Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Application of carbinoxamine maleate in preparation of anti-influenza virus medicine

A technology for carboximin maleate and anti-influenza virus, applied in the field of medicine, can solve problems such as restricted use and not widely used, and achieve the effect of solving drug resistance and broad-spectrum antiviral activity

Active Publication Date: 2021-09-24
FUDAN UNIV
View PDF5 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, continuous evolution and rapid drug resistance of influenza A viruses, especially to amantadine and oseltamivir, limit the use of these two classes of drugs
Favipiravir is an RNA-dependent RNA polymerase inhibitor. It is a broad-spectrum antiviral drug. It is currently only listed in Japan as an anti-influenza virus drug and has not been widely used.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Application of carbinoxamine maleate in preparation of anti-influenza virus medicine
  • Application of carbinoxamine maleate in preparation of anti-influenza virus medicine
  • Application of carbinoxamine maleate in preparation of anti-influenza virus medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] CAM activity in vitro Compound Example 1 in the embodiment of anti-influenza virus

[0032] In vitro experiments The present invention relates to antiviral multiple subtypes of influenza A and B viruses, including A / Shanghai / 37T / 2009 (H1N1), A / Puerto Rico / 8 / 1934 (H1N1), A / Guizhou / 54 / 1989 (H3N2) and B / Shanghai / 2017 (BY), specifically as follows:

[0033] MDCK cells were 2 × 10 4 / Well in 96 well plates at 37 ℃, 5% CO 2Thermostat incubator to cell monolayers. Compound was added to each well and 50 l of serial dilutions of 50μl 100TCID 50 After influenza virus infected cells were mixed, incubated 8h 37 ℃. Discarded mixture was added DMEM (containing 2μg / ml TPCK) Blank 200 l of medium per well, cultured for 48h. By CCK-8 binding was determined by the antiviral activity of the compounds of the protective effect of the compound on the cell, and further calculate the median effective concentration IC 50 ;

[0034] The results indicate that the compounds can ...

Embodiment 2

[0037] Example 2 Toxicity Test compound cell embodiment of the CAM

[0038] Compound CAM using CCK-8 method Cytotoxicity; in particular as follows:

[0039] MDCK cells were 1 × 10 4 / Well in 96 well plates at 37 ℃, 5% CO 2 Thermostat incubator to cell monolayers, the serial dilutions were added to DMEM CAM 96-well plate, 100 l per well, cultured for 72h, added to each well containing 20μL CCK-8 solution is incubated for 1h 37 ℃, utilizes a versatile microplate reader (Ultra 384, Tecan, NC) detection of absorbance at 450nm, to CAM cell viability as indicators of toxicity of MDCK cells; test showed small CAM cytotoxic compounds, high security, such as figure 2 , The toxicity of the compound CAM cells is small, in the concentration range 250μM little toxicity to MDCK cells which half toxic concentration (CC 50 ) Was 240.52 ± 12.53μM ( image 3 ); The highest drug testing in the present study within the selected concentration 200μM, a safe non-toxic in the concentration range.

Embodiment 3

[0040] Example 3 Activity of compounds against influenza virus in vivo CAM embodiment

[0041] The present invention is further evaluated in vivo inhibitory activity against influenza virus CAM, 4 to 8 weeks of using C57BL / 6 female mice were infected with the H7N9 influenza virus CAM 1h intervention, the detection of infection the survival rate after 14 days, as follows:

[0042] 10LD50 using influenza A virus A / Shanghai / 4664T / 2013 (H7N9) 4 to 8 weeks of age were inoculated C57BL / 6 female mice. IH after infection, respectively, a high dose (10mg / kg / day) and low dose (1mg / kg / day) intraperitoneal injection of the CAM, continuous intervention 5 days to neuraminidase inhibitor oseltamivir phosphate (or OSEs ) (1mg / kg / day) as a positive control, PBS as a negative control group, after infection with influenza virus calculated 2,4,6,8,10,12 and 14 days survival of mice; test results show that compounds of the CAM mice infected with influenza virus has a protective e...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention belongs to the technical field of medicine and relates to the application of carbinoxamine maleate in the preparation of anti-influenza A virus medicine. Experiments have shown that the carbinoxamine maleate has significant anti-influenza activity to different types and subtypes of influenza viruses at a completely non-toxic concentration, and inhibits the replication of all detected virus strains in a dose-dependent manner, indicating that Carbinoxamine maleate has a certain broad-spectrum anti-influenza virus activity, and the influenza virus described in the present invention includes influenza A and influenza B viruses, including H1N1, H3N2, H7N9, H5N1, H7N1, H7N2, H7N3, H7N7, H9N2 Or type B; the mechanism of action research of the present invention shows that carbinoxamine maleate mainly inhibits the virus from entering host cells by interfering with the endocytosis of influenza virus; described carbinoxamine maleate can be prepared for the prevention and treatment of influenza medicine , to provide new ways and means for the prevention and treatment of influenza.

Description

Technical field [0001] The present invention belongs to the field of medical technology, carbinoxamine maleate for the preparation of anti-influenza virus drugs directed. Background technique [0002] The prior art discloses influenza virus can cause acute respiratory infectious diseases with high incidence and high mortality, significant threat to human health. Influenza viruses belong to the Orthomyxoviridae family of single-stranded negative-strand RNA viruses, their host and the virulence of different types can be divided into A (A), B (B), propionate (C), D (D) four types ; where the influenza a virus (IAV) of the widest host range, pathogenicity of the strongest, while the study found that some strains of influenza B viruses can cause human infections, there are around 5 million people die from seasonal flu each year the outbreak. Although the majority of influenza virus infection is self-limiting, but they may sometimes induce severe and even fatal diseases, such as pneumo...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4402A61P31/16
CPCA61K31/4402A61P31/16
Inventor 陆路姜世勃徐巍刘腾王茜花晨王聪付玉红李佩玉
Owner FUDAN UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com