Application of dabrafenib and/or its pharmaceutically acceptable derivatives in the preparation of anti-arenavirus drugs

A virus and drug technology, applied in the field of medicine, can solve the problems of limited therapeutic effect and strong side effects of anti-arenavirus drugs

Active Publication Date: 2021-04-13
CANVEST WUHAN BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to overcome the problems that existing anti-arenavirus drugs have limited therapeutic effects and strong side effects

Method used

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  • Application of dabrafenib and/or its pharmaceutically acceptable derivatives in the preparation of anti-arenavirus drugs
  • Application of dabrafenib and/or its pharmaceutically acceptable derivatives in the preparation of anti-arenavirus drugs
  • Application of dabrafenib and/or its pharmaceutically acceptable derivatives in the preparation of anti-arenavirus drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] This example studies the cytotoxicity of the target compound dabrafenib, and the specific process is as follows:

[0026] BHK-21 cells and Vero cells were divided into 1.5×10 4 Cells / well were seeded in 96-well cell culture plates at 37°C, 5% CO 2 After culturing in the incubator for 12-16 hours, replace the medium with DMEM medium containing 2% FBS, and then use dabrafenib at a concentration of 0.5 μM, 1 μM, 2 μM, 4 μM, 8 μM, 16 μM, 32 μM, 64 μM and 128 μM For treatment, add the same volume of DMSO to the negative control, set three replicate wells for each concentration, incubate at 37°C for 36 hours, and set up zero-adjustment wells with only medium and no cells. Discard the supernatant, wash once with PBS, add 50 μl of 0.5% MTT PBS solution to each well, and place it at 37°C for 4 hours in the dark, and you can observe blue-purple crystals appearing on the bottom of the plate, and stop the culture at this time. And carefully aspirate the supernatant, add 100 μl DM...

Embodiment 2

[0029] This example studies the antiviral activity of the target compound dabrafenib against arenavirus (LCMV), the specific process is as follows:

[0030] BHK-21 cells and Vero cells were divided into 1.5×10 4 Cells / well were seeded in 96-well cell culture plates at 37°C, 5% CO 2 After culturing in the incubator for 12-16 hours, replace the medium with DMEM medium containing 2% FBS, and then use dabrafenib at a concentration of 0.5 μM, 1 μM, 2 μM, 4 μM, 8 μM, 16 μM, 32 μM, 64 μM and 128 μM For treatment, the same volume of DMSO was added to the negative control, and three replicate wells were set for each concentration. After incubation for 1 h, cells were infected with LCMV. After 36h, the effect of dabrafenib inhibiting virus replication was detected by measuring the supernatant titer, and the results on the two kinds of cells were as follows: Figure 5 and Figure 6 As shown, under different concentration conditions, the compound dabrafenib has a significant inhibitor...

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Abstract

The invention provides an application of dabrafenib and / or its pharmaceutically acceptable derivatives in the preparation of anti-arenavirus drugs. The invention detects the cytotoxicity of dabrafenib on Vero cells and BHK‑21 cells and its antiviral activity against arenaviruses, indicating that dabrafenib has a strong anti-arenavirus effect at the cellular level , providing a new direction for the prevention and treatment of arenavirus infectious diseases.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to the application of dabrafenib and / or its pharmaceutically acceptable derivatives in the preparation of anti-arenavirus drugs. Background technique [0002] Mammalian arenaviruses (Mammarenavirus) belong to the Bunyavirales (Bunyavirales) arenaviridae (Arenaviridae), mainly composed of Old World and New World arenaviruses, including many virulent viruses that have important threats to humans, such as La Lassa virus (LASV), Junín virus (JUNV), Machupo virus (MACV), etc. Among them, LASV is mainly prevalent in Nigeria, Liberia, Sierra Leone, Guinea and other West African countries. Every year, 100,000 to 300,000 people are infected and about 5,000 people die. JUNV is mainly prevalent in the Pampa region of Argentina, causing Argentine hemorrhagic fever with a fatality rate of 15%-30%. In addition, Lymphocyticchoriomeningitis virus (LCMV) exists in my country, mainly i...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/506A61P31/14
CPCA61K31/506A61P31/14
Inventor 徐国东刘愈杰幸晓莹
Owner CANVEST WUHAN BIOTECH
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