Dieckol, a SARS-CoV 3CLpro inhibitor, isolated from the edible brown algae Ecklonia cava

Bioorganic & Medicinal Chemistry
2013.0

Abstract

SARS-CoV 3CL(pro) plays an important role in viral replication. In this study, we performed a biological evaluation on nine phlorotannins isolated from the edible brown algae Ecklonia cava. The nine isolated phlorotannins (1-9), except phloroglucinol (1), possessed SARS-CoV 3CL(pro) inhibitory activities in a dose-dependently and competitive manner. Of these phlorotannins (1-9), two eckol groups with a diphenyl ether linked dieckol (8) showed the most potent SARS-CoV 3CL(pro) trans/cis-cleavage inhibitory effects (IC(50)s = 2.7 and 68.1 μM, respectively). This is the first report of a (8) phlorotannin chemotype significantly blocking the cleavage of SARS-CoV 3CL(pro) in a cell-based assay with no toxicity. Furthermore, dieckol (8) exhibited a high association rate in the SPR sensorgram and formed extremely strong hydrogen bonds to the catalytic dyad (Cys145 and His41) of the SARS-CoV 3CL(pro).

Knowledge Graph

Similar Paper

Dieckol, a SARS-CoV 3CLpro inhibitor, isolated from the edible brown algae Ecklonia cava
Bioorganic & Medicinal Chemistry 2013.0
Anti-HIV-1 activity of phloroglucinol derivative, 6,6′-bieckol, from Ecklonia cava
Bioorganic & Medicinal Chemistry 2008.0
Chemical components and its antioxidant properties in vitro: An edible marine brown alga, Ecklonia cava
Bioorganic & Medicinal Chemistry 2009.0
Acetylcholinesterase inhibitory activity of phlorotannins isolated from the brown alga, Ecklonia maxima (Osbeck) Papenfuss
Food Research International 2013.0
Hemeoxygenase 1 partly mediates the anti-inflammatory effect of dieckol in lipopolysaccharide stimulated murine macrophages
International Immunopharmacology 2014.0
Molecular docking studies of phlorotannins from Eisenia bicyclis with BACE1 inhibitory activity
Bioorganic & Medicinal Chemistry Letters 2010.0
Specific Plant Terpenoids and Lignoids Possess Potent Antiviral Activities against Severe Acute Respiratory Syndrome Coronavirus
Journal of Medicinal Chemistry 2007.0
Discovery of 9,10-dihydrophenanthrene derivatives as SARS-CoV-2 3CLpro inhibitors for treating COVID-19
European Journal of Medicinal Chemistry 2022.0
Discovery of Natural Bisbenzylisoquinoline Analogs from the Library of Thai Traditional Plants as SARS-CoV-2 3CL<sup>Pro</sup> Inhibitors: In Silico Molecular Docking, Molecular Dynamics, and In Vitro Enzymatic Activity
Journal of Chemical Information and Modeling 2023.0
New Marine Cembrane-type Diterpenoids from the Okinawan Soft Coral <i>Clavularia </i><i>k</i><i>oellikeri</i>
Journal of Natural Products 2000.0