31 August 2020

What is caryophyllene and what are its effects in cannabis?

Beta-Caryophyllene, also known as caryophyllene or (−)-β-caryophyllene is a non-psychoactive compound found in Cannabis. Due to its intense aroma, which evocates that of pepper and wood and its sweet and dry taste, β-caryophyllene is widely used both in the cosmetic industry and as a food additive. It exhibits low water solubility; making it harder for the human body to absorb.

Plants that are abundant in Caryophyllene

As a volatile component of many plants’ essential oils (EO), including that of Cannabis Sativa L. (where it represents up to 37% of the cannabis flower’s EO), Cloves (Syzygium aromaticum– 1.7–19,5%), Hops (5.1–14.5%) and Rosemary (0.1–8.3%). This aromatic compound is a member of the terpene family, and more precisely, it is a “bicyclic sesquiterpene” (1). It is usually the overall dominant terpene in cannabis extracts, particularly if they have been processed through decarboxylation (heat treatment or oxidation).

In nature, it occurs together with small amounts of its variants (called “isomers”), which include (Z)-β-caryophyllene (or iso-caryophyllene) and α-humulene (also named as α-caryophyllene), as well as with its oxidation derivative β-caryophyllene oxide (BCPO).

The Entourage Effect of Beta-Caryophyllene

β-caryophyllene activity is potentiated by cannabinoids such as THC and CBD, which synergistically interact with each other, thus creating an entourage effect. Specifically, CBD seems to potentiate the β-caryophyllene activity against inflammation and addiction, while THC’s action promotes the interaction between β-caryophyllene and CB2 receptors.

The medicinal properties of Beta-Caryophyllene

  • Antimicrobial
  • Antileishmanial
  • Antimalarial
  • Local anaesthetic
  • Spasmolytic-anticonvulsant activities

It has also been reported to partly act as an agonist of the CB2 receptor, which represents a therapeutic target for the treatment of:

  • Inflammation
  • Pain
  • Atherosclerosis
  • Inflammatory-based diseases, including colitis, cerebral ischemia and brain inflammation.

It shows a potent anti-inflammatory effect, comparable to that of phenylbutazone (a powerful non-steroidal anti-inflammatory drug). Furthermore, it has been recently shown to possess cancer-preventive properties and – when administered in combination with anticancer drugs – displayed a sensitizing power (5) on cancer cells resistant to anti-cancer drugs.

It was also found to be able to interfere with the targeted signalling pathways involved in inflammation and cancer. β-Caryophyllene demonstrated a beneficial effect on colitis, osteoarthritis, diabetes, anxiety and depression, liver fibrosis and Alzheimer-like disease types.

More importantly, it shows to have a good oral absorption; therefore, it would provide an important medicinal benefit to oral cannabis preparations. Sensitization reactions are quite rare, and if they occur, are probably due to its oxidized product BCPO.

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