CANNABIDIOL (CBD)

In part three we discussed the exciting results of several studies using cannabis ligands for their plaque punching potency in treating inflammation (atherosclerosis) via the CB system. In this final installment we’ll explore the uses of CBD, an amazing phytocannabinoid. Furthermore, CBD may exert some or all of its anti-inflammatory effects outside of these receptors. From Mohanraj Rajesh et al:

Consistently, CBD has been shown to exert anti-inflammatory and antioxidant effects both in vitro (test tube) and in various preclinical models of neurodegeneration and inflammatory disorders, independent from classical CB1 and CB2 receptors [11 citations].

Cannabidiol has been shown to be effective in protecting endothelial function and integrity in human coronary artery endothelial cells (HCAECs). The study demonstrated that CBD reversed the harmful effects of high glucose on HCAECs by inhibiting: Reactive oxygen species production by mitochondria, NF-κB activation, Transendothelial migration of monocytes, Monocyte–endothelial adhesion in HCAECs.[ref]Mohanraj Rajesh et al., Cannabidiol attenuates high glucose-induced endothelial cell inflammatory response and barrier disruption. Am J Physiol Heart Circ Physiol. Jul 2007; 293(1)[/ref]

Cannabidiol (CBD) is not psychoactive due to a low affinity for the CB1 & CB2 receptors[ref]IBID[/ref]. It has been approved for the treatment of inflammation, pain, and spasticity associated with multiple sclerosis in humans since 2005[ref]IBID[/ref].

In what can only be described as astonishing, Mohanraj Rajesh and his team were able to demonstrate that CBD may be the perfect anti-inflammatory for diabetics and cardiac patients. Its healing effects are so broad as to make one question the authenticity of this study. Basically CBD suppressed all of the adverse effects from excess serum blood sugar that they examined such as hyperglycemia induced free radical damage from NF-kB activation, and superoxide formation. Superoxide, a type of free radical, plays a significant role in the pathogenesis of diabetes-associated endothelial dysfunction[ref]IBID[/ref].

We demonstrate that CBD attenuates HG [hyperglycemia]-induced…superoxide generation, NF-κB activation,…and disruption of the endothelial barrier function in [human coronary artery endothelial cells] HCAECs by a mechanism independent from CB1 and CB2 receptors[ref]IBID[/ref].

Considering that over 80% of the American population has fasting blood sugars above the ideal range (83-85 mg/dl), CBD may be a welcome addition to our paucity of anti-inflammatory/diabetic medicines.

In other words this study shows that CBD may behave as an antidote to diabetic hyperglycemic complications, and in those patients with prediabetes or who eat excessive quantities of refined carbohydrate.

In the conclusion of the above study the author’s state: Collectively, our results suggest that the nonpsychoactive cannabinoid CBD have significant therapeutic benefits against diabetic complications and atherosclerosis.

One study indicates that blocking CB2 also decreases inflammation. While scientists elucidate the role of CB2 stimulation leading to a decrease in the inflammatory response in plaque formation, others are finding that blocking the CB2 receptor with CBD leads to a decrease in the immune response. The authors suggest that these findings may lead the way toward development of a new class of anti-inflammatory drugs[ref]British Journal of Pharmacology (2008) 153, 199–215; 2008 Nature Publishing Group[/ref].

Turning now to CBD, an important recent finding is that this cannabinoid displays unexpectedly high potency as a CB2 receptor antagonist and that this antagonism….can ameliorate inflammation…raises the possibility that CBD is a lead compound from which a selective and more potent CB2 receptor inverse agonist [a type of antagonist] might be developed as a new class of anti-inflammatory agent[ref]Br J Pharmacol. Jan 2008; 153(2): 199–215[/ref].

It is outside the scope of this article to list all of the astonishing effects of CBD in the human body. But I’ll give you a hint: they all seem to be helpful! I will run an article soon which demonstrates the vast syllabus of physiological effects from CBD administration. Now let’s see what the critics love to quote when bashing marijuana.

DARK HORSE: CANNABINOIDS AND HEART ATTACK

Just when you thought it was safe to light your spliff, dribble a single malt, and watch The World’s End for the fifth time, there remains a dark horse in the use of pot and heart disease. At least one study is getting plenty of press. They found that pot smoking increases the risk for heart attack within the first hour of smoking[ref]Mittleman MA1, Lewis RA, Maclure M, Sherwood JB, Muller JE. Triggering myocardial infarction by marijuana. Circulation. 2001 Jun 12;103(23):2805-9.[/ref]. Now, before your pants catch fire, I think we can discount the publication. This was a retrospective study involving a questionnaire on frequency of marijuana use (with pot heads no less) which makes it notoriously unreliable.

In summary, I have presented compelling animal, tissue culture, and human studies that strongly support a role for cannabinoids in moderating inflammation in general, and specifically in the treatment of cardiovascular disease which includes stroke, heart attack, and pulmonary embolus, our top killers. Drug companies do not currently have ways to treat chronic inflammation which is one of the reasons why industrialized nations have become so sick. Changing one’s lifestyle, preventing inflammation, is currently our only option. But, that’s a tough sell. We may soon see the day when your family doctor instead tells poor Mabel to smoke hash or try some new darling cannabinoid medication.

That’s why a new cannabinoid anti-inflammatory class of drugs would be embraced. Because of their unique, novel, and powerful, systemic anti-inflammatory actions, these drugs could be applied as antidotes to destructive habits, and environmental toxins that are recognized risk factors. These factors are not just for atherosclerosis but also for cancer, and neurodegenerative diseases like Alzheimer’s disease and Parkinson’s disease which are reaching pandemic proportions.

Furthermore, these novel compounds, and many more just waiting for a fresh, bushy-tailed, research fellow to expose, appear to work far upstream of the inflammatory cascade right into the very heart (pun intended) of cellular inflammation: the suppression of NF-kB. By suppressing NF-kB, a real cure for atherosclerosis could be realized, and with it cures for cancers, neurodegeneration, and a hundred more diseases of affluence. Is this really possible? Indeed. Let me leave you with one of the most profound statements I have come across in my 25 years in clinical medicine and teaching:

…cannabis is a source not only of D9-THC, CBD and D9-THCV but also of at least 67 other phytocannabinoids and as such can be regarded as a natural library of unique compounds. The therapeutic potential of many of these ligands still remains largely unexplored prompting a need for further preclinical and clinical research directed at establishing whether phytocannabinoids are indeed ‘a neglected pharmacological treasure trove’ (Mechoulam, 2005)[ref]Journal of British Pharmacology (2008) 153, 199–215; 2008 Nature Publishing Group[/ref].

Read the first 3 parts of Dr. Rasmussen’s incredible articles here:

– Part 1

– Part 2

– Part 3