Cannabinoids Block Cellular Entry of SARS-CoV‑2 and the Emerging Variants
Posted on 2022-01-10 - 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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AUTHORS (7)
Rv
Richard B. van Breemen
RM
Ruth N. Muchiri
TB
Timothy A. Bates
JW
Jules B. Weinstein
HL
Hans C. Leier
SF
Scotland Farley
FT
Fikadu G. Tafesse
KEYWORDS
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