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Article

In Silico and In Vitro Analysis of Major Cannabis-Derived Compounds as Fatty Acid Amide Hydrolase Inhibitors

1
Department of Experimental Medicine, Tor Vergata University of Rome, Via Montpellier 1, 00121 Rome, Italy
2
Department of Medicine, Campus Bio-Medico University of Rome, Via Alvaro del Portillo 21, 00128 Rome, Italy
3
Department of Chemistry “G. Ciamician”, University of Bologna, Via Selmi 2, 40126 Bologna, Italy
4
Department of Biotechnological and Applied Clinical Sciences, University of L’Aquila, Via Vetoio snc, 67100 L’Aquila, Italy
5
European Center for Brain Research/IRCCS Santa Lucia Foundation, Via del Fosso di Fiorano 54, 00143 Rome, Italy
*
Authors to whom correspondence should be addressed.
Molecules 2021, 26(1), 48; https://doi.org/10.3390/molecules26010048
Received: 9 December 2020 / Revised: 21 December 2020 / Accepted: 22 December 2020 / Published: 24 December 2020
(This article belongs to the Special Issue Pharmaceutical Drugs Based on Cannabis)
Accumulated evidence suggests that enhancing the endocannabinoid (eCB) tone, in particular of anandamide (N-arachidonoylethanolamine, AEA), has therapeutic potential in many human diseases. Fatty acid amide hydrolase (FAAH) is a membrane-bound enzyme principally responsible for the degradation of AEA, and thus it represents a relevant target to increase signaling thereof. In recent years, different synthetic and natural compounds have been developed and tested on rat FAAH, but little is known of their effect on the human enzyme. Here, we sought to investigate six major cannabis-derived compounds to compare their action on rat and human FAAHs. To this aim, we combined an in silico analysis of their binding mode and affinity, with in vitro assays of their effect on enzyme activity. This integrated approach allowed to disclose differences in efficacy towards rat and human FAAHs, and to highlight the role of key residues involved in the inhibition of both enzymes. This study suggests that the therapeutic efficacy of compounds targeted towards FAAH should be always tested in vitro on both rat and human enzymes. View Full-Text
Keywords: cannabinoids; docking; endocannabinoids; FAAH; inhibition; modeling cannabinoids; docking; endocannabinoids; FAAH; inhibition; modeling
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MDPI and ACS Style

Criscuolo, E.; De Sciscio, M.L.; Fezza, F.; Maccarrone, M. In Silico and In Vitro Analysis of Major Cannabis-Derived Compounds as Fatty Acid Amide Hydrolase Inhibitors. Molecules 2021, 26, 48. https://doi.org/10.3390/molecules26010048

AMA Style

Criscuolo E, De Sciscio ML, Fezza F, Maccarrone M. In Silico and In Vitro Analysis of Major Cannabis-Derived Compounds as Fatty Acid Amide Hydrolase Inhibitors. Molecules. 2021; 26(1):48. https://doi.org/10.3390/molecules26010048

Chicago/Turabian Style

Criscuolo, Emanuele, Maria L. De Sciscio, Filomena Fezza, and Mauro Maccarrone. 2021. "In Silico and In Vitro Analysis of Major Cannabis-Derived Compounds as Fatty Acid Amide Hydrolase Inhibitors" Molecules 26, no. 1: 48. https://doi.org/10.3390/molecules26010048

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