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Application of two nitrogen-containing heterocyclic ester compounds to preparation of drugs with resistance to enterovirus 71

A technology of ester compounds and enteroviruses, applied in antiviral agents, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve the problems of biological activity evaluation, etc., and achieve low price, easy purchase, and easy The effect of mass production promotion

Active Publication Date: 2017-06-13
HUBEI UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Its biological activity has not been evaluated

Method used

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  • Application of two nitrogen-containing heterocyclic ester compounds to preparation of drugs with resistance to enterovirus 71
  • Application of two nitrogen-containing heterocyclic ester compounds to preparation of drugs with resistance to enterovirus 71
  • Application of two nitrogen-containing heterocyclic ester compounds to preparation of drugs with resistance to enterovirus 71

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] [Example 1] Evaluation of the anti-EV71 activity of two nitrogen-containing heterocyclic ester compounds

[0021] 1. Test method:

[0022] 1.1 Toxicity of compounds to host RD cells

[0023] Plate RD cells into 96-well plates at 37 °C, 5% CO 2 After the monolayer was grown in the incubator, the cell culture solution was discarded, and the cell maintenance solution containing different concentrations of the test compound was added to continue the culture. After 48 hours, the cytotoxicity was visually observed under the microscope and recorded respectively, and the cell survival rate was determined by the MTT method. SPSS 11.5 software calculates the median toxic concentration (Medencyctoxic concentration, CC50) of the drug on the cells. Cell viability=(average OD of drug group 492 Value / average OD of cell control group 492 value) × 100%.

[0024] 1.2 Inhibitory activity of compounds against EV71

[0025] Plate RD cells into 96-well plates at 37 °C, 5% CO 2 After t...

Embodiment 2

[0034] [Example 2] Inhibitory effect of WY209 and WY210 on RD cell apoptosis caused by EV71

[0035] 1. Test method

[0036] The RD cells in the logarithmic growth phase were plated on 24-well plates, and the cells were infected with 100TCID50EV71 after the monolayer was overgrown. After incubation at 37°C for 1.5h, the virus solution was removed, and the cell maintenance solution containing 40μg / mL WY209 and WY210 was added. After about 48 hours, the cells were collected, and the apoptosis was detected on a flow cytometer using the Annexin V-FITC / PI apoptosis detection kit.

[0037] 2. Test results

[0038] Experimental results such as image 3 It shows that 40μg / mL WY209 and WY210 can effectively inhibit the apoptosis caused by EV71. In the virus control group, the apoptosis rate was 85.96% ( image 3 -b), under the condition of normal untreated cell apoptosis rate of 0.83% ( image 3 -a), the apoptosis rates of 40μg / mL WY209 and WY210 were 19.17% and 11.84% respectivel...

Embodiment 3

[0039] [Example 3] The inhibitory effect of WY210 on the production of EV71 progeny virus

[0040] 1. Test method

[0041] RD cells in the logarithmic growth phase were plated in 24-well plates, and 100TCID after the monolayer was overgrown 50 EV71 infected cells, incubated at 37°C for 1.5h, removed the virus solution, washed three times with PBS, and added cell maintenance solution containing 40μg / mL WY210. After 48 hours, the cells and supernatant were collected and lysed by freezing and thawing three times at -20°C and 37°C. TCID 50 Methods The titer of EV71 virus was determined.

[0042] 2. Test results

[0043] Such as Figure 4 As shown, compared with the virus control group, the virus titer of RD cells treated with WY210 decreased significantly, indicating that the compound has a strong inhibitory effect on the production of EV71 progeny virus.

[0044]In summary, the ester compounds WY209 and WY210 with novel structures have strong inhibitory activity against EV71...

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Abstract

The invention belongs to the field of antiviral drugs and provides application of two nitrogen-containing heterocyclic ester compounds to preparation of drugs with resistance to enterovirus 71 (EV71). The nitrogen-containing heterocyclic ester compounds are compounds expressed as formulas WY209 and WY210. Through research experiment of inhibition of novel nitrogen-containing heterocyclic ester compounds on activity of EV71, WY209 and WY210 can inhibit cytopathic effect (CPE) generated by EV71 in host cells RD; the cell survival rate is increased; the progeny virus yield is reduced; the apoptosis of the host cells caused by infection of EV71 can be inhibited; the application shows that the nitrogen-containing heterocyclic ester compounds have potentials for preparing the drugs with resistance to the EV71 virus; the synthesis process of the compounds is simple, economical and rapid; the large-scale production of the compounds is easy to implement; the compounds have clinical application prospects.

Description

technical field [0001] The invention belongs to the field of antiviral drugs, and in particular relates to the application of two nitrogen-containing heterocyclic ester compounds in the preparation of anti-enterovirus type 71 drugs. Background technique [0002] Enterovirus 71 (EV71) is a member of the genus Enterovirus in the Picornaviridae family, and is one of the most important pathogens causing hand, foot and mouth disease in infants, sometimes accompanied by severe central nervous system complications. Including aseptic meningitis, encephalitis, poliomyelitis-like paralysis, nervous cardiopulmonary failure, etc., and even death. Since the first report in 1974, EV71 infectious disease has broken out and spread many times around the world, especially in the Asia-Pacific region, especially in my country. In view of the great harm that the spread of hand, foot and mouth disease has brought to the lives and health of our people, the Chinese government has listed hand, foot...

Claims

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Application Information

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IPC IPC(8): A61K31/4402A61P31/14
CPCA61K31/4402
Inventor 魏艳红奚彩丽杨楠李栋张谦胡康洪尧晨光
Owner HUBEI UNIV OF TECH
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