Application of PI3K inhibitor NVP-BYL719 for preparing COVID-19 (Corona Virus Disease 2019) inhibitor

A BLY719, coronavirus technology, used in antiviral agents, respiratory diseases, urinary system diseases, etc., can solve the problem of the unreported PI3K inhibitor NVP-BYL719 on the virus inhibition, etc., to reduce virus drug resistance, reduce Drug toxicity and side effects, good curative effect

Inactive Publication Date: 2020-10-16
王思慧
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, no PI3K inhibitor NVP-BYL719 has been reported t

Method used

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  • Application of PI3K inhibitor NVP-BYL719 for preparing COVID-19 (Corona Virus Disease 2019) inhibitor
  • Application of PI3K inhibitor NVP-BYL719 for preparing COVID-19 (Corona Virus Disease 2019) inhibitor
  • Application of PI3K inhibitor NVP-BYL719 for preparing COVID-19 (Corona Virus Disease 2019) inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1 Toxicity test of NVP-BLY719 to cells

[0024] (1) Take well-grown Vero-E6 cells for digestion and passage, and adjust the cell density to 1×10 in cell culture medium (DMEM with 10% FBS). 5 / mL, inoculate a 96-well plate, 100 μL / well, place at 37°C, 5% CO 2 Cultivate in an incubator for 12 hours;

[0025] (2) After 12 hours, discard the medium, wash with PBS three times, dry it, add cell maintenance solution (2% FBS in DMEM), and add BLY719 at the same time (molar ratio is 1:1), so that the final concentration of the drug is 8000μM, 800μM , 400μM, 200μM, 100μM, 50μM, 25μM, 12.5μM, and set the cell control at the same time, placed in 37 ℃, 5% CO 2 incubator cultivation;

[0026] (3) After 72 hours, cell viability was detected with CellTiter-Glo reagent.

[0027] see results figure 1 . The cell survival rate can reflect the toxic effect of BLY719 on Vero-E6 cells. It can be seen from the figure that the toxic effect of NVP-BLY719 on Vero-E6 cells is small, ...

Embodiment 2

[0028] Example 2 The inhibitory effect of BLY719 on the virus at the cellular level

[0029] (1) Take well-grown Vero-E6 cells for digestion and passage, and adjust the cell density to 1×10 with cell maintenance solution. 5 / mL to inoculate a 96-well plate, 100 μL / well, placed at 37°C, 5% CO 2 Cultivate in an incubator for 12 hours;

[0030] (2) After 12 hours, the medium was discarded, washed three times with PBS, and after drying, 100 μL of NVP-BLY719 with a concentration of 100 μM was added to each well, and then 100 μL of 0.01 MOI of SARS-CoV-2 (SARS-CoV-2 / WH- 09 / human / 2020 / CHN) virus, the final concentration of BLY719 was 50 μM. Set up cell control and virus control at the same time, place at 37°C, 5% CO 2 incubator cultivation;

[0031](3) After 48 hours of inoculation, observe the cell state changes after BLY719 interacts with the virus with a microscope and take pictures for preservation.

[0032] see results figure 2 . From the microscope pictures, it can be o...

Embodiment 3

[0033] Embodiment 3 BLY719 antiviral activity (EC 50 )test

[0034] (1) Take well-grown Vero-E6 cells for digestion and passage, and adjust the cell density to 1×10 with cell culture medium. 5 / mL to inoculate a 96-well plate, 100 μL / well, placed at 37°C, 5% CO 2 Cultivate in an incubator for 12 hours;

[0035] (2) After 12 hours, dilute NVP-BLY719 with cell maintenance solution at a molar ratio of 1:1 to make the concentration 200 μM, 100 μM, 50 μM, 25 μM, 12.5 μM, 6.25 μM, 3.125 μM, 1.5625 μM;

[0036] (3) Make a mark on the cover of the 96-well plate, discard the medium in the well, wash with PBS three times, dry it, add 100 μL of diluted NVP-BLY719 to each well in the order of marking, and then add 100 μL of 0.01 MOI virus solution to each well , so that the final concentration of BLY719 was 100 μM, 50 μM, 25 μM, 12.5 μM, 6.25 μM, 3.125 μM, 1.5625 μM, 0.78125 μM; 2 incubator cultivation;

[0037] (4) After 72 hours, cell viability was detected with CellTiter-Glo reage...

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PUM

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Abstract

The invention belongs to the technical field of medicine preparation, and particularly relates to application of a PI3K inhibitor NVP-BYL719 for preparing a COVID-19 inhibitor. An in vitro cell test result indicates that the medicine can inhibit the proliferation of the COVID-19 in cells. Meanwhile, a mouse challenge test result indicates that the medicine can effectively lower the lung viral loadof an infected mouse, has an obvious treatment function for the infected mouse, can be used as the COVID-19 inhibitor and is used for treating the COVID-19 pneumonia.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, and in particular relates to the application of a PI3K inhibitor NVP-BYL719 in the preparation of novel coronavirus SARS-CoV-2 inhibitors. Background technique [0002] Corona Virus Disease 2019 (COVID-19), referred to as "New Coronary Pneumonia", is a type of acute infectious disease caused by 2019 novel coronavirus (2019-nCoV) infection. After a person is infected with the new coronavirus, the main symptoms include respiratory symptoms, fever, cough, shortness of breath, and dyspnea. In more severe cases, the infection can lead to pneumonia, severe acute respiratory syndrome, kidney failure, and even death. 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". [0003] Since the outbreak of the epidemic, r...

Claims

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Application Information

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IPC IPC(8): A61K31/4439A61P31/14A61P11/00A61P13/12
CPCA61K31/4439A61P31/14A61P11/00A61P13/12
Inventor 王思慧
Owner 王思慧
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