CBD – Great Green Hope or Hype?

CBD – Great Green Hope or Hype?
Written by Michele Vieux

The claims and hype surrounding Cannabidiol (CBD) – a type of cannabinoid found in cannabis plants – and its miraculous ability to heal appear to be both extremely significant to those suffering from a myriad of ailments and also quite valid as research is finding. What used to be considered a home remedy, alternative treatment and even a “stoner’s” drug, is becoming more mainstream and less stigmatized.

Although there is still much research to be conducted, what has already been done (mostly from studies overseas) has been extremely promising and is bringing hope to millions because of the wide variety of conditions CBD successfully treats without the toxicity and dangerous side effects of prescription drugs.

Cannabinoid Receptors & Their Function in Our Bodies
To understand how CBD works in our bodies, we must first understand what cannabinoid receptors are and what they do. Cannabinoid receptors, located throughout the body, are part of the endocannabinoid system which is involved in a variety of physiological processes including appetite, pain-sensation, mood and memory. CBD and other components of cannabis can modulate many of these physiological systems in the human brain and body.

Cannabinoid receptors are of a class of cell membrane receptors under the G protein-coupled receptor superfamily that sense molecules outside of the cell and lead to the triggering of responses like increased or decreased: depression, pain, inflammation, and more. We can control the response of these receptors by binding the proper inhibitor or antagonizer – to mute or stimulate them – with cannabinoids like CBD.

Cannabinoids, like CBD and tetrahydrocannabinol (THC), are chemical compounds that trigger cannabinoid (and other) receptors. More than 100 cannabinoids have been identified in the marijuana plant. Of these marijuana molecules, THC and CBD have been studied most extensively.

Just to note, in addition to cannabinoids produced by the plant, there are endogenous cannabinoids (such as anandamide and 2AG) that occur naturally in the mammalian brain and body, as well as synthetic cannabinoids created by pharmaceutical researchers. More to come on these synthetics versus the real deal in another article.

CBD is what we are discussing today. It’s a non-psychoactive component of the marijuana plant that acts by binding with a number of non-cannabinoid receptors and ion channels to create its therapeutic effects. Research indicates that CBD has potent antitumoral, antioxidant, antispasmodic, anti-psychotic, anticonvulsive, antidepressant and neuroprotective properties. So who exactly can benefit from its use and how?

Health Benefits without the High
Let’s dispel any rumors and stigma now. CBD is not a stoner’s drug and you won’t get “high” or create an addiction from using it.(1) It should be considered similar to any other herbal remedy or supplement like turmeric, dandelion root, echinacea, etc. And as you will learn below, CBD is non-addictive and can actually be used to treat addiction.

Most CBD products have little to no THC – the psychoactive cannabinoid in the marijuana plant – as CBD typically comes from the cannabis plant that is bred to contain low levels of THC. CBD is non-psychoactive because it does not act on the same pathways as THC. These pathways, called CB1 receptors, are highly concentrated in the brain and are responsible for the mind-altering effects of THC. In fact, CBD opposes the action of THC at the CB1 receptor, thereby muting the psychoactive effects of THC.(1)

Both CBD and THC have been found to present no risk of lethal overdose, which is important to note since they can be used as painkillers – like traditionally used opioids – which do present overdose risk and risk of death. Because cannabinoid receptors, unlike opioid receptors, are not located in the brainstem areas controlling respiration, lethal overdoses from cannabis and cannabinoids do not occur(3) as does with consumption of high levels of opioids. However, to reduce potential side effects (from THC), medical users may be better off using cannabis with higher levels of CBD. The lack of harmful, and otherwise undesirable, side effects is one of the major benefits of using CBD as medication.

Reduces Inflammation & Pain
CBD actually stops the inflammatory cycle by decreasing the production and release of pro-inflammatory cytokines as well as creating a series of reactions that result in an increased concentration of the anti-inflammatory endocannabinoid, anandamide.(18) This is especially promising for those suffering from chronic pain such as Rheumatoid Arthritis (RA) – a chronic inflammatory disease that is manifested in joint destruction, deformity and loss of function associated with joint stiffness, pain, swelling and tenderness. And osteoarthritis (OA) – characterized by breakdown of the cartilage (the tissue that cushions the ends of the bones between joints), bony changes of the joints, deterioration of tendons and ligaments, and various degrees of inflammation of the joint lining (called the synovium). As well as other inflammatory conditions such as colitis(19) – inflammation of the lining of the gut.

This anti-inflammatory and pain-reducing effect is what I experience when I apply CBD oil directly to my arthritic knee. It can also be effective when dosed in other manners, but that’s a topic for another post in this series.

So who does this hold promise for? Anyone who suffers from debilitating, inflammatory pain!

The 1% of the world’s population who suffer from debilitating RA and are currently on expensive prescription drugs with nasty side effects, may now have a viable option so that they can get out of bed each morning pain-free!

Athletes, former athletes and those who have put their bodies to the physical test and are now suffering the consequences of OA may also benefit from CBD. For me, besides being physically able to participate in the activities I like, it means not popping potentially dangerous amounts of ibuprofen, prescription pain pills or relying on cortisone shots. It also means postponing another surgery until I’m happy with the options available to me.

Sufferers of the extremely painful, inflammatory disease of the digestive tract, colitis, there is hope! Besides reducing the pain caused by inflammation, reducing the inflammation also reduces other symptoms of the disease that can keep you from leaving the comfort of your bathroom like abdominal pain, cramping and diarrhea.(19)

Modulates Bone Density, Blood Pressure & Diabetes
Does osteoporosis run in your family or are you otherwise at risk? CBD can stop you from earning the family hunchback by stopping your body from stealing minerals from your bones by acting to decrease bone resorption.(2)(17)

Peroxisome proliferator activated receptors (PPARs) are a group of three nuclear receptors—PPAR-alpha, PPAR-gamma, and PPAR-delta. PPARs are triggered by hormones, endogenous fatty acids, and various nutritional compounds. When activated, PPARs bind to certain segments of DNA to promote or prevent transcription of specific genes.

Many of the genes regulated by PPARs are involved in energy homeostasis, lipid uptake and metabolism, insulin sensitivity, and other metabolic functions. Big Pharma recognizes the importance of these nuclear receptors. Thus far, two classes of pharmaceutical PPAR activators—fibrates and thiazolidinediones—have been approved by the U.S. Food and Drug Administration.

So besides those prone to osteoporosis, CBD treatments can also be used to treat pre-diabetics and diabetes. What if you didn’t have to poke yourself with needles and use expensive test strips to monitor your blood sugar levels multiple times each day? Most genes regulated by PPARs are involved with lipid metabolism and energy storage. PPAR activation typically promotes glycolysis (glucose breakdown), lipolysis (lipid breakdown), and insulin sensitivity, These properties make PPAR activation a promising treatment for type II diabetes and obesity. (12)

Anti-Cancer Proliferation
CBD exerts an anti-cancer effect by activation of receptors and is able to induce the ability to regress tumors in human lung cancer cell lines.(2)(13) PPAR-gamma activation has demonstrated an anti-proliferative effect as well as an ability to induce tumor regression in human lung cancer cell lines. This receptor is expressed in various types of cancer so it can be used in many treatment plans.(5)(14) However, in some cases PPAR activation can also have an opposite result so more research is necessary.(2)

Even with all the advances in cancer research, up until recently, the treatment options were limited and toxic, i.e., radiation and chemotherapy. They literally kill almost the entire person in hopes of also killing the cancer. The physical side effects – nausea, vomiting, weakness – alone are enough to kill a person or at least make them wish it did. And the psychological effects a person deals with it all is a whole separate battle.

CBD offers both a treatment alternative void of these side effects and possibly one more successful in regressing cancer cells than mainstream methods. It can also be administered with dignity and in the comfort of one’s own home, instead of them having to enter the hospital or treatment center to be hooked up to machines multiple times each week. For those who still aren’t sold, CBD can at least be used in these cases to battle the nausea and vomiting caused by radiation and chemo.

Treats Anxiety, Depression & Alzheimer’s
CBD has shown evidence for improving and even eradicating many conditions of the brain and mind – depression, anxiety, addiction, schizophrenia, Alzheimer’s, Post Traumatic Stress Disorder (PTSD).(6)(7)(10) Research has been done in many areas like the ones listed above and it is still being done in populations with epilepsy, ADHD, concussions and other trauma to the brain, and more. Check out little Charlotte’s story on CNN. And an open letter to NFL Commissioner Roger Goodell from a Professor of Psychiatry at Harvard Medical School urging the NFL to not only lift CBD from its banned substance list, but to fund the research on how CBD can repair the brain after traumatic injury.

Considerable evidence suggests that cannabinoids modulate the behavioral and physiological response to stressful events.(9) Results demonstrate that the endocannabinoid system can be modulated to enhance emotional learning, and suggest that endocannabinoid modulators may be therapeutically useful as adjuncts for exposure-based psychotherapies such as those used to treat PTSD and other anxiety disorders.(6)

Think about how this can be used to treat our combat veterans and others suffering from PTSD, as well as anxiety and depression. In a case report of a 19-year-old male patient with a spectrum of severe PTSD symptoms, such as intense flashbacks, panic attacks, and self-mutilation, who discovered that some of his major symptoms were dramatically reduced by smoking cannabis resin.

Recent studies provide supporting evidence that PTSD patients may be able to cope with their symptoms by using cannabis products because cannabis may dampen the strength or emotional impact of traumatic memories through synergistic mechanisms that might make it easier for people with PTSD to rest or sleep and to feel less anxious and less involved with flashback memories.(11)

More Promising News to Come
If you want to learn more about CBD, including current regulations and laws, stay tuned for more articles in this series over the next few weeks. There is still a lot to examine about CBD, but we believe the potential benefits warrant a discussion amongst health and fitness professionals.

Sources:
1) Adams IB, Martin BR, “Cannabis: pharmacology and toxicology in animals and humans,” Addiction 91 (11): 1585-614, 1996.
2) Ament Z, et al, “Applications of metabolomics for understanding the action of peroxisome proliferator-activated receptors (PPARs) in diabetes, obesity and cancer,” Genome Medicine,” 2012.
3) Bergamaschi, M et al, “Safety and Side Effects of Cannabidiol, a Cannabis sativa Constituent,” Current Drug Safety, 2016.
4) Biscetti F, et al, “Peroxisome proliferator-activated receptors and angiogenesis,” Nutrition, Metabolism & Cardiovascular Diseases, 2009.
5) Chearwae W and Bright JJ, “PPAR-gamma agonists inhibit growth and expansion of CD133+ brain tumour stem cells,” British Journal of Cancer, 2008.
6) Chhatwal JP, “Enhancing cannabinoid neurotransmission augments the extinction of conditioned fear,” Neuropsychopharmachology, March 2005.
7) Costa M, et al, “Investigation of endocannabinoid system genes suggests association between peroxisome proliferator activator receptor-alpha gene (PPARA) and schizophrenia.,” European Psychopharmacology, 2012.
8) Esposito G, et al, “Cannabidiol reduces amyloid beta-induced neuroinflammation and promotes hippocampal neurogenesis through PPAR-gamma involvement,” PLOS One, 2011.
9) Ganon-Elazar E, “Cannabinoids and traumatic stress modulation of contextual fear extinction and GR expression in the amygdala-hippocampal-prefrontal circuit,” Psychoneuroendocrinology, February 2013.
10) Neumeister, A, “The endocannabinoid system provides an avenue for evidence-based treatment development for PTSD”, Depression and Anxiety, 2012.
11) Passie, T et al, “Mitigation of post-traumatic stress symptoms by Cannabis resin: a review of the clinical and neurobiological evidence,” Drug Test Anal., July-August 2012.
12) Penner, E, et al, “The Impact of Marijuana Use on Glucose, Insulin, and Insulin Resistance among US Adults,” The American Journal of Medicine, July 2013
13) Ramer R, et al. “COX-2 and PPAR-gamma confer cannabidiol-induced apoptosis of human lung cancer cells,” American Association for Cancer Research (AARC), 2012.
14) Rovito D, et al, “Omega-3 PUFA ethanolamides DHEA and EPEA induce autophagy through PPARg activation in MCF-7 breast cancer cells,” Journal of Cellular Physiology, 2013.
15) Song M, et al, “Modulation of diabetic retinopathy oathiohysiology by natural medicines through PPAR-g-related pharmacology,”British Journal of Pharmacology, 2012.
16) Sugden M, et al, “PPAR control: it’s SIRTainly as easy as PCG,” Journal of Endocrinology, 2010.
17) Treacy, MP and Hurst, TP, “The case for intraocular delivery of PPAR agonists in the treatment of diabetic retinopathy,” BMC Opthalmology, 2012.
18) Witcamp, R, et al, “The endocannabinoid system: an emerging key player in inflammation,” Curr Opin Clin Nutr Metab Care. 2014 Mar;17
19) Wood JD, Alpers DH, Andrews PL, “Fundamentals of Neurogastroenterology,” Gut. 1999 Sep; 45 Suppl 2():II6-II16.