Inhibition of SARS-CoV 3CL protease by flavonoids.
J Enzyme Inhib Med Chem
; 35(1): 145-151, 2020 Dec.
Article
in English
| MEDLINE | ID: covidwho-826697
ABSTRACT
There were severe panics caused by Severe Acute Respiratory Syndrome (SARS) and Middle-East Respiratory Syndrome-Coronavirus. Therefore, researches targeting these viruses have been required. Coronaviruses (CoVs) have been rising targets of some flavonoids. The antiviral activity of some flavonoids against CoVs is presumed directly caused by inhibiting 3C-like protease (3CLpro). Here, we applied a flavonoid library to systematically probe inhibitory compounds against SARS-CoV 3CLpro. Herbacetin, rhoifolin and pectolinarin were found to efficiently block the enzymatic activity of SARS-CoV 3CLpro. The interaction of the three flavonoids was confirmed using a tryptophan-based fluorescence method, too. An induced-fit docking analysis indicated that S1, S2 and S3' sites are involved in binding with flavonoids. The comparison with previous studies showed that Triton X-100 played a critical role in objecting false positive or overestimated inhibitory activity of flavonoids. With the systematic analysis, the three flavonoids are suggested to be templates to design functionally improved inhibitors.
Keywords
Full text:
Available
Collection:
International databases
Database:
MEDLINE
Main subject:
Antiviral Agents
/
Viral Proteins
/
Flavonoids
/
Severe acute respiratory syndrome-related coronavirus
/
Enzyme Inhibitors
Type of study:
Systematic review/Meta Analysis
Topics:
Traditional medicine
Limits:
Humans
Language:
English
Journal:
J Enzyme Inhib Med Chem
Journal subject:
Biochemistry
/
Chemistry
Year:
2020
Document Type:
Article
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