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Cannabinoids Block Cellular Entry of SARS-CoV-2 and the Emerging Variants.


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 (Cannabis sativa) 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.

SUBMITTER: van Breemen RB 

PROVIDER: S-EPMC8768006 | biostudies-literature | 2022 Jan

REPOSITORIES: biostudies-literature

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Cannabinoids Block Cellular Entry of SARS-CoV-2 and the Emerging Variants.

van Breemen Richard B RB   Muchiri Ruth N RN   Bates Timothy A TA   Weinstein Jules B JB   Leier Hans C HC   Farley Scotland S   Tafesse Fikadu G FG  

Journal of natural products 20220110 1


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 (<i>Cannabis sativa</i>) were found to be allosteric as well as orthosteric ligands with micromolar affinity for the spike protein. In follow-up  ...[more]

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