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Application of sesquiterpene lactone compounds in preparation of anti-influenza virus drugs

An ester compound, anti-influenza virus technology, applied in the field of medicine, to achieve the effect of good anti-influenza virus activity, easy to obtain raw materials, and simple preparation method

Inactive Publication Date: 2015-07-15
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, most influenza viruses are now resistant to amantadine and oseltamivir drugs

Method used

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  • Application of sesquiterpene lactone compounds in preparation of anti-influenza virus drugs
  • Application of sesquiterpene lactone compounds in preparation of anti-influenza virus drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Crush 300g of dry whole goose grass, pass through an 80 mesh sieve, and place it in supercritical CO 2 In the extraction instrument, the extraction pressure is 20 MPa, the extraction temperature is 30 °C, the flow rate is 15 liters / hour, and the extraction time is 2 hours, to obtain 14.8 g of supercritical carbon dioxide extract of the non-grass;

[0020] After dissolving the supercritical carbon dioxide extract of Fructus vulgaris in ethyl acetate, mix the sample with 12g silica gel (100-200 mesh), and evaporate to dryness under reduced pressure to obtain the sample; take another 90g silica gel (200-300 mesh) dry pack Column (inner diameter×length=3.5×50cm), put the sample on the column, and then cover it with a layer of silica gel, first eluting with petroleum ether, and then with petroleum ether and ethyl acetate (volume ratio 7.5:1.5) Mixed solvent elution, collect mixed solvent elution parts and concentrate and dry to obtain 2.4 g of mixed solvent elution parts;

[0021...

Embodiment 2

[0023] Example 2 Test of anti-influenza A virus activity of sesquiterpene lactones

[0024] Take a 96-well cell culture plate covered with a single layer of MDCK cells, discard the supernatant, wash twice with PBS, and add 100TCID 50 100 μL / well of virus solution was adsorbed for 1 h, and then 100 μL of medicinal solution diluted with MEM was added to each well. Cell control group, virus control group, and blank control group were set up. Ribavirin was used as the positive control drug. Place at 37℃, saturated humidity, 5% CO 2 Incubate in an incubator. After 48 hours, the old solution in the 96-well plate was aspirated and discarded, and the original CCK8 solution was diluted ten times and added to the tested well at 100 μL per well. After incubating for 1 h in the incubator, measure the absorbance at 450 nm with a microplate reader. IC 50 The calculation method is as follows: cell survival rate = (dosing hole OD value-virus control OD value) / (cell control OD value-virus cont...

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PUM

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Abstract

The invention belongs to the field of medicines, and specifically discloses applications of sesquiterpene lactone compounds in the preparation of anti-influenza virus drugs. The anti-influenza virus drugs contain sesquiterpene lactone compounds with an effective dose and pharmaceutically-acceptable carriers. The invention finds that sesquiterpene lactone compounds have an anti-influenza virus effect, and novel compounds are provided for the preparation of anti-influenza virus drugs. The provided sesquiterpene lactone compounds have a very good anti-influenza virus activity, and the experiment results show that the anti-influenza virus IC50 value of the sesquiterpene lactone compounds is smaller than that of a positive reference drug ribavirin.

Description

Technical field [0001] The invention relates to the field of medicine, in particular to the application of sesquiterpene lactone compounds in the preparation of anti-influenza virus drugs. Background technique [0002] Influenza viruses are a major threat to human health. Respiratory diseases caused by influenza viruses are called influenza (flu), which has the characteristics of wide spread, strong contagion, and high incidence. According to statistics, there are 600-1.2 billion influenza cases worldwide each year, of which there are 3-5 million cases of severe influenza and 250,000-500,000 deaths. The case fatality rate of severe influenza can reach 10%. [0003] Due to the variation of influenza virus antigens, conventional vaccines cannot effectively prevent influenza outbreaks and epidemics. Therefore, the research of anti-influenza virus drugs is of great significance in influenza treatment. The anti-influenza drugs currently on the market can be roughly divided into two ca...

Claims

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Application Information

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IPC IPC(8): A61K31/365C07D307/93A61P31/16
Inventor 王国才张晓丽张玉波李国强
Owner JINAN UNIVERSITY
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