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Application of 1,3-dihydroxy-6-benzo[c]chromenone in the preparation of anti-influenza virus drugs

An anti-influenza virus, influenza virus technology, applied in the field of medicine, can solve the problems that the application of anti-influenza virus has not been reported.

Active Publication Date: 2020-05-22
SOUTHERN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] 1,3-Dihydroxy-6-benzo[C]chromenone, referred to as compound J2, has no report on the application of anti-influenza virus

Method used

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  • Application of 1,3-dihydroxy-6-benzo[c]chromenone in the preparation of anti-influenza virus drugs
  • Application of 1,3-dihydroxy-6-benzo[c]chromenone in the preparation of anti-influenza virus drugs
  • Application of 1,3-dihydroxy-6-benzo[c]chromenone in the preparation of anti-influenza virus drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Cytotoxicity Detection of Example 1 Compound J2

[0029] The cytotoxicity of compound J2 was detected by MTT method. The specific method is as follows:

[0030] MDCK or A549 cells by 1×10 4 / well seeded in 96-well plate at 37°C, 5% CO 2 Cultured in a constant temperature cell incubator until monolayer, DMEM or 1640 serially diluted compound J2 was added to a 96-well plate, 200 μl per well, and cultured for 48 hours. Discard the culture supernatant, add 100 μL of 1640 or DMEM medium containing 0.5 mg / ml MTT to each well, and incubate at 37°C for 4 hours. The absorbance at 570 nm was detected with a multifunctional microplate reader (Genios Pro, Tecan, US). The survival rate of the cells was used as an indicator of the toxicity of compound J2 to MDCK or A549 cells.

[0031] Cell viability (%)=E / N×100

[0032] E is the absorbance of the drug group, and N is the absorbance of the cell control group.

[0033] Test results: Compound J2 has low cytotoxicity and high bio...

Embodiment 2

[0035] Example 2 Anti-influenza A virus activity detection of compound J2 in vitro

[0036] In the in vitro antiviral experiment of the present invention, various subtypes of influenza A viruses are involved, including H1N1 and H3N2, and the specific methods are as follows:

[0037] MDCK cells by 2 x 10 4 / well seeded in 96-well plate at 37°C, 5% CO 2 cultured to a monolayer in a constant temperature cell incubator. Use 100TCID 50 Cells were infected with influenza A virus, 100 μl per well, incubated at 37°C for 1 h, discarded the virus solution, and added compound J2 serially diluted in DMEM (containing 1 μg / ml TPCK), 200 μl per well, and continued to incubate for 48 h. Combined with MTT assay and plaque assay, the antiviral activity of compound J2 was detected. The protective effect of compound J2 on cells was evaluated by observing the cytotoxic phenomenon (CPE) caused by the virus and detecting the survival rate of the cells by observing compound J2, and further calcul...

Embodiment 3

[0043] Example 3 Compound J2 Inhibitory Experiment on Replication of Influenza A Virus

[0044] In order to evaluate the inhibitory effect of compound J2 on influenza virus replication, the present invention uses three methods of indirect immunofluorescence, Q-PCR and Western blotting to detect the effect of compound J2 on virus replication from the expression levels of genes and proteins. The specific method is as follows:

[0045] MDCK cells by 2 x 10 4 / well seeded in a 6-well plate at 37 °C, 5% CO 2 cultured to a monolayer in a constant temperature cell incubator. Use 100TCID 50 Infected cells with influenza A virus, 1ml per well, incubated at 37°C for 1h, discarded the virus solution, added compound J2 serially diluted in DMEM (containing 1μg / ml TPCK), 2ml per well, and continued to incubate for 24h. Thereafter, NP protein and cell nuclei were stained with 4% paraformaldehyde for 20 minutes, and 3 visual fields were randomly selected to take pictures of the expression...

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Abstract

The invention discloses application of 1, 3-dyhydroxy-6-benzo[C]chromone to preparing anti-influenza virus drugs. Influenza viruses are influenza A viruses, preferably, H1N1, H3N2, H5N1, H7N1, H7N2, H7N3, H7N7, H7N9, H9N2 or H10N8; the mechanism of action of the 1, 3-dyhydroxy-6-benzo[C]chromone comprises binding with PB2cap protein to inhibit activity of vRNP (virus ribonucleoprotein complexes) to prepare drugs for preventing and treating influenza; the binding loci between the 1, 3-dyhydroxy-6-benzo[C]chromone and the PB2cap protein of the influenza viruses are His357 (histidine 357), Phe404(phenylalanine 404), Phe323, Glu361 (glutamic acid 361), Lys376 (lysine 376), Phe363 and Asn429 (asparagine 429).

Description

technical field [0001] The invention relates to the application of 1,3-dihydroxy-6-benzo[C]chromenone in anti-influenza virus drugs, and belongs to the technical field of medicine. Background technique [0002] Influenza viruses belong to the single-stranded negative-sense RNA virus of the Orthomyxoviridae family and are divided into three subtypes: A (A), B (B) and C (C). Recently, the outbreak of highly pathogenic H5N1 avian influenza has posed a serious threat to both humans and animals, with a fatality rate as high as 60%. In 2013, China reported a new subtype of recombinant avian influenza virus that continues to threaten human life. In addition, other recombinant avian influenza viruses have emerged over the past two years, pointing to the unpredictability we face in preventing influenza virus infection in the future. Currently, effective therapeutic drugs against influenza infection are still insufficient due to antiviral drug resistance and vaccine escape, especial...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/37A61P31/16
CPCA61K31/37
Inventor 杨洁刘叔文田园新刘腾陈飞敏陈芳昭
Owner SOUTHERN MEDICAL UNIVERSITY
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