Application of myricetin in preparing medicine for preventing or treating coronavirus and influenza virus

A technology of coronavirus and influenza virus, which is applied in the field of medicine, achieves good market application prospects and reduces the effect of inflammatory response in the body

Pending Publication Date: 2021-03-26
MACAU UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The discovery and application of such active ingredients in the prior art needs to be further improved in order to better prevent and treat new coronaviruses or other viruses

Method used

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  • Application of myricetin in preparing medicine for preventing or treating coronavirus and influenza virus
  • Application of myricetin in preparing medicine for preventing or treating coronavirus and influenza virus
  • Application of myricetin in preparing medicine for preventing or treating coronavirus and influenza virus

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1: Interaction between myricetin and new coronavirus-related targets

[0033] After consulting the three-dimensional structure of myricetin and the new coronavirus SARS-CoV-2 from the database in the prior art, the molecular docking calculation method was used to find the active ligand of the protein in the workstation to determine the relationship between myricetin and the new coronavirus SARS-CoV-2. 2 Interactions between related targets. The results showed that myricetin interacted with viral replication protease (PLpro), 3C-like protease (3CLpro), ribonucleic acid synthetase (RdRp), spike protein-host cell ACE2 receptor (S- ACE2) and other 4 targets have interactions, and the results are shown in Table 1 (the negative absolute value in Table 1 greater than 5 indicates that there is a stronger interaction between myricetin and the target; the greater the negative absolute value, It shows that the interaction between myricetin and the target is stronger).

...

Embodiment 2

[0037] Embodiment 2: Myricetin and spike protein (Spike) affinity test in ACE2, SARS-CoV-2

[0038] After diluting myricetin into 6 concentration gradients by two-fold gradient dilution method, they were detected with the prepared RBD probe and ACE2 probe on a molecular interaction instrument. The detection results showed that myricetin and RBD protein (Kd=12.31± 4.95), ACE2 protein (Kd=26.2±4.38) has a strong affinity (the smaller the Kd value, the greater the affinity, and Kd<100 μM indicates a strong affinity, μM means μmol / L), the results are shown in Table 2 .

[0039] Table 2: Affinity of myricetin with the binding domain of Spike protein (spike protein) and ACE2 protein of SARS-CoV-2

[0040] RBD probe Kd(μM) ACE2 probe Kd(μM) 12.31±4.95 26.2±4.38

Embodiment 3

[0041] Embodiment 3: Myricetin is to the inhibitory activity test of SARS-CoV-2, HCoV-229E, H1N1 virus

[0042] Add 100 μL to each well of a 96-well culture plate at a concentration of 2×10 5 cells / mL of Huh-7 or Vero E6 cells at 37°C, 5% CO 2 Cultivate for 24 hours; Add 50 TCID50 (half the tissue culture infection dose) of HCoV-229E or SARS-CoV-2 virus solution 100 μ L / hole to drug experiment group and virus control group, 37 ℃, 5% CO 2 Incubator adsorption for 1 hour. The culture medium was discarded, and 100 μL / well of two-fold serial dilution of the test drug was added, with 4 replicate wells for each concentration, and a cell control, virus control (negative control) and positive drug control Remdesivir (Remdesivir) were set up at the same time. 37°C, 5% CO 2 After incubating in the incubator for 3 days, record CPE (cytopathies caused by viruses) under an optical microscope, and record the percentage of cells with CPE in the total cells according to the following 6-lev...

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Abstract

The invention belongs to the technical field of medicines, and discloses an application of myricetin in preparation of medicines for preventing or treating coronavirus and influenza virus, and administration dosage of myricetin or pharmaceutically acceptable salt thereof is 0.1-1000 mg / kg. The myricetin has high protein affinity to a target point of interaction of SARS-CoV-2, an RBD protein of a Spike protein binding domain of the SARS-CoV-2 and a receptor protein ACE2. In addition, the myricetin can also inhibit activity of SARS-CoV-2, HCoV-229E and H1N1 viruses, and can relieve in-vivo inflammatory reaction of an inflammatory animal model. According to the invention, it is determined for the first time that myricetin has an inhibition effect on SARS-CoV-2 and an action target thereof, and no toxic reaction occurs.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to the application of myricetin in the preparation of medicines for preventing or treating coronaviruses and influenza viruses. Background technique [0002] Severe acute respiratory syndrome coronavirus 2 (i.e. SARS-CoV-2 or COVID-19) infection is a highly contagious new infectious disease with a long incubation period. The crowd is generally susceptible, and respiratory droplets and contact transmission are the main routes of transmission. For the SARS-CoV-2 infectious disease, there is still no definite and effective treatment. Therefore, how to rapidly develop drugs for preventing and treating this viral infection is a global hot issue. [0003] In the fight against the SARS-CoV-2 epidemic, traditional Chinese medicine has played an important role. It has been found that the active ingredients contained in Chinese herbal medicines against the new coronavirus can be prepared i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61P31/14A61P31/16A61K8/49A61Q19/00A23L33/105
CPCA61K31/352A61P31/14A61P31/16A61K8/498A61Q19/00A23L33/105A23V2002/00A23V2200/30A23V2200/314A23V2250/21
Inventor 刘良潘胡丹杨子峰姚小军李润峰
Owner MACAU UNIV OF SCI & TECH
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