Topical Endocannabinoid System Interactions – CBG & CBG

What is the Endocannabinoid System?

Endogenous cannabinoid system > endocannabinoid system > ECS

The ECS is an essential biological modulatory system that regulates and communicates with other systems in the body to maintain homeostasis.

Homeostasis: a self-regulating process by which biological systems maintain stability while adjusting to changing external conditions. 

The ECS is composed of cannabinoid receptors, endogenous cannabinoids (endocannabinoids), and the enzymes responsible for the synthesis and degradation of the endocannabinoids.

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Cannabinoid receptors:

There are two well characterised cannabinoid receptors with distinct physiological properties. The CB1 receptor is mainly located in the central nervous system and mediates most of the psychoactive effects of cannabinoids, whereas the CB2 receptor is mainly located in the immune system and peripheral tissues. The CB2 is principally involved in anti-inflammatory and immunosuppressive actions.

CB1: “The brain receptor for cannabinoids”, which outnumbers many of the other receptor types on the brain. They control the levels and activity of most of the other neurotransmitters with an immediate response, turning up or down the activity of whichever system needs to be adjusted, such as hunger, temperature, or alertness.

CB2: “The body receptor for cannabinoids”. It is mainly expressed in immune tissues and has been shown to modulate immune cell functions, both in cellulo and in animal models of inflammatory diseases. This suggests that therapeutic strategies aiming at modulating CB2 signalling could be promising for the treatment of various inflammatory conditions. A particularly interesting feature of CB2 receptors is that they appear to be highly inducible, with expression in CB2 increasing up to 100 fold following tissue injury or during inflammation.

Endogenous Cannabinoids (Endocannabinoids): 

Endocannabinoids are produced by almost every organism in the animal kingdom. They are natural endogenous ligands produced by human and animal organisms that bind to cannabinoid receptors. 

Ligand: something that binds with a biological molecule to form a complex and produce some effect. In neuroscience, ligand frequently refers to substances that bind to receptors.

Function of the endocannabinoid system:

The core function of the ECS is maintaining homeostasis within the body. It does this via interaction with fundamental biological systems such as the endocrine system, immune system, digestive system, and central nervous system. Disruption of the ECS is implicated in various inflammatory conditions.

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Historic use of cannabis – phytocannabinoid medicines

As early as 2737 B.C. the mystical Emperor Shen Neng of China was prescribing cannabis tea for the treatment of gout, rheumatism, malaria and, oddly enough, poor memory. The drug’s popularity as a medicine then spread throughout Asia, the Middle East and down the eastern coast of Africa, and certain Hindu sects in India used cannabis for religious purposes and stress relief. Ancient physicians prescribed cannabis for everything from pain relief to earache to childbirth. It’s thought that the main reason for the therapeutic properties of cannabis, now and throughout history, is the interaction between phytocannabinoids and the ECS. The most abundant phytocannabinoids are delta-9-Tetrahydrocannabinol (THC), which is the main psychotropic cannabinoid, and cannabidiol (CBD), but over 120 phytocannabinoids have been discovered so far within the plant. 

Cannabinol (CBN) was the first of the plant cannabinoids (phytocannabinoids) to be isolated, from an oil extract of cannabis, at the end of the 19th century, 1899. A second phytocannabinoid, cannabidiol (CBD), was later isolated in 1940, followed shortly after by THC in 1942. CBG was later discovered in 1964. Since then, despite the prohibition status of cannabis, there has been continued study in the field of research regarding the effects of phytocannabinoids on the human body and the therapeutic potential of compounds such as CBD, cannabigerol (CBG), and THC.

What Are CBD/CBG & How Are They Different To THC?

Cannabidiol (CBD), cannabigerol (CBG) and Tetrahydrocannabinol (THC) are phytocannabinoid compounds from the cannabis plant. CBD, CBG, and THC (and all other plant cannabinoids) occur naturally in an acidic form, titled CBDA, CBGA, and THCA respectively. The first phytocannabinoid acid to develop is CBGA, which then breaks down into the various other phytocannabinoid acids we have discovered, namely CBDA and THCA. For this reason, CBG is often referred to as the grandfather cannabinoid, mother cannabinoid, or other such parental nicknames. All cannabinoids start as CBG, or perhaps more accurately, CBGA.

The key difference between THC and our two focus cannabinoids, CBD & CBG, stems from the extent to which they engage the CB1 receptor and therefore elicit a psychoactive or psychotropic response in the human brain. The CB1 receptor is the primary cannabinoid receptor in the brain, and thus all cannabinoids which engage with the CB1 receptor are known as psychoactive or psychotropic.

Not all psychoactive substances are psychotropic but all psychotropic substances are psychoactive.

Psychoactive: Psychoactive drugs are substances that, when taken in or administered into one’s system, affect mental processes, e.g. perception, consciousness, cognition or mood and emotions.

Psychotropic: Psychotropic drugs have effects on psychological function. They include antidepressant agents, hallucinogens and tranquillising agents (including antipsychotics and anti-anxiety agents).

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CBD and the ECS

CBD is a non-psychotropic compound found in the cannabis plant. It interacts with the ECS in several ways, including activating receptors, inhibiting enzymes, and modulating endocannabinoid signalling. One of the primary ways that CBD interacts with the ECS is by inhibiting the breakdown of anandamide, an endocannabinoid that plays a crucial role in pain sensation and mood regulation.

Research has shown that CBD can reduce pain and inflammation by interacting with the ECS. A 2015 study found that topical CBD application can help reduce inflammation and pain in rats with arthritis. The researchers suggested that CBD’s effects were due to its ability to interact with the ECS, specifically by reducing the levels of inflammatory cytokines.

CBD may also have potential in treating skin conditions such as acne, psoriasis, and eczema. A study published in the ‘Journal of Clinical Investigation’ found that CBD can inhibit the production of sebum, a waxy substance that can cause acne. Additionally, CBD has been shown to reduce inflammation and itching in people with eczema.

CBG and the ECS

CBG is a non-psychotropic cannabinoid found in the cannabis plant. It interacts with the ECS by binding to CB1 and CB2 receptors and inhibiting the uptake of anandamide. CBG also acts as a partial agonist for the 5-HT1A receptor, which is involved in mood regulation.

Research on CBG’s potential therapeutic benefits is still in the early stages. However, studies have shown that CBG may have neuroprotective properties and could potentially be used to treat conditions such as Huntington’s disease and multiple sclerosis.

CBG may also have potential in treating glaucoma, a condition that can cause vision loss due to increased pressure in the eye. A study published in the ‘Journal of Glaucoma’ found that CBG can reduce intraocular pressure, a common symptom of glaucoma.

Combining CBD and CBG

While CBD and CBG have their unique interactions with the ECS, some researchers believe that combining the two may enhance their therapeutic benefits. This is because CBD and CBG can work synergistically to provide a more comprehensive range of therapeutic effects.

A study published in the journal ‘Cannabis and Cannabinoid Research’ found that combining CBD and CBG can enhance the anti-inflammatory effects of both compounds. The researchers suggested that this combination could potentially be used to treat conditions such as inflammatory bowel disease.

Another study published in the journal ‘Medicines’ found that combining CBD and CBG can enhance the analgesic effects of both compounds. The researchers suggested that this combination could potentially be used to treat chronic pain.

Potential Benefits of Topical CBD and CBG

  1. Anti-inflammatory Effects: CBD and CBG have been shown to possess anti-inflammatory properties, which may help in reducing inflammation and redness of the skin. This can be beneficial for individuals with inflammatory skin conditions such as acne, eczema, and psoriasis.
  2. Antioxidant Effects: CBD and CBG are known to have antioxidant properties, which can help neutralise free radicals and protect the skin from oxidative stress. This may result in anti-aging effects, helping to reduce the appearance of wrinkles and fine lines on the skin.
  3. Antibacterial Effects: CBD and CBG have shown potential antibacterial properties, which may help in fighting against bacteria that can cause skin infections. This can be beneficial for individuals with acne-prone skin or other bacterial skin conditions.
  4. Neuroprotective Effects: CBD and CBG have been found to possess neuroprotective properties, which may help protect nerve cells from damage and promote nerve regeneration. This may be beneficial for individuals with conditions such as neuropathic pain or nerve-related skin conditions.
  5. Pain Relief: CBD and CBG may interact with receptors involved in pain perception, potentially offering pain-relieving effects when applied topically. This can be beneficial for individuals with localised pain.

Conclusion

CBD and CBG are two compounds found in the cannabis plant that interact with the ECS. CBD interacts with the ECS by inhibiting the breakdown of anandamide, while CBG interacts with the ECS by binding to CB1 and CB2 receptors and inhibiting the uptake of anandamide. Both CBD and CBG have shown potential therapeutic benefits, including anti-inflammatory, analgesic, and neuroprotective properties. Combining CBD and CBG may enhance their effects and provide a more comprehensive range of benefits.

Topical application of CBD and CBG has gained attention due to its potential for localised relief. When applied topically, CBD and CBG can interact with the ECS in the skin and underlying tissues, potentially providing targeted relief for various skin conditions, pain, and inflammation. Additionally, topical application allows for localised application without the risk of systemic effects, making it a preferred method of use for some individuals.

However, it’s important to note that research on CBD, CBG, and their interactions with the ECS is still in the early stages, and more studies are needed to fully understand their mechanisms of action and potential therapeutic benefits.

In conclusion, CBD and CBG are two compounds found in the cannabis plant that interact with the ECS and have shown potential therapeutic benefits. Their topical interactions with the ECS may provide localised relief for various conditions, and combining CBD and CBG may enhance their effects. Research is ongoing and we expect to discover more about their mechanisms of action and safety profile.

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