tetano
Editor, Senior Moderator
J Nat Prod
. 2022 Jan 10.
doi: 10.1021/acs.jnatprod.1c00946. Online ahead of print.
Cannabinoids Block Cellular Entry of SARS-CoV-2 and the Emerging Variants
Richard B van Breemen[SUP] 1 [/SUP], Ruth N Muchiri[SUP] 1 [/SUP], Timothy A Bates[SUP] 2 [/SUP], Jules B Weinstein[SUP] 2 [/SUP], Hans C Leier[SUP] 2 [/SUP], Scotland Farley[SUP] 2 [/SUP], Fikadu G Tafesse[SUP] 2 [/SUP]
Affiliations
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.
. 2022 Jan 10.
doi: 10.1021/acs.jnatprod.1c00946. Online ahead of print.
Cannabinoids Block Cellular Entry of SARS-CoV-2 and the Emerging Variants
Richard B van Breemen[SUP] 1 [/SUP], Ruth N Muchiri[SUP] 1 [/SUP], Timothy A Bates[SUP] 2 [/SUP], Jules B Weinstein[SUP] 2 [/SUP], Hans C Leier[SUP] 2 [/SUP], Scotland Farley[SUP] 2 [/SUP], Fikadu G Tafesse[SUP] 2 [/SUP]
Affiliations
- PMID: 35007072
- DOI: 10.1021/acs.jnatprod.1c00946
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.
