An analgesic compound 30 times more powerful than aspirin is produced in cannabis


They target inflammation at the source, making them ideal pain relievers

Are flavonoids the next step in research? Once considered by lawmakers to be a purely recreational drug, cannabis now has real medical potential, especially when it comes to helping patients relieve pain. New research in the journal Phytochemistry suggests that this relieving ability comes from some lesser-known chemicals in the plant which have real potential to form the basis of non-addictive pain relievers of the future.

Let's put aside for a moment the CBD and terpenes, it seems that the next big constant evolution in the world of research is going to be flavonoids.

"Flavonoids" are chemicals found in all plants (not just cannabis), which are responsible for the pigment in fruits and vegetables. This is not the case with all flavonoids, however, other functions have been of interest to researchers for some time, since many flavonoids have been shown to have antioxidant properties. This is the main reason why people say we must ” eat by color  And, quite often, when an unsuspecting plant is labeled a "superfood" it has something to do with its flavonoids.

Cannflavins exhibit 30X greater anti-inflammatory activity than aspirin

In the study publié, researchers at the University of Guelph showed how two molecules called: cannflavin A et cannflavin B (discovered in 1985) exhibit anti-inflammatory activity thirty times higher to that of aspirin.

Even for those familiar with the cannabis science landscape, cannflavin A and cannflavin B, which belong to the flavonoid family, can be unfamiliar names. However, this flavonoid is already raising hopes that one day we may have a whole new way to treat the pain.

But this news is not really new. The potential analgesic powers of cannflavins were first discovered by Marilyn Barrett, a researcher at the Faculty of Pharmacy at the University of London, in the 1980s. So why haven't we heard more about edible cannabis like a new superfood? Because cannflavins make up a tiny amount of plant material, and a huge amount would have to be consumed for it to work as an effective anti-inflammatory.

Cannflavines are present in about 0,014 percent of the fresh weight of the plant.

"This is very characteristic of many natural products that have therapeutic value," says Tariq Akhtar, assistant professor in the Department of Molecular and Cellular Biology at the University of Guelph. You can't just cultivate fields and expect to get enough bioactive compounds out of them, because the amounts are so low and hard to come by due to their complex chemical nature. It is possible to extract and purify them, but it is not economically viable. "


Thanks to Akhtar and his colleagues, Dr Steven Rothstein, Dr José Casaretto and lead author Kevin Rea, there is finally a solution to these light flavonoids. Using the 'in silico' extraction of the genome, the team identified the cannabis genes responsible for making the cannaflavins in question, allowing metabolic engineering of cannaflavin A and B to be achieved without culturing the whole plant. .

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With the help of the University of Guelph, the process was quickly patented. Shortly afterwards, a medical cannabis company, Anahit International, licensed the patent to explore commercial product development. Of course, it is still too early to make big statements about the potential impact of their work, but given the crisis in opioids, the possibility of another method of pain treatment is really exciting.

“What's interesting about cannabis molecules is that they stop inflammation at the source,” Akhtar says. “And most natural products don't have the toxicity associated with over-the-counter pain relievers, which, while very effective, carry health risks. So looking at natural products as an alternative is a very attractive model. "

La heavy consumption of anti-inflammatory drugs nonsteroidal drugs (NSAIDs) and other over-the-counter pain relievers is associated with an increased risk of kidney disease (ibuprofen) and stomach problems (acetylsalicylic acid). Even pain relievers, such as acetaminophen, if used excessively and in combination with alcohol, can lead to liver problems. Given all of this (combined with the devastation drug companies have left with their aggressive marketing of opioids), one wonders why no one jumped on Marilyn Barrett's original cannflavin discovery in the 1980s.

The answer ? Well, the development of in silico computer technology has helped but the main reason for the delay is that cannabis research has been blocked due to the legal status of the plant. It's not just about the logistics needed for a university to agree to allow marijuana plants in campus labs, it's also about finding the funding to explore a so-called "illegal" substance.

We would not have been able to do this without the current climate in this country which is really pushing people like us to do this research. There is still a lot of research to be done and I think that working in Canada right now, at a time when our government has really supported this program and where there is a lot of industrial and financial support available to do research in this area opens up very interesting prospects.

He adds: “Especially for old smothered professors like me in a field like plant biochemistry. "

As part of this study, the team examined the genome and biochemistry of cannabis to identify the genes responsible for the production of the two cannflavins as well as the chain of chemical reactions that produce them. This is the first time that this biological process has been documented for cannabis stakeholders.

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Akhtar and his team hope this will help scientists develop alternatives to opioids for patients with acute or chronic pain, not by interacting with the opioid receptors in the brain, but by reducing inflammation at the site. pain.

For now, the most scientific and popular attention is on Δ9-tetrahydrocannabinol (THC) and cannabidiol (CBD), two of the most abundant active molecules in cannabis by volume. Known for its psychoactive properties, THC may help treat chronic pain, but it has also been linked to psychosis with frequent and excessive use. CBD, on the other hand, is the active ingredient in Epidiolex, the first cannabis drug. FDA approved for infantile convulsive disorders, but its long-term side effects are poorly understood and the pseudo drug too expensive.

If they can be synthesized in sufficient quantity, cannflavins A and B could become equally well known. Akhtar and several of his co-authors have applied for a US patent for the possible results of this research, so given the thorny regulatory backdrop for CBD, they could potentially benefit from a new class of CBD-derived products. cannabis that are not hampered by the stigma and stigma associated with drugs.

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Summary: In addition to the psychoactive constituents generally associated with Cannabis sativaL., there are many other specialized metabolites in this plant that are believed to contribute to its medicinal versatility. This study focused on two of these compounds, called cannflavin A and cannflavin B. These prenylated flavonoids specifically accumulate in C. sativa and are known for their potent anti-inflammatory activity in various animal cell models. However, almost nothing is known about their biosynthesis. By combining phylogenomic and biochemical approaches, an aromatic prenyltransferase from C. sativa(CsPT3) which catalyzes the regiospecific addition of geranyl diphosphate (GPP) or dimethylallyl diphosphate (DMAPP) to the methylated flavone, chrysoerol, to produce cannflavins A and B, respectively. Additional evidence is presented for an O-methyltransferase (CsOMT21) encoded in the genome of C. sativa which specifically converts the flavone from the widely distributed plant known as luteolin to chrysoerol, both of which accumulate in C. sativa . These results therefore imply the following reaction sequence for the biosynthesis of cannflavins A and B: luteolin ► chrysoerosol ► cannflavin A and cannflavin B. Together, the identification of these two unique enzymes represents a branching point of the flavonoid pathway. generals at C. sativa. and provide an easy path to metabolic engineering strategies designed to produce these two medicinal cannabis compounds.

Tags : Pain killerAnti-inflammatoryflavonoidopioidsSearch

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