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ElaKiri Talk!
Cannabinoids Block Cellular Entry of SARS-CoV-2 and the Emerging Variants
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<blockquote data-quote="imhotep" data-source="post: 27280027" data-attributes="member: 562115"><p>[ATTACH=full]157173[/ATTACH]</p><p></p><p>In a recent study by researchers at the Linus Pauling Institute, Oregon State University - <strong>Two cannabinoids have shown the highest affinities for the SARS-CoV-2 spike glycoprotein</strong>, and those were cannabidiolic acid (CBDA) and cannabigerolic acid (CBGA). They have successfully blocked infection of human epithelial cells by a pseudovirus expressing the spike glycoprotein.</p><p></p><p>An even more significant finding was that both CBDA and CBGA from hemp could effectively halt the infection with not only the original live SARS-CoV-2 but also variants of concern such as B.1.1.7 (alpha strain) and B.1.351 (beta strain). Of note, at the time of these experiments, omicron strain was still not identified.</p><p></p><p>The authors further note that the concentrations necessary to block infection by 50% of viruses are clinically achievable. The data on bioavailability (primarily for CBDA) show that micromolar plasma and serum concentrations should be possible, which is necessary for efficacy and tolerability.</p><p>With extensive use of cannabinoids, resistant SARS-CoV-2 variants may still surface. Still, the combination of vaccines and CBDA/CBGA treatment may open the door for a more demanding environment where SARS-CoV-2 will have a highly reduced opportunity for escape.</p><p></p><p><strong>Abstract-</strong></p><p></p><p>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 (<em>Cannabis sativa</em>) 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.</p></blockquote><p></p>
[QUOTE="imhotep, post: 27280027, member: 562115"] [ATTACH type="full"]157173[/ATTACH] In a recent study by researchers at the Linus Pauling Institute, Oregon State University - [B]Two cannabinoids have shown the highest affinities for the SARS-CoV-2 spike glycoprotein[/B], and those were cannabidiolic acid (CBDA) and cannabigerolic acid (CBGA). They have successfully blocked infection of human epithelial cells by a pseudovirus expressing the spike glycoprotein. An even more significant finding was that both CBDA and CBGA from hemp could effectively halt the infection with not only the original live SARS-CoV-2 but also variants of concern such as B.1.1.7 (alpha strain) and B.1.351 (beta strain). Of note, at the time of these experiments, omicron strain was still not identified. The authors further note that the concentrations necessary to block infection by 50% of viruses are clinically achievable. The data on bioavailability (primarily for CBDA) show that micromolar plasma and serum concentrations should be possible, which is necessary for efficacy and tolerability. With extensive use of cannabinoids, resistant SARS-CoV-2 variants may still surface. Still, the combination of vaccines and CBDA/CBGA treatment may open the door for a more demanding environment where SARS-CoV-2 will have a highly reduced opportunity for escape. [B]Abstract-[/B] 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 ([I]Cannabis sativa[/I]) 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. [/QUOTE]
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