Next Article in Journal
Pt-Free Metal Nanocatalysts for the Oxygen Reduction Reaction Combining Experiment and Theory: An Overview
Previous Article in Journal
Synthesis of Zwitter-Ionic Conjugate of Nido-Carborane with Cholesterol
Previous Article in Special Issue
Cannabis-Derived Compounds Cannabichromene and Δ9-Tetrahydrocannabinol Interact and Exhibit Cytotoxic Activity against Urothelial Cell Carcinoma Correlated with Inhibition of Cell Migration and Cytoskeleton Organization
Article

Role of Caryophyllane Sesquiterpenes in the Entourage Effect of Felina 32 Hemp Inflorescence Phytocomplex in Triple Negative MDA-MB-468 Breast Cancer Cells

1
Department of Physiology and Pharmacology “V. Erspamer”, Sapienza University of Rome, P.le Aldo Moro 5, 00185 Rome, Italy
2
Department of Biochemical Sciences, Sapienza University of Rome, P.le Aldo Moro 5, 00185 Rome, Italy
3
Department of Drug Chemistry and Technologies, Sapienza University of Rome, P.le Aldo Moro 5, 00185 Rome, Italy
*
Authors to whom correspondence should be addressed.
Academic Editors: Hinanit Koltai and Dvora Namdar
Molecules 2021, 26(21), 6688; https://doi.org/10.3390/molecules26216688
Received: 24 August 2021 / Revised: 28 October 2021 / Accepted: 1 November 2021 / Published: 5 November 2021
(This article belongs to the Special Issue Pharmaceutical Drugs Based on Cannabis)
Cannabis sativa L. crops have been traditionally exploited as sources of fibers, nutrients, and bioactive phytochemicals of medical interest. In the present study, two terpene-rich organic extracts, namely FOJ and FOS, obtained from Felina 32 hemp inflorescences collected in June and September, respectively, have been studied for their in vitro anticancer properties. Particularly, their cytotoxicity was evaluated in different cancer cell lines, and the possible entourage effect between nonintoxicating phytocannabinoids (cannabidiol and cannabichromene) and caryophyllane sesquiterpenes (β-caryophyllene, β-caryophyllene oxide and α-humulene), as identified at GC/MS analysis, was characterized. Modulation of cannabinoid CB1 and CB2 receptors was studied as a mechanistic hypothesis. Results highlighted marked cytotoxic effects of FOJ, FOS, and pure compounds in triple negative breast cancer MDA-MB-468 cells, likely mediated by a CB2 receptor activation. Cannabidiol was the main cytotoxic constituent, although low levels of caryophyllane sesquiterpenes and cannabichromene induced potentiating effects; the presence in the extracts of unknown antagonistic compounds has been highlighted too. These results suggest an interest in Felina 32 hemp inflorescences as a source of bioactive phytocomplexes with anticancer properties and strengthen the importance of considering the possible involvement of minor terpenes, such as caryophyllane sesquiterpenes, in the entourage effect of hemp-based extracts. View Full-Text
Keywords: hemp inflorescences; phytocannabinoids; cannabidiol; cannabichromene; β-caryophyllene; β-caryophyllene oxide; α-humulene; chemosensitizing effects; triple negative breast cancer; entourage effect hemp inflorescences; phytocannabinoids; cannabidiol; cannabichromene; β-caryophyllene; β-caryophyllene oxide; α-humulene; chemosensitizing effects; triple negative breast cancer; entourage effect
Show Figures

Graphical abstract

MDPI and ACS Style

Di Giacomo, S.; Mariano, A.; Gullì, M.; Fraschetti, C.; Vitalone, A.; Filippi, A.; Mannina, L.; Scotto d’Abusco, A.; Di Sotto, A. Role of Caryophyllane Sesquiterpenes in the Entourage Effect of Felina 32 Hemp Inflorescence Phytocomplex in Triple Negative MDA-MB-468 Breast Cancer Cells. Molecules 2021, 26, 6688. https://doi.org/10.3390/molecules26216688

AMA Style

Di Giacomo S, Mariano A, Gullì M, Fraschetti C, Vitalone A, Filippi A, Mannina L, Scotto d’Abusco A, Di Sotto A. Role of Caryophyllane Sesquiterpenes in the Entourage Effect of Felina 32 Hemp Inflorescence Phytocomplex in Triple Negative MDA-MB-468 Breast Cancer Cells. Molecules. 2021; 26(21):6688. https://doi.org/10.3390/molecules26216688

Chicago/Turabian Style

Di Giacomo, Silvia, Alessia Mariano, Marco Gullì, Caterina Fraschetti, Annabella Vitalone, Antonello Filippi, Luisa Mannina, Anna Scotto d’Abusco, and Antonella Di Sotto. 2021. "Role of Caryophyllane Sesquiterpenes in the Entourage Effect of Felina 32 Hemp Inflorescence Phytocomplex in Triple Negative MDA-MB-468 Breast Cancer Cells" Molecules 26, no. 21: 6688. https://doi.org/10.3390/molecules26216688

Find Other Styles
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Back to TopTop