What is CBD?


Cannabidiol, also known as CBD, belongs to a family of fat-soluble organic compounds called cannabinoids that interact with the human body in fascinating ways. Cannabinoids were originally discovered in the oily resin produced by the Cannabis plant, in tiny nodules called “trichomes” that cover Cannabis inflorescences.

Over 100 cannabinoids have been discovered in Cannabis1. Since their discovery, cannabinoids have also been found in many other plants, animals, and even fungi2 throughout the natural world. We are just beginning to learn what hidden potential these many cannabinoids may offer.

One cannabinoid in particular, Delta-9-tetrahydrocannabinol, or THC, was isolated in 19643 and identified as the “active ingredient”4 in Cannabis. THC produces the intoxicating sensation that many people associate     with the plant. While most other cannabinoids such as CBD do not produce this sensation, they show promise in a variety of therapeutic applications.

Most Cannabis plants produce CBD, but concentrations vary depending on the cultivar. CBD concentrations tend to be very low in Cannabis varieties grown for THC, but can be very high in varieties classified as “hemp,”  which contain low to non-detectable concentrations of THC.

CBD “isolate” is pure crystalline CBD which is used in many CBD products. CBD “isolate” does not always come directly from hemp, but may be derived  from microorganisms like yeast and bacteria, or even from  synthetic laboratory processes.

At Green Earth Medicinals, we focus exclusively on CBD-rich broad-spectrum extract for several reasons, chiefly through our belief that a broad-spectrum profile containing many other phytochemicals, including additional cannabinoids, terpenes, and flavonoids, contributes to a beneficial “entourage effect.” In CBD therapy, as with so many things in life, the whole is greater than the sum of its parts.
 

CBD and the Body


It has taken scientists many years and countless hours of diligent research, but we are finally beginning to understand the complex ways in which cannabinoids contribute to our wellbeing. Our bodies naturally produce their own cannabinoids, termed “endocannabinoids.” Endocannabinoids are responsible for signaling our cells to perform various metabolic functions.

In school we learned about the basic systems of the human body — the nervous system, the circulatory system, the immune system, etc. We learned that each system is composed of distinct body parts that perform specific functions that keep our bodies alive. For instance, the circulatory system includes the heart, arteries, veins, and capillaries, and its job is to deliver nutrients and oxygen to our cells, and then to remove waste materials.

Scientists have recently discovered a new body system, termed the “Endocannabinoid System,” or ECS. Understanding how the ECS functions is crucial to developing a full appreciation of the potential benefits of CBD. The ECS is composed of three primary elements. The first piece includes microscopic proteins called “receptors” that are embedded in the membranes of our cells. These receptors protrude from our cell membranes like tiny antennae. Their job is to bind to passing cannabinoids.

Cannabinoids are the second piece of the ECS. They act as messenger molecules that stimulate or suppress cellular activities. The ECS also includes many enzymes responsible for building and breaking down cannabinoids.

To add to the complexity, we have two primary types of endocannabinoid receptors, termed CB1 and CB2. CB1 receptors are located primarily in brain cells, but also in some peripheral tissues. CB1 receptors affect appetite, muscle control, pain, cognition, thermoregulation, and stress response. CB1 receptors are responsible for the intoxicating effects of THC, as well as short-term memory loss, allowing  to ‘forget’ the experience of pain or trauma. CB1 receptors can regulate nervous system function and pain response by modulating the relationship between two specific neurotransmitters, glutamate and GABA.

Meanwhile, CB2 receptors are primarily found throughout the immune system. They also exist in the gastrointestinal system, brain and peripheral nervous system, as well as the skin and other organs and tissues. CB2 activation is associated with immune function and immune cell proliferation, inflammation, and pain response5.

As part of its close association with the immune system, CB2 plays a vital role in two essential processes with potentially profound implications for wellness: autophagy and apoptosis. These terms refer to the cleaning of cellular debris and the programmed death of unneeded or malfunctioning cells in our bodies.

Now, here is the tricky part: Unlike THC, CBD does not bind very well to the body’s cannabinoid receptors. In fact, it doesn’t bind to CB1 receptors at all, and very little to CB2. Rather than binding to receptors on its own, CBD functions to increase the presence of the body’s5,6,7 own endocannabinoids. Your body’s endocannabinoids, namely anandamide and 2-AG, then go on to aid in the regulation of nervous and immune system responses.

CBD also binds with other receptors outside of the endocannabinoid system. Here are some examples:

  • CBD binds with Adenosine8,9 receptors, which are associated with heart rate and blood pressure regulation.
  • CBD binds with Vanilloid10 receptors, which are associated with sensations of pain and heat.
  • CBD binds with Serotonin11 receptors, which are associated with heart rate and mood.
  • CBD binds with PPAR Gamma12, 13 receptors, which are located in the membranes of the nuclei inside our cells and are associated with insulin sensitivity and blood sugar regulation.

Inflammation is at the root of many chronic conditions, and CBD can help regulate inflammatory response14. CBD has also shown promise in the treatment of epilepsy, Tourette’s syndrome, PTSD, acne, and mood disorders, among others.

Commonly reported adverse effects associated with CBD include drowsiness, lethargy, and mild    gastrointestinal issues15. Large doses of CBD may be contraindicated for people with compromised immune systems, among other conditions. CBD at high concentrations affects the liver’s capacity to metabolize many common drugs, including drugs like blood thinners and chemotherapy drugs, so it is vital that such patients work with physicians who are familiar with the benefits and limitations of CBD therapy.

There are many ways to ingest CBD, including:

  • Smoke/Vape - When CBD is smoked or vaped, absorption is immediate and systemic, but not always the best choice when targeted relief is desired, and it can be very difficult to standardize dosage.
  • Sublingual - When CBD oil is held under the tongue, it is absorbed directly into the blood through the mucous membranes in the mouth. As with smoking or vaping, sublingual administration has a rapid, systemic effect.
  • Oral - When CBD is swallowed, it first must be metabolised via the liver before it is distributed into the bloodstream, requiring significantly more time before onset.
  • Topical - CBD is fat-soluble, and therefore has difficulty penetrating the skin to reach blood vessels located in the dermis. Efficacy of topical CBD is greatly increased with the addition of “carrier” phytochemicals that increase skin permeability.
  • Other Methods - CBD can also be administered via injection or suppository in consultation with a qualified practitioner.

The Art of CBD Formulation

A CBD extract derived from Cannabis contains many more active botanical compounds than CBD isolates do. We use the term “broad spectrum” to describe the presence of other minor cannabinoids, terpenes, and flavonoids present in the hemp extracts used in our products. Broad-spectrum extracts such as ours have much greater long-term efficacy rates than those made from CBD isolate.16

Terpenes are aromatic compounds found throughout nature that impart flavors and aromas to plants. For instance, a terpene called limonene lends a lemony scent to many citrus plants and culinary herbs. A terpene called pinene gives many evergreens their refreshing pine forest fragrance.

Cannabis is a fantastic source of terpenes. These aromatic compounds contribute more than just the characteristic aromas associated with various Cannabis cultivars. Terpenes interact with cannabinoids and our ECS in ways that we are only just starting to understand scientifically.

The addition of certain terpenes to topical CBD formulas is particularly essential because they act as skin penetration enhancers that allow CBD to penetrate the outer layer of skin to the blood vessels and cannabinoid receptors located in the dermis. A particularly effective terpene for this purpose is limonene, which we include in the form of tangerine extract in our CBD Relief topical line.

Flavonoids are another crucial set of compounds found in the Cannabis plant that are not found in CBD isolates. Flavonoids are antioxidants that contribute to cellular health by scavenging harmful free radicals. Just as they protect the body from unnecessary harm, flavonoids prevent cannabinoids and terpenes from oxidizing or degrading over time.

Finally, we at Green Earth Medicinals enhance our CBD products with additional beneficial botanicals. Informed by diligent research and many hours of clinical experience, our physician formulators combine CBD with other ingredients designed to maximize the efficacy of each product.
 


Citations:

  1. Pertwee, R (2014). Handbook of Cannabis. Oxford: Oxford University Press
  2. Pacioni, G (2015). Truffles contain endocannabinoid metabolic enzymes and anandamide. Phytochemistry, 110, 104-110.
  3. Gaoni, Y., & Mechoulam, R. (1964). Isolation, Structure, and Partial Synthesis of an Active Constituent of Hashish. Journal of the American Chemical Society, 86 (8), 1646–1647.
  4. Mechoulam, R. & Gaoni, Y. (1965). A Total Synthesis of dl-Δ1-Tetrahydrocannabinol, the Active Constituent of Hashish. Journal of the American Chemical Society, 87 (14), 3272-3275.
  5. Cabral, G. A. & Griffin-Thomas, L. (2009). Emerging Role of the CB2 Cannabinoid Receptor in Immune Regulation and Therapeutic Prospects. HHS Author Manuscripts.
  6. Laprairie, R. B. et. al. (2015). Cannabidiol is a negative allosteric modulator of the cannabinoid CB1 receptor. British Pharmacological Society Journals.
  7. Elmes, M. W. et.al. (2015). Fatty acid-binding proteins (FABPs) are intracellular carriers for Δ9-tetrahydrocannabinol (THC) and cannabidiol (CBD). Journal of Biological Chemistry, 14, 8711-21.
  8. Deutsch, D. G. (2016). A Personal Retrospective: Elevating Anandamide (AEA) by Targeting Fatty Acid Amide Hydrolase (FAAH) and the Fatty Acid Binding Proteins (FABPs). Front Pharmacol 13, 7:370.
  9. Ianotti, R et. al. (2014). Nonpsychotropic Plant Cannabinoids, Cannabidivarin (CBDV) and Cannabidiol (CBD), Activate and Desensitize Transient Receptor Potential Vanilloid 1 (TRPV1) Channels in Vitro: Potential for the Treatment of Neuronal Hyperexcitability. American Chemical Society, 5 (11), pp 1131–1141.
  10. Russo, E. B. et. al. (2005). Agonistic Properties of Cannabidiol at 5-HT1a Receptors. Neurochemical Research 30 (8), 1037-1043.
  11. Esposito, G et. al. (2011). Cannabidiol Reduces Aβ-Induced Neuroinflammation and Promotes Hippocampal Neurogenesis through PPARγ Involvement.
  12. Sun, Yan & Bennet, A. (2007). Cannabinoids: A New Group of Agonists of PPARs. PPAR Research.
  13. Burstein, S (2015). Cannabidiol (CBD) and its analogs: a review of their effects on inflammation. Bioorganic and Medicinal Chemistry, 23 (7), 1377-1385.
  14. Iffland, K. and Grotenherman, F. (2017). An Update on Safety and Side Effects of Cannabidiol: A Review of Clinical Data and Relevant Animal Studies. Cannabis and Cannabinoid Research 2 (1).
  15. Galilly, R et. al. (2015). Overcoming the Bell-Shaped Dose-Response of Cannabidiol by Using Cannabis Extract Enriched in Cannabidiol. Pharmacology & Pharmacy, 6 (2).