Applications of celastrol

A technology of sapogenin and influenza virus, which is applied in the field of medicine and can solve problems such as no reports on the application of sapphirein to influenza virus diseases.

Active Publication Date: 2017-01-18
JIANGSU KANION PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] There is currently no report on the application of cereli in the pre...

Method used

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  • Applications of celastrol
  • Applications of celastrol
  • Applications of celastrol

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] The cytotoxicity of embodiment 1 cerelin

[0041] Method steps: MDCK cells are seeded in a 96-well cell culture plate, and the drug-containing medium is added after the cells adhere to the wall. After adding the drug and culturing, observe the cytopathic effect (CPE) caused by the drug under a light microscope, add Incubate at 37°C for 2h, detect fluorescence In the case of reduction, the excitation light is 540nm, and the emission light is 595nm.

[0042] Cell activity (%)=(sample well-blank control) / (cell control-blank control)*100%

[0043] Table 1 cerelin cytotoxicity test data

[0044]

[0045] The results are shown in Table 1, figure 1 It is the toxicity of ceheriferin to MDCK dog kidney cells in Example 1 of the present invention. Depend on figure 1 It can be seen that cerelin has no cytotoxicity to MDCK cells at 0.41 μM.

Embodiment 2

[0046] The inhibitory activity of embodiment 2 cerelin to influenza A virus

[0047] Method steps: MDCK cells were inoculated in a 96-well cell culture plate, cultured overnight at 37°C and then used for later use. After MDCK cells were washed twice with PBS, influenza virus liquid and drugs with gradient dilution concentrations were added at the same time. After cultured in a cell incubator at 37°C for 24 hours, the cytopathic changes (CPE) were observed under a microscope; the supernatant of the culture medium was taken to detect neuraminidase activity.

[0048] In the experiment, blank control wells (normal cells), virus control wells (no drug added after virus infection), and positive drug control wells (ribavirin added after infection) were set.

[0049] Inhibition rate (%)=100-(sample well-blank control) / (virus control-blank control)*100%

[0050] Table 2 The results of the inhibitory activity of ceheriferin on influenza virus strain H1N1

[0051]

[0052] Table 3 ...

Embodiment 3

[0057] Therapeutic effect of embodiment 3 shertenin gavage (oral) administration to mouse infection caused by influenza A virus

[0058] First, a preliminary experiment was performed to determine the LD50 of influenza virus A / PuertoRico / 8 / 1934 (H1N1). 80 mice were randomly divided into 4 groups, 20 in each group. They were: (1) normal control group: intragastric administration of distilled water, (2) model group: intragastric administration of distilled water, (3) positive group: intragastric administration of oseltamivir aqueous solution (20mg / kg), (4) South Shertenin group: shertenin aqueous solution (20 mg / kg) was given by intragastric administration. 4 hours before virus inoculation and 5 consecutive days after virus inoculation, once a day. After ether anesthesia, 10LD 50 Dosage Nasal inoculation of influenza virus 50 μL. Take 10 mice in each group for continuous observation for 14 days, and record the death situation of the mice (calculate the death rate and average s...

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Abstract

The present invention relates to the technical field of medicines, particularly to applications of celastrol. The invention provides applications of celastrol in preparation of influenza virus inhibitors and drugs for prevention and/or treatment of influenza virus diseases. According to the present invention, the experimental results show that the celastrol can significantly reduce the mouse death caused by influenza virus infection and prolong the average survival time of the mice, can significantly inhibit mouse lung infection caused by influenza virus infection and effectively relieve the lung infection symptoms of the mice, can treat influenza, pneumonia and other respiratory tract infection diseases caused by influenza virus, can prevent the proliferation and the spread of viruses in vivo and protect normal tissue from injury, and can prevent the occurrence of viral infectious diseases.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the application of shertenin. Background technique [0002] Influenza (abbreviated as influenza) is an acute respiratory infection caused by influenza virus, and it is also a disease with strong contagion and fast transmission speed. It is mainly spread through droplets in the air, person-to-person contact or contact with contaminated items. Typical clinical symptoms are: sudden onset of high fever, general pain, significant fatigue and mild respiratory symptoms. Generally, autumn and winter are the high-incidence period, and the complications and death caused by it are very serious. The disease is caused by influenza virus, which can be divided into three types: A (A), B (B), and C (C). Type A virus often undergoes antigenic variation, is highly contagious, spreads rapidly, and is very prone to large-scale epidemics. Type A H1N1 is a type of type A. Influenza is self-limiti...

Claims

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Application Information

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IPC IPC(8): C07J63/00A61K31/56A61P31/16
CPCA61K31/56C07J63/00
Inventor 萧伟刘文君房卉程宁波尚婵孟兆青胡玉梅杨彪黄文哲王振中胡晗绯
Owner JIANGSU KANION PHARMA CO LTD
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