Better pain relief: Scientists synthesize potent anti-inflammatory compound found in cannabis

Cannabis has been used for millennia to treat pain, inflammation, and a variety of other ailments. But only in more recent years have we begun to understand which chemicals in the plant are responsible for that therapeutic benefit.

In work partly conducted at the Canadian Light Source (CLS) at the University of Saskatchewan, researchers have discovered a way to recreate in the lab a rare compound found in cannabis, which shows promise as an anti-inflammatory drug.

Plant biochemist Tariq Akhtar and his colleagues at the University of Guelph have been studying some of the less-studied compounds found in cannabis, such as cannabistilbene – one of a group of molecules (bibenzyls) believed to offer relief from acute and chronic inflammation.

“If you look through the literature there’s precedent for this molecule and other related molecules for being potent anti-inflammatories, so that piqued our interest and we decided to explore it a little more,” he says.

The problem is that these potentially helpful compounds are only present in tiny amounts in the plants: An acre of cannabis would yield just 21 milligrams of cannabistilbene, says Akhtar, making it “totally impractical” to harvest naturally. This molecule is also very challenging to synthesize using traditional chemistry approaches.

So, Akhtar and his team set out to find a method for identifying enzymes that can synthesize the compound more efficiently, to test its potential as an anti-inflammatory.

“Nowadays with advances in biotechnology if we know what the molecule is and how it is built, we can put the parts together in clever ways to manufacture molecules in a more efficient way than the plant does,” he says.

They started with a common plant molecule called resveratrol which they used as a “scaffold,” then looked for enzymes that could transform it into cannabistilbene. They found two enzymes – one from cannabis and one from a bacterium – that enabled them to create the molecule in a test tube, with no plants required. They published their results in the Journal of Natural Products.

The powerful X-ray light at the CLS was important in the research, as it allowed the team to see how the first enzyme modifies the molecule precisely at a single position, says Matthew Kimber, a structural biologist at the University of Guelph who was part of the project.

“It also sets the stage for potentially engineering these enzymes to make them more efficient,” he said.

Testing in mice revealed that the synthetic cannabistilbene does indeed have some promising anti-inflammatory properties, blocking two different molecular pathways that can cause inflammation. This dual-inhibition function makes cannabistilbene more effective than nonsteroidal anti-inflammatory drugs (NSAIDs), which could be a major help for people living with inflammatory pain, says Akhtar.

“For most people suffering from acute and chronic inflammation there’s really only one line of therapy, over-the-counter painkillers like Tylenol and Aspirin which are effective but also come with significant side effects for many patients,” he says. “So, there is an interest in developing natural products that can do the job just as effectively.”

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Boddington, Kelly F., Eric Soubeyrand, Kristen Van Gelder, Colby Perrin, Taylor JB Forrester, Jennifer Holborn, José A. Casaretto et al. "Cell-Free Synthesis of Cannabistilbene I: A Dual Acting Anti-Inflammatory from Cannabis sativa." Journal of Natural Products (2026). https://doi.org/10.1021/acs.jnatprod.6c00318

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Greg Basky
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Canadian Light Source
306-370-9446
greg.basky@lightsource.ca