A new promising study shows that cannabigerolic acid (CBGA) and cannabidiolic acid (CBDA) could be effective in both preventing and treating COVID-19. CBGA and CBDA were found to be equally effective against the alpha and the beta variant of the virus, which could provide synergy with the vaccination efforts in the global fight against the pandemic.
Research led by Richard B. van Breemen from Oregon State’s Global Hemp Innovation Center, College of Pharmacy, and Linus Pauling Institute was published in the Journal of Natural Products on January 10, 2022.
The scientists found that CBGA and CBDA prevented the infection of human epithelial cells by a pseudovirus expressing the SARS-CoV-2 spike protein as well as prevented entry of live SARS-CoV-2 into cells.
THCA also effective
CBGA and CBDA were not the only effective cannabinoid precursors detected in this study. Tetrahydrocannabinolic acid (THCA) also demonstrated potentially high effectiveness, but its legal status as a controlled substance prevented scientists from acquiring sufficient quantities to examine its full potential.
The other observed compounds – Δ9-tetrahydrocannabinol (Δ9-THC), Δ8-tetrahydrocannabinol (Δ8-THC), cannabichromene (CBC), cannabigerol (CBG), cannabinol (CBN), and cannabidiol (CBD) showed only weak or no potential in this study.
So far, we have witnessed numerous results of previous studies in human and animal models, compared to the recorded clinical practice using CBD formulations to treat COVID-19. Before this groundbreaking study, one of the latest findings published in October 2021 in Phytotherapy Research show the potential effects of CBD in counteracting SARS-CoV-2 hyper-inflammation in the gut. The newest findings show that multiple cannabinoids in complex mixtures from plant extracts could act independently to inhibit SARS-CoV-2.
How does it work in the body?
Cell entry inhibitors could be used to prevent SARS-CoV-2 infection and shorten the course of COVID-19 infections by preventing virus particles from infecting human cells. The infection of host cells by SARS-CoV-2 begins with the attachment of the receptor-binding domain (RBD) of the S1 protein to the human cell surface receptor angiotensin-converting enzyme-2 (ACE2), abundant in human lungs, arteries, heart, kidneys, and intestines. When cell entry inhibitors bind to the spike proteins, those proteins are prevented from binding to the ACE2 enzyme. The scientific approach of blocking virus-receptor interactions has also been useful in examining solutions for other viruses, including HIV type 1 and hepatitis C.
The binding of the viral spike protein of SARS-CoV-2 to the host cell receptor ACE2 is seen as a critical step during the infection. For that reason, cell entry inhibitors as CBDA and CBGA could potentially be life-saving solutions for the COVID-19 pandemic. The spike protein is the same target used in COVID-19 vaccines and antibody therapy.
The novel method and its findings
The group of scientists from the Oregon State University, including professor van Breemen, have developed an advanced method of the magnetic microbead affinity selection screening (MagMASS), described in their earlier paper published in the Journal of the American Society for Mass Spectrometry.
During the screening of botanical extracts using MagMASS, extracts of Cannabis Sativa L. produced several hits, with the best results identified with CBGA, THCA-A, and CBDA. Excluding THC-A because of its controlled status, CBDA and CBGA were found to block infection of human epithelial cells by a pseudovirus expressing the spike protein. What is most important, both CBDA and CBGA prevented virus entry into cells even when the scientists used the authentic SARS-CoV-2 virus.
The bioavailability of CBDA and CBGA
The scientists established that the concentrations needed to block infection by 50% of viruses are high but might be achievable. It has already been found that CBDA administered orally to human volunteers at 0.063 mg/kg showed greater bioavailability than CBD. In beagle dogs, oral administration of CBDA at 1 mg/kg was well tolerated, was two-fold more bioavailable than CBD. There is no scientific data for the bioavailability of CBGA yet, but the scientists in this study are optimistic the needed concentration can be achieved.
What is the best way to consume these compounds?
As explained by professor van Breemen in an interview for Vice magazine, when fighting COVID-19, it could be effective to consume CBDA and CBGA in the form of a dietary supplement like a pill or an oil or a gummy just after one gets exposed to a positive person and before becoming severely ill.
”The active compounds we’ve discovered in hemp are cannabidiolic acid, CBD-A, CBG-A, and THC-A. ‘A’ stands for an acid group, a carboxylic acid — this group can be removed upon treatment. So if these hemp products containing these compounds are smoked or vaped, the heat exposure could cause the chemical decomposition or conversion of CBD-A to CBD, CBG-A to CBG, and THC-A to THC. So, we know that CBD, CBG, and THC are not active against the virus. So, we would recommend in favor of an oral administration of these compounds instead of smoking them, inhaling them from vaping,” said professor van Breemen.
The scientists led by professor van Breemen believe that there could even be enhanced effectiveness in using the mixtures compared to individual compounds. There is already strong evidence in favor of the entourage effect theory.
For example, a study on mice conducted by scientists from the University of Sidney and published in the magazine Nature in July 2021 shows that CBDA concentration in mice plasma was 14 times higher when it was administrated from the full-spectrum extract than when it was administrated as a single molecule.
Creating a challenging environment for viral variants
One of the primary concerns of the scientists trying to find a solution in the ongoing pandemic is the spread of viral variants, of which there are many, with some of the most concerning and widespread being the alpha variant (B.1.1.7) and beta variant (B.1.351), both observed in this study. These variants are well known for evading antibodies against early lineage SARS-CoV-2, which is particularly concerning because current vaccination strategies rely on the early lineage spike RBD as an antigen. The scientists hope that this trend will extend to other existing and future variants.
With the widespread use of cannabinoids, resistant variants could still arise, but the combination of vaccination and CBDA/CBGA treatment should create a more challenging environment for the virus, the scientists emphasize.
In addition to promoting public knowledge about CBD and other cannabinoids, at Ilesol Pharmaceuticals, we strongly believe in the importance of providing scientific evidence prior to claiming any possible health benefits, and we, therefore, do not advise our customers or readers of our blog to use any product in the treatment of any illness before it has been approved by the international drug regulatory agencies.