The Natural Stilbenoid (–)-Hopeaphenol Inhibits Cellular Entry of SARS-CoV-2 USA-WA1/2020, B.1.1.7, and B.1.351 Variants
Ian Tietjen, Joel Cassel, Emery T. Register, Xiang Yang Zhou, Troy E. Messick, Frederick Keeney, Lily D. Lu, Karren D. Beattie, Topul Rali, Pablo Tebas, Hildegund C. J. Ertl, Joseph M. Salvino, Rohan A. Davis, Luis J. Montaner
Abstract
s, 1.0 to 7.3 μM). Notably, (-)-hopeaphenol also inhibited two emerging variants of concern, B.1.1.7/Alpha and B.1.351/Beta in both viral and spike-containing pseudovirus assays with similar or improved activities over the USA-WA1/2020 variant. These results identify (-)-hopeaphenol and related stilbenoid analogues as potent and selective inhibitors of viral entry across multiple SARS-CoV-2 variants of concern.
Topics & Concepts
CytotoxicityViral entryCytopathic effectViral replicationCell cultureBiologySmall moleculeChemistryEnzymeBinding siteIn vitroBiochemistryReceptorCellTransfectionVirusHEK 293 cellsRecombinant DNAResveratrolCell biologyLigand binding assayBinding domainPlasma protein bindingDrug discoveryMutantIn vivoReporter geneBiological activityFlow cytometryHigh-throughput screeningStructure–activity relationshipVirologyViral envelopeMolecular biologyPhenotypic screeningSirtuins and Resveratrol in MedicinePharmacological Receptor Mechanisms and EffectsBiological and pharmacological studies of plants