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Application of sesquiterpene lactone compound in centipeda minima in preparation of drug having antiviral effect

A technology of sesquiterpene lactones and antiviral effects, applied in antiviral agents, pharmaceutical formulations, organic active ingredients, etc., can solve the problems of antiviral effects of undisclosed compounds, and achieve remarkable antiviral effects

Inactive Publication Date: 2018-11-06
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Although the Chinese invention patent CN104771393B discloses that sesquiterpene lactone compounds have anti-influenza virus effects, it does not disclose whether the above-mentioned compounds also have other anti-viral effects

Method used

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  • Application of sesquiterpene lactone compound in centipeda minima in preparation of drug having antiviral effect
  • Application of sesquiterpene lactone compound in centipeda minima in preparation of drug having antiviral effect
  • Application of sesquiterpene lactone compound in centipeda minima in preparation of drug having antiviral effect

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] The preparation of embodiment 1 sesquiterpene lactone compound

[0022] Grind 300g of dried goose-free grass, pass through a 80-mesh sieve, and place in supercritical CO 2 In the extractor, 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, and 14.8 g of supercritical carbon dioxide extract of Goose Bubivora is obtained;

[0023] Dissolve the supercritical carbon dioxide extract of Goose Bubivora in ethyl acetate, mix the sample with 12g of silica gel (100-200 mesh), and evaporate to dryness under reduced pressure to obtain the sample; take another 90g of silica gel (200-300 mesh) for dry packing Column (inner diameter × length = 3.5 × 50cm), put the sample on the column, cover with a layer of silica gel, first elute with petroleum ether, and then use petroleum ether and ethyl acetate (volume ratio: 7.5:1.5) Mixed solvent elution, collecting the mixed solvent eluted part, concentra...

Embodiment 2

[0026] Example 2 Sesquiterpene lactone anti-herpes simplex virus activity test

[0027] Using a 96-well cell culture plate, prepare 1×10 per mL 5 Cells, add 100 μL per well, place in 5% CO 2 , Incubate overnight in a cell culture incubator at 37°C. After the cells grow into a single layer, discard the growth medium and add 100TCID 50 100 μL of virus solution, after 1 hour, discard the virus solution, wash twice with PBS, dilute the sample with TPCK-Trypsin, then add 100 μL of the diluted drug to be tested in each well, and place in 5% CO 2 , Continue to culture at 37°C for 2-3 days, when the virus control cells reach the pathological changes, record the results, and calculate the IC by the Reedand Muench method 50 , the results are shown in Table 1.

[0028] The virus liquid contains herpes simplex virus type 1 (HSV-1) or herpes simplex virus type 2 (HSV-2). Among them, the experimental group 1 used arnica lactone B; the experimental group 2 used arnica lactone D; the expe...

Embodiment 3

[0032] Example 3 Sesquiterpene lactones anti-hepatitis B virus activity test

[0033] A 96-well cell culture plate was used to prepare 5×10 per mL 4 One liver cancer cell HepG22.2.15 cells transfected with HBV, add 100 μL to each well, place in 5% CO 2 , Incubate overnight in a 37°C cell culture incubator, add 100 μL of the diluted drug to be tested in each well, and place in 5% CO 2 、Continue culturing at 37°C for 9 days, detect the viral DNA in the supernatant, and calculate the IC 50 , the results are shown in Table 2.

[0034] The virus liquid contains hepatitis B virus (HBV). Among them, the experimental group 1 used arnica lactone B; the experimental group 2 used arnica lactone D; the experimental group 3 used geranidin; the experimental group 4 used arnica lactone A mixture of ester B, arnicalide D and geraniol in a mass ratio of 2:1:1; the arnicalide D and geraniin used in experimental group 5 were in a mass ratio It was a mixture of 1:1 composition; what experime...

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Abstract

The invention relates to the technical field of pharmaceutical chemistry, and concretely discloses an application of a sesquiterpene lactone compound in centipeda minima in preparation of a drug having antiviral effect. The sesquiterpene lactone compound is selected from one of arnicolide B, arnicolide D, and brevilin and a mixture of more than one of the above materials. The sesquiterpene lactonecompound has good antiviral effects for herpes simplex virus, hepatitis B virus, and human cytomegalovirus.

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry, and in particular to the application of a sesquiterpene lactone compound in goosebubivorous herbicides in the preparation of medicines with antiviral effects. Background technique [0002] Goose does not eat grass is the whole herb with flowers of Centipeda minima (L.) A.Br.et.Aschers, a plant of Compositae. There are records. In my country, geese do not eat grass and are mainly produced in Zhejiang, Jiangsu, Guangdong, Hubei and other places, and are also distributed in Guangxi, Henan, Jiangxi, Fujian, Anhui and other places. The herbal medicine was included in the 2000 and 2005 editions of the "Chinese Pharmacopoeia", which can "clear the nose and relieve cough", and is used for "wind-cold headache, cough with phlegm, stuffy nose, nasal sinus runny nose" and so on. The chemical constituents of geese not herbivorous mainly include volatile oils, terpenoids, flavonoids and sterols. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61P31/22A61P31/20A61P31/12
CPCA61K31/365A61P31/12A61P31/20A61P31/22A61K2300/00
Inventor 李药兰张晓丽王国才和君李满妹
Owner JINAN UNIVERSITY
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