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Application of compound MEAN (6-methoxyethylamino-numonafide) in preparation of anti-HBV (Hepatitis B Virus) drugs

A compound and drug technology, applied in the field of medicine, can solve the problem of no report on antiviral activity, and achieve the effect of strong anti-HBV activity and strong targeting of PTB protein

Inactive Publication Date: 2014-12-17
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Compound MEAN (6-methoxyethylamino-numonafide) is a newly synthesized class of numonafide compounds, and the synthetic route of this compound has been reported in the literature (JohnT.Norton, Anti-Cancer Drugs2008 , 19(11)), but its antiviral activity has not been reported, the present invention provides the new application of compound MEAN (6-methoxyethylamino-numonafide) anti-HBV activity

Method used

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  • Application of compound MEAN (6-methoxyethylamino-numonafide) in preparation of anti-HBV (Hepatitis B Virus) drugs
  • Application of compound MEAN (6-methoxyethylamino-numonafide) in preparation of anti-HBV (Hepatitis B Virus) drugs
  • Application of compound MEAN (6-methoxyethylamino-numonafide) in preparation of anti-HBV (Hepatitis B Virus) drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Effects of target compounds on HBV DNA replication

[0034] Such as figure 1 As shown, 40 μM and 20 μM compounds are toxic to HepG2.2.15 cells, 10 μM is not toxic to HepG2.2.15 cells, IC50 is 14.89 μM. Therefore, the concentration of 10 μM or below was used as the intervention concentration to determine the anti-HBV efficacy.

[0035] Compounds were used to intervene HepG2.2.15 cells at concentrations of 8 μM, 4 μM and 2 μM for 2 days, and the level of HBV DNA in the cell supernatant was detected by fluorescent quantitative PCR. The instrument used is ABI7500 real-time fluorescence quantitative PCR system. The specific steps are operated in accordance with the instructions of the Hepatitis B Virus Nucleic Acid Quantitative Detection Kit, and the brief description is as follows: the viral DNA in the cell culture supernatant is extracted with the nucleic acid extraction solution of the kit, and then the viral DNA is used as a template, and the prepared reaction system i...

Embodiment 2

[0038] Effects of target compounds on the secretion and expression of HBeAg

[0039] The compound was intervened in HepG2.2.15 cells at 8 μM, 4 μM and 2 μM concentrations for 2 days, and the HBeAg level in the cell supernatant was detected by electrochemiluminescence technology. The instrument used was Abbott Architect I2000sr (Abbott), and the reagent used was hepatitis B HBeAg matched with the Abbott Architect I2000sr instrument. Quantitative detection manual (Abbott), the specific steps are operated according to the manual.

[0040] Such as image 3 As shown, compared with the blank control group, 8 μM compound MEAN has a significant difference in the inhibitory effect on HBeAg, while other concentrations have no significant difference.

[0041] Effects of target compounds on the secretion and expression of HBsAg

[0042] The compound was intervened in HepG2.2.15 cells at concentrations of 8 μM, 4 μM and 2 μM for 2 days, and the level of HBsAg in the cell supernatant was de...

Embodiment 3

[0045] Effect of target compound on PTB protein expression

[0046] WesternBlot was used to detect the expression level of PTB protein. Total cell protein was extracted and quantitatively analyzed according to the operating instructions of the BCA protein quantification kit. 40 μg of the above-mentioned total cellular protein was separated by SDS-PAGE and transferred to a nitrocellulose membrane. After blocking with 1% bovine serum albumin, the membrane was incubated with antibodies PTB (self-made) and β-actin (Cellsignalingtechnology) at 4°C overnight, and the secondary antibody was incubated for 1 hour and detected with chemiluminescence reagent ECL (Pierce).

[0047] Such as Figure 5 As shown, compared with the blank control group, MEAN can significantly down-regulate the expression of PTB protein in cells, and there is a significant difference. Different from the literature reports, for RNA viruses, MEAN can inhibit PTB nucleus-cytoplasm translocation in RNA-infected c...

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Abstract

The invention belongs to the field of medicines, relates to novel medicinal application of a compound MEAN (6-methoxyethylamino-numonafide) of human-targeting PTB (polypyrimidine tract-binding) protein, and particularly relates to application of a novel compound MEAN of the human-targeting PTB protein in the preparation of anti-HBV (Hepatitis B Virus) drugs. Shown by results of the application, the compound MEAN has relatively strong antiviral activity, particularly, can lower the expression level activity of HBsAg, and has a PTB protein targeting effect. The lead compound disclosed by the invention has relatively good application prospects; the compound can be used for preparing anti-HBV drugs and can also be used for preparing drugs taking PTB protein as a target.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to a new medicinal use of a compound MEAN (6-methoxyethylamino-numonafide) targeting human PTB (polypyrimidinetract-binding protein) protein, in particular to the preparation of anti-HBV anti-HBV compound MEAN targeting human PTB protein application in medicine. Background technique [0002] It is known that hepatitis B is one of the infectious diseases that seriously threaten human health. Hepatitis B Virus (HBV) is a small DNA virus belonging to the family Hepatophagoviridae. This virus was discovered by Dana (Dane) in 1965, and it was named Dana (Dane) particles (Seeger and Mason 2000). HBV is distributed globally. At present, there are about 350 million chronic carriers of HBV in the world, and about 1 million people die of diseases caused by HBV every year. my country is a high prevalence area of ​​HBV infection. The 2012 "China Health Statistical Yearbook" shows that the incidence of...

Claims

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Application Information

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IPC IPC(8): A61K31/473A61P31/20A61P1/16A61P29/00
Inventor 陈智杨英刘艳宁郑敏
Owner ZHEJIANG UNIV
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