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

An arenavirus and clofazimine technology, applied in the field of medicine, can solve the problems of limited therapeutic effect of anti-arenavirus drugs, strong side effects and the like

Active Publication Date: 2021-07-30
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 clofazimine and/or its pharmaceutically acceptable derivatives in the preparation of anti-arenavirus drugs
  • Application of clofazimine and/or its pharmaceutically acceptable derivatives in the preparation of anti-arenavirus drugs
  • Application of clofazimine and/or its pharmaceutically acceptable derivatives in the preparation of anti-arenavirus drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

[0026] BHK-21 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 clofazil at concentrations of 0.25 μM, 0.5 μM, 1 μM, 2 μM, 4 μM, 8 μM, 16 μM, 32 μM and 64 μM Add the same volume of DMSO to the negative control, set up three replicate wells for each concentration, and incubate at 37°C for 36 hours. At the same time, it is necessary to 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 in 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. Carefully suck off the supernatant, add 100 μl DMSO to each well...

Embodiment 2

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

[0030] BHK-21 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 clofazil at concentrations of 0.25 μM, 0.5 μM, 1 μM, 2 μM, 4 μM, 8 μM, 16 μM, 32 μM and 64 μM The same volume of DMSO was added to the negative control, and three replicate wells were set up for each concentration. After incubation for 1 h, cells were infected with LCMV. After 36h, detect the effect of clofazimine inhibiting virus replication by measuring supernatant titer, the results on two kinds of cells are respectively as follows image 3 and Figure 4 As shown, under different concentration conditions, the compound clofazimine has a significant inhibitory effect on LCMV. By dra...

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Abstract

The invention provides an application of clofazimine and / or its pharmaceutically acceptable derivatives in the preparation of anti-arenavirus drugs. The invention detects the cytotoxicity of clofazimine on Vero cells and BHK-21 cells and its antiviral activity against arenaviruses, indicating that clofazimine exhibits strong anti-arenavirus effects 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 clofazimine 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 ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/498A61P31/14
CPCA61K31/498A61P31/14
Inventor 刘愈杰徐国东袁冰
Owner CANVEST WUHAN BIOTECH
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