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Aurones: A Promising Scaffold to Inhibit SARS-CoV-2 Replication
Guilherme S Caleffi, Alice S Rosa1, Luana G de Souza
1Laboratório de Morfologia e Morfogênese Viral, Instituto Oswaldo Cruz, Fundação Oswaldo Cruz, 21040-900 Rio de Janeiro, Brazil.
Journal of Natural Products
|May 31, 2023
Summary
New aurone compounds show potent antiviral activity against SARS-CoV-2. Several derivatives demonstrated significant efficacy with low cytotoxicity, offering promising therapeutic potential for COVID-19 treatment.
Area of Science:
- Medicinal Chemistry
- Virology
- Drug Discovery
Background:
- Aurones are a class of flavonoids structurally isomeric to flavones and flavonols.
- Flavonoids, including flavones and flavonols, have demonstrated inhibitory effects on SARS-CoV-2 replication.
- The specific antiviral potential of aurones against SARS-CoV-2 remains an area for exploration.
Purpose of the Study:
- To design and synthesize a novel series of aurone derivatives.
- To evaluate the anti-SARS-CoV-2 activity of these synthesized compounds.
- To investigate the structure-activity relationships of aurones against SARS-CoV-2.
Main Methods:
- Chemical synthesis of 25 aurone derivatives with varied oxygenated substituents on the A- and/or B-rings.
- Cell-based screening assays to determine anti-SARS-CoV-2 activity (EC50).
- Cytotoxicity assays in Calu-3 cells to assess safety.
- Molecular dynamics calculations to explore potential interactions with SARS-CoV-2 3CLpro.
Main Results:
- Twelve out of 25 synthesized aurones exhibited EC50 values below 3 μM.
- Five compounds demonstrated EC50 values below 1 μM with no significant cytotoxicity.
- Aurone 8q showed the highest potency (EC50 = 0.4 μM) and selectivity (SI = 2441.3), outperforming myricetin and baicalein.
- Methoxy, methoxymethoxy, and difluoromethyl groups on the rings enhanced antiviral activity.
Conclusions:
- The synthesized aurone derivatives represent a promising class of compounds for anti-SARS-CoV-2 drug development.
- Specific substitutions, particularly methoxy-containing groups, are crucial for potent antiviral activity.
- Further investigation is warranted to elucidate the precise mechanism of action and identify the specific viral target.
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