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Application of E-2-styryl benzimidazole compound to preparation of drugs resisting hepatitis B virus

A benzimidazole and styryl technology, applied in the application field of ethanol compounds, can solve the problems of poor tolerance, high cost, many side effects, etc., and achieve the effects of good antiviral effect, wide application prospect, and no toxic and side effects.

Inactive Publication Date: 2018-10-16
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, interferon-α and pegylated interferon-α-2α have many disadvantages, such as poor tolerance, frequent subcutaneous administration (interferon-α), many side effects, high cost, etc.; Except for NOV-205, which is a small molecule non-nucleoside antiviral drug listed in Russia, the other six antiviral drugs are nucleosides / nucleotides that act on the reverse transcriptase (RT) of hepatitis B virus Analogs, which suffer from resistance and side effects (eg, nephrotoxicity and myopathy)
Moreover, none of the current antiviral drugs can de novo antiviral against HBV itself, and cannot completely remove hepatitis B virus

Method used

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  • Application of E-2-styryl benzimidazole compound to preparation of drugs resisting hepatitis B virus
  • Application of E-2-styryl benzimidazole compound to preparation of drugs resisting hepatitis B virus
  • Application of E-2-styryl benzimidazole compound to preparation of drugs resisting hepatitis B virus

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Study on the Inhibitory Effect of E-2-Styrylbenzimidazole on Interbinding of HBV c Antigen

[0026] Experimental method: Take well-grown human adrenal cell line 239t cells and inoculate them in a 96-well transparent flat-bottomed plate, with 5×104 cells per well. The medium used is complete medium: high-glucose DMEM, 10% fetal bovine serum and 1% double antibody, the culture condition is 5% carbon dioxide, 37°C; C and pcDNA3.1-HBVcAg-VFP-N two plasmids. For transfection, liposome-encapsulated transfection was used, lipo2000 was used as the reagent, and 20 μl of transfection solution was used. After 4 hours of transfection, the compound to be screened was added, 2 μl per well, with a final concentration of 50 μM. After culturing for 48 hours, the expression of green fluorescent protein VFP was detected. If there is a decrease in the expression of green fluorescent protein VFP, the compound may become an antiviral drug candidate. Experimental results such as figure 1...

Embodiment 2

[0028] E-2-Styrylbenzimidazole inhibits viral replication of wild-type HBV

[0029] Experimental method: E-2-styrylbenzimidazole compounds of the present invention wild-type HBV virus replication research: take the cell line HepG2.2.15 that grows well and can produce wild-type HBV virus, the amount of cells used is 2×104 / well, 24 hours after the 96-well plate was plated, different concentrations of compounds were added, 2 μl of the compound per well (final concentration 250 μM, 50 μM, 10 μM, 2 μM, 0.4 μM, 0.08 μM, 0.016 μM, 0 μM); use 2% Triton X-100 to process and collect The supernatant of the cells was collected and cultured for 8 days, and then the DNA content of HBV in the cell culture supernatant was detected. Experimental results such as figure 2 shown. It can be seen from the experimental results that E-2-styrylbenzimidazole has a good effect on inhibiting the replication of wild-type HBV virus, and its IC50 is 2.845 μM.

Embodiment 3

[0031] Cytotoxicity of E-2-Styrylbenzimidazole in 293t Cells

[0032] Experimental method: inoculate cells, use DMEM medium containing 10% fetal calf serum to prepare 293t into a single cell suspension, inoculate 1000 cells per well into a 96-well plate with a volume of 200ul per well; add the compound after 24 hours of adherence , 2 μl per well, the final concentrations were 50 μM, 5 μM, 0.5 μM, 0.05 μM, 0.005 μM, 0.0005 μM, 0 μM; after 48 hours of culture, add 20 μl of MTS solution to each well, and continue to incubate in the incubator for 2 to 4 hours; choose 490 nm wavelength, the light absorbance value of each well was measured on an enzyme-linked immunosorbent monitor, and the cytotoxicity of the compound to 293t cells was observed. Experimental results such as image 3 shown. From the experimental results, it can be seen that E-2-styrylbenzimidazole has low toxicity and shows no cytotoxicity in 293t cells.

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Abstract

The invention provides an application of an E-2-styryl benzimidazole compound to preparation of drugs resisting hepatitis B virus. The E-2-styryl benzimidazole compound is used for preparing the drugsresisting the hepatitis B virus, has the effect of inhibiting assembly of core protein of the hepatitis B virus, can inhibit replication of the hepatitis B virus fundamentally, has no toxic and sideeffects for cells and has wide application prospect in the aspect of treatment of the hepatitis B virus.

Description

technical field [0001] The invention belongs to the application technical field of ethanol compounds, and relates to the application of E-2-styrylbenzimidazole compounds in the preparation of anti-hepatitis B virus drugs. Background technique [0002] Hepatitis B virus (HBV) infection is an important public health problem worldwide. After acute hepatitis B virus infection, about 8% still develop into chronic hepatitis B infection, and persistent HBV infection will lead to liver cirrhosis and even liver cancer. my country is a big country with hepatitis B, and there are nearly 130 million hepatitis B virus carriers, accounting for about 9% of the total population. Although the new hepatitis B infection rate has been effectively controlled with the widespread popularization of hepatitis B vaccine, the population base of hepatitis B carriers is large, and the prevention and treatment of hepatitis B has become the top priority of public health problems in my country. Hepatitis...

Claims

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Application Information

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IPC IPC(8): A61K31/4184A61P31/20C07D235/08C07D235/10C07D235/12
CPCA61K31/4184A61P31/20C07D235/08C07D235/10C07D235/12
Inventor 潘婷张辉
Owner SUN YAT SEN UNIV
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