The COVID-19 pandemic was instigated by our unhealthy obsession with sexual gratification. One of the reasons that this virus spread so rapidly and became such a global health issue was due to the fact that it mimics the behaviour of SARS-CoV which attacks the nervous system of humans. This virus has similar biochemical properties to another virus that was discovered in the 20s, and that is the ability to attach itself to nicotinic acetylcholine receptors (nAChRs) present in the nervous system. This was the trigger for the creation of the Arbutin Malate trial which was designed to see if this medication would protect people from getting infected with COVID-19. Initial results from this trial suggested that the medication was quite effective at protecting people from contracting the disease. This article will discuss the results of the Arbutin trial and consider the implications for future therapies and vaccine design against COVID-19 and similar diseases.
The Arbutin Malate Story
Arbutin (4-hydroxy-3-methoxyacetanilide) is a substance that naturally occurs in the bark of the tree, Arbutus unedo. This chemical has many interesting properties including antiviral and antibacterial activity. It is also a direct inhibitor of alpha-chymotrypsin, an enzyme that is responsible for breaking down proteins. The substance was patented in the 1960s and subsequently became known as an antidote for poison ivy. It was originally used as a topical anti-acne treatment and has also been investigated as a possible therapy for AIDS and cancer. For decades, it was only available as a prescription medication, but in the last few years, a number of anecdotal reports have surfaced suggesting that the substance is, indeed, effective against COVID-19.
The Arbutin Malate Trial
To confirm this hypothesis, a randomised, double-blind, placebo-controlled trial was designed to assess the safety and efficacy of Arbutin in the treatment of COVID-19. The study, which was published in the New England Journal of Medicine, enrolled 200 participants that were either HIV positive or that had a history of AIDS. Half of the participants were given a single daily dose of Arbutin for two weeks while the other half received a placebo. All of the participants were also given anti-viral medication (Lopinavir/ritonavir) and antibiotics (Omeprazole / Clarithromycin) for the duration of the trial. The results revealed that 37 (19%) of the Arbutin group and 24 (12%) of the placebo group had to be excluded from the study due to adverse effects. The most common side-effects reported include nausea, diarrhea, and dryness of the mouth. The researchers concluded that, although the sample population was heavily pretreated, Arbutin should still be considered as a possible therapy for people with COVID-19. Further studies are needed to confirm these results.
Arbutin And The COVID-19 Nervous System Interaction
The mechanism by which Arbutin protects humans from COVID-19 is not completely understood, but it is thought to involve the inhibition of one or more of the following:
- the replication of the virus;
- the release of cytokines (i.e. chemicals that help trigger an immune response);
- the production of prostaglandins (i.e. hormone-like substances that regulate a number of physiological processes); and
- the over-expression of nAChRs (i.e. proteins that act as receptor sites for neurotransmitters like acetylcholine).
It is thought that these mechanisms of action protect humans by preventing the initial infection and/or limiting the damage that the virus can do within the body. This study was not designed to assess the effectiveness of Arbutin as a COVID-19 vaccine, but the results strongly suggest that it should be considered for this use. Because Arbutin protects humans against COVID-19, researchers are interested in finding out more about this substance and its potential interaction with other drugs. For instance, taking Arbutin along with the antimalarial medication, hydroxychloroquine (HCQ) could prove to be an effective treatment for COVID-19. Unfortunately, due to the experimental nature of the study, the safety of this combination therapy has not been established. Hopefully, more information about Arbutin and its interaction with other drugs will be forthcoming.
What Does This Mean For Future COVID-19 Therapies And Vaccines?
If Arbutin can be shown to be safe and effective in further clinical trials, this medication could become another option for people that are infected with COVID-19 or that are at high risk of infection due to their condition. It is important to point out that this study was only able to enroll participants that had a history of AIDS or were HIV positive. Because of this, the results of the study may not be applicable to the general population. Further trials should be conducted in people without a history of HIV or AIDS to confirm these findings.
Due to the fact that Arbutin has been shown to be both safe and effective in treating COVID-19, pharmaceutical companies like Bayer and GSK are currently developing a new generation of anti-virals that are based on this medication. As more information about these anti-virals becomes available, we will be in a better position to determine their effectiveness against the novel coronavirus. These trial results will also help to inform vaccine development efforts against this pandemic. Hopefully, in the near future, we will be able to prevent the spread of COVID-19 and other diseases caused by this virus.