TitleCannabinoids Block Cellular Entry of SARS-CoV-2 and the Emerging Variants.
Publication TypeJournal Article
Year of Publication2022
Authorsvan Breemen RB, Muchiri RN, Bates TA, Weinstein JB, Leier HC, Farley S, Tafesse FG
JournalJ Nat Prod
Volume85
Issue1
Pagination176-184
Date Published2022 Jan 28
ISSN1520-6025
KeywordsAngiotensin-Converting Enzyme 2, Animals, Antiviral Agents, Benzoates, Cannabinoids, Chlorocebus aethiops, COVID-19, COVID-19 Drug Treatment, Humans, Ligands, Mass Spectrometry, Models, Molecular, Protein Binding, SARS-CoV-2, Spike Glycoprotein, Coronavirus, Vero Cells, Virus Internalization
Abstract

As a complement to vaccines, small-molecule therapeutic agents are needed to treat or prevent infections by severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) and its variants, which cause COVID-19. Affinity selection-mass spectrometry was used for the discovery of botanical ligands to the SARS-CoV-2 spike protein. Cannabinoid acids from hemp () were found to be allosteric as well as orthosteric ligands with micromolar affinity for the spike protein. In follow-up virus neutralization assays, cannabigerolic acid and cannabidiolic acid prevented infection of human epithelial cells by a pseudovirus expressing the SARS-CoV-2 spike protein and prevented entry of live SARS-CoV-2 into cells. Importantly, cannabigerolic acid and cannabidiolic acid were equally effective against the SARS-CoV-2 alpha variant B.1.1.7 and the beta variant B.1.351. Orally bioavailable and with a long history of safe human use, these cannabinoids, isolated or in hemp extracts, have the potential to prevent as well as treat infection by SARS-CoV-2.
DOI10.1021/acs.jnatprod.1c00946
Alternate JournalJ Nat Prod
PubMed ID35007072
PubMed Central IDPMC8768006
Grant ListT32 HL083808 / HL / NHLBI NIH HHS / United States