Table A2.
Selected Cannabis sativa L.-derived terpenes, their targets, mechanisms of action, and potential resultant pharmacological effects.
| Targets | Mechanisms of Action | Potential Pharmacological Effects | References |
|---|---|---|---|
| Caryophyllene | |||
| CB2 | Agonist | Analgesic ** Chemotherapy-induced peripheral neuropathy attenuation ** Anti-inflammatory ** Steatohepatitis protecting ** Metabolic dysregulation attenuation ** |
[201,202,203,204,205,206,207] |
| PPAR-α | Agonist | Intracellular lipid modification * Steatohepatitis protecting * |
[207] |
| PPAR-γ | Agonist | Intracellular lipid modification * Steatohepatitis protecting * |
[207] |
| MAPK | Inhibitor Agonist |
Chemotherapy-induced peripheral neuropathy attenuation ** Anti-cancer * |
[206,208] |
| TLR4 | Inhibitor | Microglial activation inhibition ** Neuroprotective *,** Anti-inflammatory *,** |
[209,210] |
| Limonene | |||
| 5-HT-1A | Agonist | Anti-stress ** Anxiolytic ** Anti-depressant ** |
[211] |
| TRPA1 | Agonist | Analgesic ** | [212] |
| NFκB | Inhibitor | Anti-inflammatory **,*** Analgesic ** Colitis reduction ** |
[213,214] |
| A2A | Agonist | Not reported | [215] |
| FTase | Inhibitor | Anti-cancer *** | [216] |
| Pinene | |||
| MAPK NFκB |
Inhibitor | Anti-inflammatory ** | [217] |
| ERK/AKT | Agonist | Anti-cancer *,** | [218] |
| Virus particle (not further specified) |
Inhibitor | Anti-viral * | [219] |
| Myrcene | |||
| TRPV1 | Agonist | Analgesic * | [220] |
| A2A | Agonist | Analgesic ** | [221] |
| Linalool | |||
| A1A | Agonist | Analgesic ** | [222] |
| A2A | Agonist | Analgesic ** | [222] |
| GABA-A | Agonist | Anxiolytic ** | [223] |
| Cancer cell (not further specified) |
Inhibitor | Anti-cancer *,** | [224] |
* Pre-clinical in vitro study. ** Pre-clinical in vivo study. *** Clinical study. N.B.: This table is non-exhaustive, broadly elucidating selected compounds and some of their potential pharmacological effects currently present in the pre-clinical literature. Depending on study parameters, the compounds show differing, sometimes biphasic, affinities and effects at different targets, thus highlighting the contradictory and equivocal evidence state. For a more extensive review on terpene mechanisms of actions and pharmacological effects, see these extensive reviews on the subject: Goncalves et al. [225], Liktor-Busa et al. [226], and Odieka et al. [33,71]. Abbreviations: 5-hydroxytryptamine receptor 1A (5-HT-1A); adrenergic receptor alpha-1 (A1A); adrenergic receptor alpha-2 (A2A); cannabinoid receptor 2 (CB2); Extracellular-regulated kinase/serine/threonine kinase (ERK/AKT); Farnesyltransferase (FTase); gamma-aminobutyric acid type A receptor(GABA-A); mitogen-activated protein kinase (MAPK); Nuclear factor kappa B (NFκB); peroxisome proliferator-activated receptor alpha/gamma (PPAR-α/γ); Toll-like receptor 4 (TLR4); transient receptor potential cation channel type A1 (TRPA1); transient receptor potential vanilloid type 1 (TRPV1).