Abstract
The primary objective of this study was to evaluate the effect of the natural product pterostilbene on enzymes responsible for the catabolism of endocannabinoids. Previous studies in our laboratory have established an anxiolytic effect of pterostilbene. The current study evaluated the compound for binding to CNS target receptors involved in anxiety. The study revealed no significant interaction of ptersotilbene with GABA, serotonin, or cannabinoid receptors. In an attempt to clarify the mechanism underlying the in vivo anxiolytic action of pterostilbene, the compound was evaluated for potential inhibition of FAAH and MAGL, enzymes primarily responsible for degradation of endocannabinoids. Results revealed that pterostilbene exerted a concentration dependent inhibition of the human recombinant FAAH enzyme, with an IC50 value of 5.42 ± 0.26 μM, with no significant inhibition of the MAGL enzyme. These results suggest that pterostilbene has the potential to become a candidate compound for therapeutic drug development for anxiety disorders.
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