Cannabinoids Block Cellular Entry of SARS-CoV‑2
and the Emerging Variants
Posted on 10.01.2022 - 20:34
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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van Breemen, Richard B.; Muchiri, Ruth N.; Bates, Timothy A.; Weinstein, Jules B.; Leier, Hans C.; Farley, Scotland; et al. (2022): Cannabinoids Block Cellular Entry of SARS-CoV‑2 and the Emerging Variants. ACS Publications. Collection. https://doi.org/10.1021/acs.jnatprod.1c00946
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Richard B. van Breemen
Ruth N. Muchiri
Timothy A. Bates
Jules B. Weinstein
Hans C. Leier
Fikadu G. Tafesse
virus neutralization assayssafe human usemolecule therapeutic agentscannabis sativa </beta variant bhuman epithelial cellscov ‑ 22 spike proteinspike proteinpseudovirus expressingprevented entryorthosteric ligandsorally bioavailablemicromolar affinitylong historyhemp extractshemp (<equally effectivecause covidcannabinoid acidscannabigerolic acidcannabidiolic acidbotanical ligands