It doesn't get any better than sour, according to Dr. Mechoulam

“Originally, there are only acids that appear in the plant, and those acids are a mysterious world of compounds that are much more powerful than cannabinoids.” So said the world’s most renowned cannabis researcher, Dr. Raphael Mechoulam, who died in Israel in March of this year at the age of 92. This statement formed the basis of his research. 

The acid forms were considered by Dr. Mechoulam to be the most powerful cannabinoids. The big problem is that they are very unstable . CBDa for example decarboxylates largely into CBD before it can be used therapeutically. 

CBDa (cannabidiolic acid) and THCa (tetrahydrocannabinolic acid) are usually the main cannabinoids of the cannabis plant and are the precursors to the stable and decarboxylated CBD and THC. Except of course the CBG strains, which mainly contain only CBGa (cannabigerolic acid). 

The instability of cannabinoid acids such as CBDa still poses an obstacle to its development as a medicine .

CBDa, a cannabinoid acid with therapeutic promise

The cannabis plant has over 140 cannabinoids, with hundreds of terpenes, flavonoids and other components. The effects of most of these are unknown and have not even been researched.

CBDa is one of the most common cannabinoids currently being studied and has shown great potential in terms of potential therapeutic benefits.

What you need to know is that only CBGa (cannabigerolic acid) can be formed by the plant itself. That is why it is also called 'the mother of all cannabinoids' .

The CBDa, CBCa and THCa are then formed by an enzymatic conversion of the CBGa during flowering in the cannabis plant.

Previously, the acid forms of cannabinoids such as CBDa, CBGa, CBCa, and THCa were thought to be pharmacologically inactive and unable to affect the body’s endocannabinoid system like their decarboxylated counterparts CBD, THC, CBG, and CBC. They were therefore not studied for their potential pharmacological effects, unlike the decarboxylated forms. 

Cannabinoids are the engine and terpenes/flavonoids are the steering wheel and accelerator

What we should certainly not forget is that the terpenes and flavonoids in the plant are essential for the “medicinal” effect , and are partly responsible for the so-called entourage effect of cannabis.                       

“Whole plant extracts consisting of all these components are superior to isolates and distillates”

I sometimes explain it like this: the cannabinoids are the engine and the terpenes & flavonoids are the steering wheel and accelerator with which we can give the car the direction and its speed. That is why it is such a waste to decarboxylate (heat) the cannabinoids. In doing so, we largely destroy the terpenes and flavonoids that are present at that time and the car has become uncontrollable.

The pure, fresh cannabinoids have a completely different “medicinal” effect than the decarboxylated form. But the decarboxylation process cannot be stopped and is not only done by heating the product, but also by LIGHT and TIME. 

In other words, if we leave the extract as it is produced in the plant, there will ALWAYS be a portion that is naturally decarboxylated. This means that the final extract will contain both forms, including the other hundreds of unique components of the cannabis plant that make the “ medicinal ” effect superior.

“ If you look at a field of cannabis, none of the plants actually contain THC and CBD, they contain THCa and CBDa. THC and CBD only appear in the plant after the plant has died.”

What can the cannabis consumer actually do with CBDa?

Recent scientific studies and research indicate that full -spectrum CBDa has enormous potential. We will take a closer look at some of its promises.                                                   

Anti-inflammatory effect of CBDa

Due to its properties as a specific Cox-2 inhibitor CBDa has anti-inflammatory and pain-relieving properties and can be very effective in reducing inflammation and pain.

Ibuprofen and aspirin are examples of nonsteroidal anti-inflammatory drugs (NSAIDs) that are designed to block the action of these Cox enzymes.

CBDa is a selective Cox-2 inhibitor that blocks the Cox enzymes  blocks without the risk of seriously damaging the stomach lining and intestines. In other words: “CBDa works in the same way as drugs, but without the adverse effects and risk of overdose”.

Nausea

Studies indicate that CBDa full-spectrum extracts – together with other cannabinoids – can help reduce vomiting and nausea caused by chemotherapy in cancer patients.

CBDa is up to 1,000 times more effective than CBD!

CBD and CBDA both affect serotonin receptors , but CBDa does so at a much higher rate.

Antiepileptic effects of CBDa 

Epidiolex , a CBD-based medication , is the first prescription drug approved by the US FDA for the treatment of epilepsy.

Epidiolex – Manufacturer GW Pharmaceuticals conducted tests that pitted the effects of CBDa and CBD against each other. Their research showed that smaller doses of CBDa were needed for effectiveness, and in several cases, CBDa performed significantly better than CBD in reducing seizure frequency.

Julian S. Gangolli is the former CEO of GW Pharmaceuticals. “We had children who were having 40 or 50 seizures a week, and this product ( Epidiolex) did very little to improve that,” Gangolli said, describing Epidiolex’s Phase 3 clinical trials. 

He said the increased potency of cannabis acid synthesis allows for the use of treatments derived from it to treat a “huge range of inflammatory conditions,” especially compared to his previous experience with Epidiolex .

CBDa has shown great potential by exhibiting anti-epileptic activity, as supported in thispublication .

Cancer

While they say cannabinoid acids can't cure cancer, there are few molecules that are as effective at slowing and slowing the spread of cancer. According to a recent publication in the journal Toxicology Letters , some cannabinoids like CBDa can hinder the spread of breast cancer cells .

This means there is potential to provide therapeutic benefits, especially if this is done in conjunction with the naturally occurring terpenes and flavonoids in the plant, which in my view are crucial.

Despite these encouraging reports, we are still unable – due to legal requirements – to obtain concrete results. 

Antiviral Activity of CBDa & CBGa Against SARS-CoV-2

In this current study (28-07-2023), the antiviral activity of various cannabinoids was assessed in vitro against all SARS-CoV-2 variants and other viruses. It indicates that CBDa and CBGa are active.

CBDa and other cannabinoid acids ALWAYS decarboxylate gradually over HEAT, LIGHT and TIME.

This unstoppable decarboxylation has prevented it from receiving sufficient attention to be deployed as a viable clinical treatment.

However, Dr. Raphael Mechoulam, announced at the 2019 CannMed conference that he and a group of other scientists have found a way to stabilize CBDa so that it would retain its therapeutic potential.

To solve the instability problem of CBDa, a CBDa methyl ester was tested for its antiviral activity for the first time. This CBDa methyl ester showed a neutralizing effect on all tested SARS-CoV-2 variants.

In vitro stability was confirmed by ultra-high-performance liquid chromatography (UHPLC) analysis combined with high-resolution mass spectrometry (HRMS).

Furthermore, the ability of both CBDa and its derivative to interact with the virus spike protein was assessed. These results demonstrated that CBDa methyl ester can be considered as a lead compound that can be further developed as a novel effective drug against (all) viruses. 

These developments are certainly positive. But if they were to be registered as official “medicine”, they would often immediately become outrageously expensive compared to the real full-spectrum cannabis extracts, which often work much better as a “food supplement”. 

The costs for reimbursement of Epidiolex , for example, vary per patient from €30,000 to €50,000 per year. 

Is CBDa psychoactive?

CBDa can give a feeling of calm and relaxation, but certainly does not provide the “high” and psychoactivity that THC weed does.

How to best consume CBDa?

CBDa cannot be smoked or vaporized in its natural form, as this will convert the CBDa into CBD. However, you can very well use the fresh (CBD) buds and leaves raw in a salad, or a smoothie of freshly squeezed cannabis juice to make.

You can also make tea from fresh cannabis buds with a high CBDa content. Simply put, you have to put them in a cup and let them steep.

And nowadays there are also full-spectrum extracts with a high CBDa percentage for sale. This does not seem to be a problem if we look at the many advertisements  may believe, but unfortunately that is usually not the case and it is almost always a regular CBD product with traces of CBDa in it. 

A big exception are the CBDa dominant full-spectrum extracts of CBD Spain Medicinal Food who in 2016 developed an extraction method in which the unstable cannabis acids remain unprecedentedly stable. And that for many years, whereby almost all natural terpenes and flavonoids present in the plant are simultaneously extracted and preserved.

In other words: “All cannabinoid acids, terpenes and flavonoids as present in the cannabis plant are extracted from the plant simultaneously and in one go during CBD Spain's unique extraction process without the  “change its composition, whereby the unwanted chlorophyll and waxes are NOT included.” 

Extracts bound to specific cannabis species (strain)

These extracts are therefore always 'strain-bound', because each strain has its own unique composition of terpenes, flavonoids and cannabinoids - which therefore also have a unique "medicinal" effect. 

That being said, it is therefore of great importance that the strains used are as uniform as possible in terms of composition of terpenes, flavonoids and cannabinoids, otherwise the “medicinal” effect will always be different. 

Partly because of this statement, the use of seeds is strongly discouraged, as each seed has its own unique components and composition. 

To solve this problem, it is best to work with clones from a “mother plant” so that you can reproduce a cannabis extract with the same composition year after year. 

A great example of this is the “Charlottes´ Web”, a CBD Strain from the Stanley Brothers, who used their “mother plant” from 2014 still have them for a year, and now make millions of clones per year from that same mother plant.

Cannaflavins as an extra

What makes CBD Spain extracts even more potent is the fact that even cannaflavins A, B and C are extracted from the cannabis plant with their extraction method and are abundantly present in all our extracts. 

These cannaflavins are unique to the cannabis plant and have an unprecedented pharmacological effect. They are 30 times stronger than aspirin and are even used as medication for pancreatic cancer .

Pancreatic cancer is a particularly deadly form of cancer, claiming more than 90% of its victims within five years of diagnosis. It is resistant to most standard therapies, including surgery, chemotherapy, radiation therapy, immunotherapy, and targeted therapy, and metastasizes early, often before diagnosis. Only very localized tumors are curable.

Now, however, a new cannabis derivative called FBL-03G shows promise in killing cancer cells in a treated tumor and in other distant parts of the body. FBL-03G is a unique cannabis flavonoid, a synthetic derivative of cannaflavin B.

“May 17, 2023 – Flavocure Biotech, Inc. (“Flavocure”) today announced that it has received approval from the U.S. Food and Drug Administration for its Investigational New Drug (IND) application to initiate a Phase I, first-in-human clinical trial with caflanone (FBL-03G) for the treatment of pancreatic cancer.”

The cannabinoid acids CBGa, THCa and CBCa are almost the same story, but that's for next time.

Peter Vermeul