posted on 2022-01-10, 20:34authored byRichard B. van Breemen, Ruth N. Muchiri, Timothy A. Bates, Jules B. Weinstein, Hans C. Leier, Scotland Farley, Fikadu G. Tafesse
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.