host cell liver nuclear factor HNF A drug-like combination for the clinical treatment of hepatitis B virus infection. Background technique [0002] According to the latest statistical data from the Ministry of Health in 2010, the prevalence rate of hepatitis B surface antigen in the country is 7.18%, which is 11% higher than before, and the downward trend is obvious, indicating that the current prevention and control measures are effective. Due to China's huge population base, there are still about 93 million hepatitis B virus carriers in China, of which about 20-30 million are chronic hepatitis B patients. Statistical research on correlations shows that chronic hepatitis caused by hepatitis B virus in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K31/7048A61P31/20A61P1/16A61K31/513A61K31/522
Inventor 史训龙黄海周伟朱海燕周珮
Owner FUDAN UNIV
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