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Application of estradiol benzoate or pharmaceutically acceptable salt thereof in preparation of anti-coronavirus drugs

A technology of estradiol benzoate and coronavirus, applied in the field of medicine, can solve problems such as no estradiol benzoate yet

Pending Publication Date: 2021-03-19
SOUTHERN MEDICAL UNIVERSITY +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no application of estradiol benzoate and estradiol benzoate analogues in anti-coronavirus

Method used

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  • Application of estradiol benzoate or pharmaceutically acceptable salt thereof in preparation of anti-coronavirus drugs
  • Application of estradiol benzoate or pharmaceutically acceptable salt thereof in preparation of anti-coronavirus drugs
  • Application of estradiol benzoate or pharmaceutically acceptable salt thereof in preparation of anti-coronavirus drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1 Inhibitory activity detection of estradiol benzoate to SARS-CoV-2 in vitro

[0035] 1. Drug inhibitory activity test:

[0036] 1) Take Vero-E6 cells in the logarithmic growth phase, 3*10^5 cells / well, inoculate in a 48-well plate, 37°C, 5% CO 2 Incubate overnight.

[0037]2) Drug pre-incubation: the drug is diluted with DMEM medium containing a total volume of 2% fetal bovine serum. The initial concentration of the drug is set to 200 μM (the solvent is DMSO), the drug is diluted threefold, and 3 replicate holes are set for each concentration, with a total of 6 drug gradients (200, 66.67, 22.22, 7.41, 2.47, 0.82 μM); set the solvent Dimethyl sulfoxide (DMSO) was used as a control group, which was diluted with DMEM medium containing 2% fetal bovine serum in total volume, and given the same volume of DMSO as the drug. After removal of the cell supernatant, 100 μl of diluted drug was added to each well of the 48-well plate in 1) for the experimental group, and ...

Embodiment 2

[0064] Example 2 Estradiol Benzoate Inhibitory Activity Detection of SARS-CoV-2S Pseudovirus Entry

[0065] 1. Method:

[0066] 1) SARS-CoV-2S pseudovirus packaging:

[0067] 4*10^5 HEK-293T cells in the logarithmic growth phase / ml, 2ml per well were uniformly seeded in a 6-well plate. 37°C, 5% CO 2 Incubate for 24 hours in a cell culture incubator. Replace the fresh medium half an hour before transfection, and use 100 μl blank DMEM medium to prepare plasmid dilution and transfection reagent (PolyJet) dilution respectively. The preparation ratio for each well is as follows (plasmid DNA needs to be extracted with an endotoxin-free extraction kit) :

[0068] pNL4-3.Luc.R-E-1000ng

[0069] pcDNA3.1-SARS-CoV-2-S 500ng

[0070] PolyJet 6μl

[0071] The specific preparation method is as follows: pNL4-3.Luc.R-E-plasmid and pcDNA3.1-SARS-CoV-2-Spike plasmid are simultaneously added to 100 μl blank DMEM medium and mixed, and PolyJet is diluted and mixed with 100 μl blank DMEM me...

Embodiment 3

[0077] Cytotoxicity detection of embodiment 3 estradiol benzoate

[0078] 1. Method:

[0079] 1) Cell inoculation:

[0080] For Vero-E6 and 293T-ACE2 cells in the logarithmic growth phase, adjust the cell density to 1*10^4 cells / well, inoculate 100 μL / well in 96-well plates, and culture overnight.

[0081] 2) Drug concentration design:

[0082] Vero-E6 cells: 6 concentration gradients were diluted 3 times in DMEM medium containing a total volume of 2% fetal calf serum before administration, and the initial concentration of the drug was set to 200 μM (200, 66.66, 22.22, 7.41, 2.47, 0.82 μM ); Add 100 μL of the diluted drug in each well to the Vero-E6 cells in the 96-well plate in 1), with a final volume of 200 μL in each well. Three replicate wells were set up for each drug concentration. The DMSO solvent treatment group was used as the blank control.

[0083]293T-ACE2 cells: 8 concentration gradients were diluted 2-fold in DMEM medium containing 2% fetal bovine serum in t...

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Abstract

The invention discloses application of estradiol benzoate or a pharmaceutically acceptable salt thereof in preparation of anti-coronavirus drugs. The application of estradiol benzoate or the pharmaceutically acceptable salt thereof in preparation of the anti-coronavirus drugs is proposed for the first time, the application expands the application range of estradiol benzoate, and particularly, under the condition of epidemic global new coronal pneumonia, a new drug is provided for inhibiting new coronal pneumonia caused by SARS-CoV-2.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to an application of estradiol benzoate or a pharmaceutically acceptable salt thereof in the preparation of anti-coronavirus drugs. Background technique [0002] There are 6 kinds of coronaviruses known to infect humans in the past, namely human coronaviruses HCoV-229E, HCoV-OC43, HCoV-NL63 and HCoV-HKU1, and severe acute respiratory syndrome coronavirus SARS-CoV and Middle East respiratory syndrome Coronavirus MERS-CoV. SARS-CoV-2 is currently the seventh known coronavirus that can infect humans. It is a single-stranded RNA positive-strand enveloped β-coronavirus with a genome length of about 26-32 kb. The entry of SARS-CoV-2 into host cells is mediated by the transmembrane spike S glycoprotein (Spike protein, S), which can be cleaved into S1 and S2 subunits under the action of host cell membrane surface proteases, wherein S2 is a coronavirus Evolutionary conserved domain, with ...

Claims

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Application Information

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IPC IPC(8): A61K31/565A61P31/14
CPCA61K31/565A61P31/14
Inventor 徐伟刘叔文杨婵牛晓阁潘晓彦肖庚富孙静赵金存
Owner SOUTHERN MEDICAL UNIVERSITY
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