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Application of GS-441524 in preparation of novel coronavirus SARS-CoV-2 inhibitor

A technology of GS-441524, 1. GS-441524, which is applied in the field of preparing new coronavirus SARS-CoV-2 inhibitors, can solve the problems of no vaccine and the new coronavirus is in the initial stage of exploration, and achieve less toxic side effects and safety sex high effect

Inactive Publication Date: 2020-05-12
HUAZHONG AGRI UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since the outbreak of the epidemic, research on the infectious disease has mainly focused on epidemiological investigations, sequence comparison and analysis of clinically isolated strains, virus detection methods, etc. Research on the invasion, replication, and immune regulation mechanisms of new coronaviruses Research on antiviral drugs for SARS-CoV-2 is of great importance as it is still in the early stages of exploration and no vaccine can provide sufficient protection

Method used

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  • Application of GS-441524 in preparation of novel coronavirus SARS-CoV-2 inhibitor
  • Application of GS-441524 in preparation of novel coronavirus SARS-CoV-2 inhibitor
  • Application of GS-441524 in preparation of novel coronavirus SARS-CoV-2 inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Example 1 Toxicity test of GS-441524 to cells

[0017] experiment method:

[0018] 1) Take Vero-E6 cells in good growth state for digestion and passage, and adjust the cell density to 1×10 with cell growth medium. 5 / mL to inoculate a 96-well plate, 100 μL / well, placed at 37°C, 5% CO 2 Cultivate in an incubator for 16 hours;

[0019] 2) After 16 hours, discard the medium in the well, wash with 1×PBS three times, dry it, add cell maintenance solution, and add GS-441524 at the same time, so that the final concentration of GS-441524 is 10000 μM, 1000 μM, 500 μM, 100 μM, 50 μM, 25 μM , 12.5μM, 6.25μM, and set the cell control at the same time, placed at 37 ° C, 5% CO 2 incubator cultivation;

[0020] 3) After 72h, use Reagents for cell viability assays.

[0021] test results:

[0022] see results figure 1 . Determination of cell viability can reflect the toxic effect of GS-441524 on Vero-E6 cells. As can be seen from the figure, GS-441524 has less toxic effect on ...

Embodiment 2

[0023] Example 2 The inhibitory effect of GS-441524 on the virus at the cellular level

[0024] experiment method:

[0025] 1) Take Vero-E6 cells in good growth state for digestion and passage, and adjust the cell density to 1×10 5 / mL inoculated in a 96-well plate, 100 μL / well, placed at 37°C, 5% CO 2 Cultivate in an incubator for 16 hours;

[0026] 2) After 16 hours, the medium in the well was discarded, washed three times with 1×PBS, and after drying, 100 μL of GS-441524 with a concentration of 100 μM was added to each well, and 100 μL of 0.01 MOI of SARS-CoV-2 virus was added to each well to make GS- The final concentration of 441524 was 50 μM. Set up cell control and virus control at the same time, place at 37°C, 5% CO 2 incubator cultivation;

[0027] 3) After 48 hours of inoculation, observe the changes in the cell state after the compound and the virus interact with a microscope and take pictures for preservation.

[0028] test results:

[0029] see results fi...

Embodiment 3

[0030] Embodiment 3 GS-441524 antiviral activity (EC 50 )test

[0031] experiment method:

[0032] 1) Take Vero-E6 cells in good growth state for digestion and passage, and adjust the cell density to 1×10 with cell growth medium. 5 / mL inoculated in a 96-well plate, 100 μL / well, placed at 37°C, 5% CO 2 Cultivate in an incubator for 16 hours;

[0033] 2) After 16 hours, dilute GS-441524 with cell maintenance solution so that the concentrations are 200 μM, 100 μM, 50 μM, 25 μM, 12.5 μM, 6.25 μM, 3.125 μM, 1.5625 μM;

[0034] 3) Mark on the lid of the 96-well plate, discard the medium in the well, wash three times with 1×PBS, dry it, add 100 μL of diluted GS-441524 to each well in the order of marking, and add 100 μL of 0.01MOI virus to each well solution, so that the final concentration of GS-441524 is 100 μM, 50 μM, 25 μM, 12.5 μM, 6.25 μM, 3.125 μM, 1.5625 μM, 0.78125 μM, set the cell control group and the virus control group, and place them at 37 ° C, 5% CO 2 incubator c...

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PUM

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Abstract

The invention discloses the application of GS-441524 in the preparation of a novel coronavirus SARS-CoV-2 inhibitor. In-vitro cell test results show that the GS-441524 can significantly inhibit the infection of normal cells by SARS-CoV-2, has an inhibition effect on the novel coronavirus SARS-CoV-2 at a cellular level, can significantly reduce the virus titer of the novel coronavirus in cells andinhibit the proliferation of the novel coronavirus in cells, and has dose dependence. Therefore, the GS-441524 can be used as a novel coronavirus SARS-CoV-2 inhibitor, and has the potential of treating COVID-19 pneumonia of human beings caused by infection with the coronavirus or other diseases of animals caused by infection with the coronavirus.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to the new application of GS-441524 in preparing novel coronavirus SARS-CoV-2 inhibitors. Background technique [0002] Corona Virus Disease 2019 (COVID-19), referred to as "New Coronary Pneumonia", is a disease caused by the new coronavirus SARS-CoV-2, characterized by fever, dry cough, fatigue and a certain lethality. Contact infectious diseases. [0003] Since the outbreak of COVID-19 in December 2019, the number of confirmed cases of infection has surpassed that of SARS, and the number of deaths has continued to increase, causing serious social harm and economic losses. public health event". Since the outbreak of the epidemic, research on the infectious disease has mainly focused on epidemiological investigations, sequence comparison and analysis of clinically isolated strains, virus detection methods, etc. Research on the invasion, replication, and immune regulation mechan...

Claims

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Application Information

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IPC IPC(8): A61K31/706A61P11/00A61P31/14
CPCA61K31/706A61P11/00A61P31/14
Inventor 彭贵青刘紫微陈西田大勇
Owner HUAZHONG AGRI UNIV
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