Application of compound PS-341 in preparation of inhibitor of enterovirus of picornaviridae

A PS-341, RNA virus technology, applied in antiviral agents, medical preparations containing active ingredients, organic active ingredients, etc.

Inactive Publication Date: 2019-03-08
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it has not been reported whether the compound PS-341 can inhibit the replication of Enteroviruses of the family Picornaviridae.

Method used

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  • Application of compound PS-341 in preparation of inhibitor of enterovirus of picornaviridae
  • Application of compound PS-341 in preparation of inhibitor of enterovirus of picornaviridae
  • Application of compound PS-341 in preparation of inhibitor of enterovirus of picornaviridae

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] The application of compound PS-341 in the preparation of Picornaviridae Enterovirus genus virus inhibitors, said compound PS-341 has a structure shown in formula (I):

[0022]

[0023] The Enteroviruses of the family Picornaviridae are EV D68 virus and CV A16 virus.

Embodiment 2

[0024] Example 2. The effect of PS-341 on the viability of Hela cells and RD cells.

[0025] Prepare RD cells and Hela cells in a 96-well plate, adjust the concentration of the cell suspension, and divide into 96-well plates, 3000-10000 cells / well. The cell growth density is moderate, and the PS-341 drug concentration gradient is set to 0nM, 6.25nM, 12.5nM, 25nM, 50nM, 100nM, 200nM, 400nM. Each group is set with a drug control and a cell control. The drug control group is DMSO with a concentration of 1%. , the cell control group was not treated, and each group had 3 replicate wells. The cell viability of each treatment group was detected by the MTT cell viability assay method.

[0026] virus culture

[0027] Rhabdomyosarcoma cells (RD), which are susceptible to enterovirus D68, were selected as the inoculation objects. Inoculate RD cells in T75 culture flasks, when the cell density is 80%-90%, remove the cell culture medium, add DMEM, take an appropriate amount of virus sto...

Embodiment 3

[0048] Example 3. Effects of different concentrations of PS-341 on the replication of enterovirus EV D68.

[0049] This experiment was carried out in RD cells and Hela cells.

[0050] The specific implementation steps of cell recovery are the same as in Example 2.

[0051] cell culture

[0052] 1) Culture of RD cells

[0053] RD cells were cultured in DMEM liquid medium containing 10% FBS, 1% penicillin-streptomycin, and incubated in an incubator containing 5% CO2 at 37°C. After about 48 hours, digest with trypsin containing 0.25% EDTA. After about 3-5 minutes, add fresh medium with 10% FBS to terminate. Centrifuge at room temperature at 800 rpm for 5 minutes. Discard the supernatant. Take an appropriate amount of fresh medium to resuspend. One part was placed in a culture bottle to continue culturing, and the rest was transferred to a 96-well cell culture plate.

[0054] 2) Culture of HeLa cells

[0055] HeLa cells were cultured in DMEM liquid medium containing 10% FBS a...

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PUM

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Abstract

The invention discloses application of a compound PS-341 in preparation of an inhibitor of an enterovirus of picornaviridae. The structure of the compound PS-341 is shown as the formula (I). The enterovirus of the picornaviridae comprises a virus EV D68 and a virus CV A16. An experiment shows that the compound PS-341 has a function of inhibiting replication of the enteroviruses EV D68and CV A16, and an effective scheme is provided for preventing and treating the enteroviruses EV D68 and CV A16.

Description

technical field [0001] The present invention relates to a new application of compound PS-341, in particular to the application of compound PS-341 in the preparation of Picornaviridae Enterovirus inhibitors. Background technique [0002] Enteroviruses (Enterovirus, Picornaviridae, Enterovirus genus) are non-enveloped single-stranded positive-sense RNA viruses, which are common human pathogens and can cause from mild fever to fatal meningitis and viral encephalitis. A wide range of clinical symptoms. The VP1 gene, the gene encoding the VP1 protein, one of the four capsid proteins, is widely used to distinguish enteroviruses of different serotypes. It is now recognized that there are four types of enteroviruses: A, B, C, and D. [0003] Human Enterovirus D68 (EV D68), one of five serotypes (D70, D94, D111, D68, D120) of EV group D virus, was first identified in 1962 by four children in California isolated from throat swabs of patients with systemic diseases. Unlike other en...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4965A61P31/14
CPCA61K31/4965A61P31/14
Inventor 王志云张可可刘思华王涛
Owner TIANJIN UNIV
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