Slide 3

William Courtney, MD
Candidate for the United States House of Representatives, 2nd District of California

Non-psychotropic plant cannabinoids new therapeutic opportunities from an ancient herb

Issues

Cannabinoid acids are, at least, a conditionally essential dietary element required as an antioxidant/ anti-inflammatory for individuals in the 4th decade and beyond. The ability of Exogenous Eicosanoids to regulate dysfunctional uterine contractions and mitigate pediatric oncologic incidence argue for the designation of Cannabinoid Acids as Essential across the entire life span. I have thousands of patients who are beginning the largest informal clinical trials in the world, regarding the regular use of 600 mg of CBDA & THCa, provided by juicing 17 grams of raw Cannatonic bud and 20-30 green leafs / day on a q.i.d. (5 times a day) schedule.

At ICRS 2008, in Scotland, we learned cannabinoid acids such as THCa, delicate molecules destroyed during preparation of GC analysis, possessed immune modulating capacities lost during the application of heat. The decarboxylation of THCa to THC via heat was the central dogma of medical marijuana. Out of respect for the volatility of the terpenes and the delicate nature of the carboxyl bond, we switched from using dried, encapsulated leaf to fresh-juiced leaf in June 2008.

At the ICRS symposium in June 2009, my wife, Kristen, presented herself as a case study in, Putative Abberation of the Endoginous Cannabinoid System, and was subsequently asked to participate in a patient panel at the International Cannabis As Medicine Conference in Koln, Germany in October of 2009. An audience member was sure he knew why the leaf had such an impact on Kristen’s immune system. Marcel DeWit ,invited us to his home in Rotterdam, where he gave us scientific papers on THCa and International Patents on the Cannabinoid Acids. His passion for non-psychoactive THC Acid resonated with our interest in the whole plant.

Review of DeWit’s literature showed that there was but 90gm/ml neutral THC in the unheated plant, yet after heating the THC increased to 10,060gm/ml. We confirmed that the 14,500 μgm / ml of non-psychoactive THCa was potently active in modulating the immune system, and was tolerated because the 90 μgm / ml of free THC does not cross the CB1 stimulation threshold. Many middle-aged patients cannot tolerate THC, even if it alleviates their symptoms, due to the dysphoria that interferes with their day-to-day functions. Patients become dysphoric on 10-20mg of THC, well before they can take in a full dose (200 to 1,000 mg) of the non-psychoactive cannabinoids. Age or heat decarboxylate THCa to THC, reducing the tolerable dose from 2000 mg to 10 mg, and resulting in the loss of the inflammatory, anti-spasmodic and anti-proliferative activities of the cannabinoids. Until heated, the plant is not psychoactive, therefore it can be consumed as a raw vegetable to provide unique antioxidant and neuroprotective properties.

Armed with this finding, upon my return, I began to consume 60 to 100 times more raw flower than could be tolerated after sautéing, steeping, baking, vaporizing or smoking. To my relief and surprise, the first experiment did not leave me psycho-toxic on THC. Word of mouth spread rapidly amongst patients, friends, and individuals who were becoming asymptomatic with the combination of juiced raw flower and leaf. We have discovered that dietary leaf therapy is a gradual process that increases over the first two months or regular use. Once the plant is absorbed, cannabinoids clear in 50 minutes supporting a q3-4 hour dosing.

The US Patent, held by the United States of America Department of Health and Human Service, US Patent 6, 630,507 B1, clearly identifies clear the dramatic benefit of cannabidiol. This patent, issued in 2003, establishes the medical properties and uses of cannabis. Clearly cannabis does not qualify as a ‘Highly addictive drug with no medical benefit,’ and therefore should be removed from the Convention One Treaty by amendment. US Patent 6,946,150 B2, on Pharmaceutical Formulation, further articulates the range of benefits provided by the cannabinoids of cannabis.

Clearly, exogenous Eicosanoids, synergistic terpenes, and flavioinds comprise a dietary essential only effective at antioxidant levels, i.e. 500 to 1000 mg /day in divided doses, secondary to 50 minute serum clearance after a 2-4 hour absorption. Current pharmaceutical formulations, such as Sativex, frequently use 2-4 sprays, or 2.5 mg THC per spray. Standard usage supplies the classic 10 mg THC dose, which is severely restricted by the psychoactive side effects. The topical, nasal, sublingual, and oral formulations, utilizing pure phtyocannabinoid CBD extracts hold enormous promise. Personally, I would like to be pivotal in providing 6.97 billion daily doses of the Essential Cannabinoid Acids as fresh or fresh frozen juice.

Last fall, we presented in Austria and Israel, and spent time conducting CBD research in Spain and Morocco. Moroccan men live longer than any other men in the world, and we are investigating whether their intake of 40% CBD hash is a contributing factor. We have a contact that is helping to organize the study.

In Israel, Ruth Ross, and her team at the University of Aberdeen, presented one of the most important papers I have seen in six years, Modulation of GPR55 Signally by Phytocannabinoids Measured Using the Alphascreen Assay. Using their assay, they found CBDA and CBGA modulated 2-4 times stronger than CBD and CBG. This provides the first evidence for a structure-activity relationship of cannabis constituents at GPR55. GPR55 is a receptor for the phytocannabinoids found in raw, unheated, fresh cannabis.

In the Israeli paper, Effect of Cannabinoids on Microglial Cells and Their Protective Role in An Animal Model of Multiple Sclerosis, gene array analysis demonstrated that CBD downregulates the expression of many of the LPS-stimulated pro-inflammatory genes, exerting a much greater effect than THC. CBD downregulates 524 genes, while THC downregulates 36; CBD upregulates 681 genes, while THC only 58. We are very interested in using gene array analysis on the cannabinoid acids, especially in light of Ruth Ross’s paper, which showed these acids have a known site of activity and are 200-400% greater than the classic neutral cannabinoids.

In Spain, we had the pleasure of meeting the creator of the Cannatonic cannabis plant strain. Just this month The Werc Lab analyzed 17 Cannatonic samples for us, and found that one had 19.8% CBD. This is the highest CBD content found in a cannabis plant to date, and would allow patients to use significantly less plant material than the current Californian plants.

Cannabis is unique as a food substance in providing highly digestible globular protein, which is balanced for all of the essential amino acids. Cannabis provides the ideal ratio of omega 6 to omega 3 essential fatty acids. Critically, cannabis is the only known source nutritionally significant levels of the essential cannabinoid acids. It is clear that the 1-2 billion individuals living on $1-2 / day would benefit from access to cannabis as a unique functional food. Cannabis International Foundation has set for itself the following sequence of activities: Amend Treaty One; Identification of a hardy broad-profile cannabis plant; High volume seed production (ALMP) and the consequent provision of 1 billion pounds of seed to assist access to this dietary essential that is capable of providing the benefits summarized below in the recent review Non-psychotropic plant cannabinoids: new therapeutic opportunities from an ancient herb, Angelo A. Izzo1,4, Francesca Borrelli1,4, Raffaele Capasso1,4, Vincenzo Di Marzo2,4 and Raphael Mechoulam3.