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Application of polyphenols in resisting coronavirus

A coronavirus, polyphenol technology, used in the field of biomedicine

Active Publication Date: 2021-08-27
SHANGHAI TECH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0039] In the prior art, none of the above drugs can be used to treat related diseases caused by coronavirus

Method used

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  • Application of polyphenols in resisting coronavirus
  • Application of polyphenols in resisting coronavirus
  • Application of polyphenols in resisting coronavirus

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0108] High-throughput screening was carried out from different compound libraries, and the 33 compounds successfully screened had good inhibitory effects on the main protease of the new coronavirus. The specific conditions of the enzyme activity experiment are:

[0109] Fluorescent substrate for enzyme activity experiment: MCA-AVLQSGFR-Lys(Dnp)-Lys-NH2, the excitation wavelength and emission wavelength of this fluorescent substrate are 320nm and 405nm, respectively.

[0110] The enzyme activity reaction buffer is 50mM Tris–HCl (pH 7.3), 1mM EDTA; the enzyme activity reaction temperature: 30°C. The reaction was initiated by adding protease, the final concentration of protease was 0.2 μM, the concentration of substrate was 20 μM, and the concentration of inhibitors (33 kinds of small molecule compounds) was 1.5 μM. (Xue X, Yang H, Shen W, et al. Production of authentic SARS-CoV Mpro with enhanced activity: application as a novel tag-cleavage endopeptidase for protein overprodu...

Embodiment 2

[0115] The fluorescent substrate used in the determination of enzyme activity inhibition curve: MCA-AVLQSGFR-Lys(Dnp)-Lys-NH2, the excitation wavelength and emission wavelength of this fluorescent substrate are 320nm and 405nm respectively.

[0116] The enzyme activity inhibition curve assay buffer was 50mM Tris–HCl (pH 7.3), 1mM EDTA; reaction temperature: 30°C. The reaction was initiated by adding protease, the final concentration of protease was 0.2 μM, and the substrate concentration was 20 μM. 11 different concentrations of carmofur were used for measurement. The test results showed that IC 50 The value is 1.82μM ( Figure 34 ) (Jin Z, Du X, Xu Y, et al. Structure of Mpro from COVID-19 virus and discovery of its inhibitors [J]. Nature, 2020, 582(7811): 1-9.).

[0117] In the in vitro cell antiviral experiment, 6 different concentrations of carmofur were used to treat Vero E6 cells infected with SARS-CoV-2 for 1 hour, and the virus MOI (multiplicity of infection) was 0.05...

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Abstract

The invention discloses an application of various compounds such as polyphenols in resisting coronavirus. The invention relates to the application of one or more of a polyphenol substance, a proton pump inhibitor, p-benzoquinone and a derivative thereof, an active ingredient of sappan wood, TDZD-8, thiomersalate, alkannin, Tidelusib, protoflavin, rabeprazole sodium, PX-12, Dixanthophygen, methyl cholate, carbamofluorine, corilagin, dihydromyricetin, chloramine T, merbromin, gallocatechin, fraxetin, meisoindigo, a lactic acid ethacridine monohydrate and sousoprazole in preparation of drugs for treating and / or preventing diseases caused by coronavirus. In-vitro enzyme activity experiments show that various compounds such as 1, 4-naphthoquinone and the like can well inhibit the activity of main protease in the coronavirus, and the defect that diseases caused by the coronavirus cannot be treated in the prior art is overcome.

Description

technical field [0001] The invention belongs to the technical field of biomedicine and relates to the application of polyphenols in anti-coronavirus, in particular to the application of compounds such as polyphenols in the preparation of medicines for treating and / or preventing diseases caused by coronaviruses. Background technique [0002] Coronaviruses are a class of viruses that are closely related to humans and animals. Coronaviruses HCoV-229E and HCoV-OC43 cause the common cold (van der Hoek, L., Pyrc, K., Jebbink, M. et al. Identification of a newhuman coronavirus. Nat Med 2004, 10, 368–373). The recently circulating SARS-CoV-2 virus can cause COVID-19, clinically manifested as fever, dry cough and dyspnea, severe illness can cause death (Jeannette Guarner, MD, Three Emerging Coronaviruses in Two Decades: The Story of SARS, MERS, and NowCOVID-19, American Journal of Clinical Pathology,, aqaa029). Coronaviruses have a huge impact on animal husbandry: porcine epidemic ...

Claims

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Application Information

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IPC IPC(8): A61K31/122A61K31/352A61K31/433A61K31/305A61K31/4439A61K31/473A61K31/4164A61K31/265A61K31/513A61K31/575A61K31/7024A61K31/18A61K31/37A61K31/353A61K31/335A61K31/404A61K31/216A61P31/14
CPCA61P31/14A61K31/352A61K31/335A61K36/48A61K31/145A61P11/00
Inventor 杨海涛靳振明杨秀娜赵耀饶子和
Owner SHANGHAI TECH UNIV
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