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Application of candesartan cilexetil or pharmaceutically acceptable salt thereof in preparation of drug for preventing and/or treating COVID-19

A technology of candesartan medoxomil and coronavirus, applied in the directions of antiviral agents, medical preparations containing active ingredients, pharmaceutical formulations, etc., can solve problems such as lack of effective prevention and treatment drugs, and achieve the effect of strong binding strength

Active Publication Date: 2020-07-17
SUN YAT SEN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The purpose of the present invention is to address the current problem of lack of effective prevention and treatment drugs for lung and other related inflammatory diseases caused by new coronaviruses, and to provide candesartan cilexetil or a pharmaceutically acceptable salt thereof in the preparation of prevention and / or treatment of new coronaviruses Applications in Inflammation Drugs

Method used

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  • Application of candesartan cilexetil or pharmaceutically acceptable salt thereof in preparation of drug for preventing and/or treating COVID-19
  • Application of candesartan cilexetil or pharmaceutically acceptable salt thereof in preparation of drug for preventing and/or treating COVID-19
  • Application of candesartan cilexetil or pharmaceutically acceptable salt thereof in preparation of drug for preventing and/or treating COVID-19

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Example 1 Binding mode of candesartan cilexetil and metabolite candesartan to novel coronavirus target 3CL hydrolase (Mpro)

[0048] This example relies on supercomputers such as Tianhe-2 and Shenzhen Supercomputing and the team independently developed drug / target binding strength accurate prediction software (GA-FEP), using molecular docking, kinetic simulation and absolute free energy perturbation methods (specific methods refer to J Med Chem, 2019, 62, 2099-2111) predicted the binding strength of candesartan cilexetil and the target 3CL hydrolase (Mrpo high-resolution crystal structure, PDB ID: 6LU7) of pneumonia caused by the new coronavirus, and its binding mode (such as attached figure 1 shown), the benzimidazole ring of candesartan cilexetil forms a π-π interaction with the No. 41 histidine of the Mpro protein; And the hydrophobic pocket composed of No. 49 methionine, and the tetrazole ring on the biphenyl forms a pair of hydrogen bond interactions with No. 163 ...

Embodiment 2

[0051] Example 2 Inhibitory effect of candesartan cilexetil on novel coronavirus target 3CL hydrolase

[0052] (1) Experimental materials:

[0053] The recombinant plasmid containing the 3CL gene was synthesized by Wuhan Pujian Biotechnology Company, GST Beads were purchased from SmartLifescience Company, the multifunctional microplate reader was SpectraMax i3 from Molecular Device Company of the United States, and the 96-well black plate was purchased from Corning, Candesartan Medoxil and others in the United States Commonly used reagents were purchased from Sigma.

[0054] (2) Experimental method:

[0055] a. Expression and purification of recombinant 3CL hydrolase

[0056] Transform the 3CL recombinant plasmid (pGEX4T1) containing the origin of SARS-CoV-2 into E. coli strain BL21 (codonplus), and then grow the strain to OD in LB or 2x YT medium 600 0.6-0.8, then add 0.1mM isopropyl-1-thio-β-D-galactoside (IPTG) and continue to grow at 15°C for 24 hours to induce expressi...

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Abstract

The invention discloses an application of candesartan cilexetil or a pharmaceutically acceptable salt thereof in preparation of a drug for preventing and / or treating COVID-19. The candesartan cilexetil and hydrolysate candesartan have stronger binding strength with SARS-CoV-2 target 3CL hydrolase (MPro) that causes inflammation in the lung, and can significantly inhibit the activity of the 3CL hydrolase, wherein the IC50 of the candesartan cilexetil and the hydrolysate candesartan against the 3CL hydrolase (Mpro) is 2.78+ / -0.31 [mu]M and 9.45+ / -0.73 [mu]M, respectively, and the results indicate that the candesartan cilexetil and the hydrolysate candesartan have the effect of preventing and treating pneumonia caused by the SARS-CoV-2, and can be used to prepare an anti-pneumonia drug for application.

Description

technical field [0001] The present invention relates to the field of pharmaceutical technology and pulmonary disease technology, more specifically, relates to the application of candesartan cilexetil or a pharmaceutically acceptable salt thereof in the preparation of a drug for preventing and / or treating novel coronavirus inflammation. Background technique [0002] Novel coronavirus pneumonia (COVID-19) refers to pneumonia caused by a new type of coronavirus (SARS-CoV-2) infection. Its clinical features are fever, dry cough, fatigue, and gradually progress to symptoms such as asthma and shortness of breath. Although some mild patients can recover spontaneously, there are still many patients with rapid disease progression in the later stage, developing acute respiratory distress syndrome (ARDS), sepsis, renal failure, metabolic acidosis that is difficult to correct, and hemorrhage and coagulation obstacle. The disease is mainly transmitted by respiratory droplets and contact...

Claims

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Application Information

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IPC IPC(8): A61K31/4184A61P31/14
CPCA61K31/4184A61P31/14
Inventor 罗海彬王鑫李哲黄仪有周倩
Owner SUN YAT SEN UNIV
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