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Application of 2-(2-methyl benzothiazole) ethanol compound in preparing anti-HBV drugs

A technology of methylbenzothiazole and hepatitis B virus, which is applied in the direction of antiviral agents, pharmaceutical formulas, and medical preparations containing active ingredients, can solve the problems of many side effects, poor tolerance, and high cost, and achieve non-toxic side effects, Broad application prospects, effect of suppressing duplication

Inactive Publication Date: 2018-11-30
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 2-(2-methyl benzothiazole) ethanol compound in preparing anti-HBV drugs
  • Application of 2-(2-methyl benzothiazole) ethanol compound in preparing anti-HBV drugs
  • Application of 2-(2-methyl benzothiazole) ethanol compound in preparing anti-HBV drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Study on the Inhibitory Effect of 2-(2-Methylbenzothiazole)ethanol on the Reciprocal Binding of HBV c Antigen

[0030] 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, compound A 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 candidate drug. The experimental resul...

Embodiment 2

[0032] 2-(2-Methylbenzothiazole)ethanol inhibits viral replication of wild-type HBV

[0033] Experimental method: Take the well-grown cell line HepG2.2.15 that can produce wild-type HBV virus, the amount of cells is 2×104 / well, add compound A after 24 hours of laying on a 96-well plate, and compound 2 μl per hole (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 treat the collected supernatant, harvest the cultured cell supernatant for 8 days, and then detect the HBV content in the cell culture supernatant DNA content, experimental results such as figure 2 shown. from figure 2 It can be seen from the experimental results that 2-(2-methylbenzothiazole)ethanol has a good effect on inhibiting the replication of wild-type HBV virus, and its IC50 is 4.851uM.

Embodiment 3

[0035] Cytotoxicity of 2-(2-methylbenzothiazole)ethanol in 293t cells

[0036] 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 A, 2 μl per well, the final concentrations are 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; 490nm wavelength, measure the light absorption value of each hole on the enzyme-linked immunosorbent monitor, observe the cytotoxicity of the compound to 293t cells, the experimental results are as follows image 3 shown. from image 3 From the experimental results, it can be seen that the toxicity of 2-(2-methylbenzothiazole)ethanol is low, and it shows no cytotoxicity in 293t cells.

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Abstract

The invention provides an application of a 2-(2-methyl benzothiazole) ethanol compound in preparing anti-HBV (Hepatitis B Virus) drugs. The 2-(2-methyl benzothiazole) ethanol compound according to theinvention is used for preparing the anti-HBV drugs, has a function of inhibiting HBV core protein assembly, is capable of fundamentally inhibiting HBV, has no toxic side effect to cells and has a wide application prospect at the aspect of HBV treatment.

Description

technical field [0001] The invention belongs to the application technical field of ethanol compounds, and relates to the application of a 2-(2-methylbenzothiazole) ethanol compound 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....

Claims

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Application Information

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IPC IPC(8): A61K31/428A61P31/20
CPCA61K31/428A61P31/20
Inventor 潘婷张辉
Owner SUN YAT SEN UNIV
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