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

Richard B. van Breemen; Ruth N. Muchiri; Timothy A. Bates; Jules B. Weinstein; Hans C. Leier; Scotland Farley; Fikadu G. Tafesse

doi:10.1021/acs.jnatprod.1c00946

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

Richard B. van Breemen, Ruth N. Muchiri, Timothy A. Bates, Jules B. Weinstein, Hans C. Leier, Scotland Farley, Fikadu G. Tafesse

Molecular Microbiology and Immunology

Research output: Contribution to journal › Article › peer-review

75 Scopus citations

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.

Original language	English (US)
Pages (from-to)	176-184
Number of pages	9
Journal	Journal of Natural Products
Volume	85
Issue number	1
DOIs	https://doi.org/10.1021/acs.jnatprod.1c00946
State	Published - Jan 28 2022

ASJC Scopus subject areas

Analytical Chemistry
Molecular Medicine
Pharmacology
Pharmaceutical Science
Drug Discovery
Complementary and alternative medicine
Organic Chemistry

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10.1021/acs.jnatprod.1c00946

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title = "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.",

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AU - Farley, Scotland

AU - Tafesse, Fikadu G.

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

Abstract

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