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.

Role of caryophyllane sesquiterpenes in the entourage effect of felina 32 Hemp inflorescence phytocomplex in triple negative MDA-MB-468 breast cancer cells / Di Giacomo, Silvia; Mariano, Alessia; Gullì, Marco; Fraschetti, Caterina; Vitalone, Annabella; Filippi, Antonello; Mannina, Luisa; Scotto d'Abusco, Anna; Di Sotto, Antonella. - In: MOLECULES. - ISSN 1420-3049. - 26:21(2021), p. 6688. [10.3390/molecules26216688]

Role of caryophyllane sesquiterpenes in the entourage effect of felina 32 Hemp inflorescence phytocomplex in triple negative MDA-MB-468 breast cancer cells

Di Giacomo, Silvia
;
Mariano, Alessia;Gullì, Marco;Fraschetti, Caterina;Vitalone, Annabella;Filippi, Antonello;Mannina, Luisa;Scotto d'Abusco, Anna;Di Sotto, Antonella
2021

Abstract

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.
2021
cannabichromene; cannabidiol; chemosensitizing effects; entourage effect; hemp inflorescences; phytocannabinoids; triple negative breast cancer; α-humulene; β-caryophyllene; β-caryophyllene oxide
01 Pubblicazione su rivista::01a Articolo in rivista
Role of caryophyllane sesquiterpenes in the entourage effect of felina 32 Hemp inflorescence phytocomplex in triple negative MDA-MB-468 breast cancer cells / Di Giacomo, Silvia; Mariano, Alessia; Gullì, Marco; Fraschetti, Caterina; Vitalone, Annabella; Filippi, Antonello; Mannina, Luisa; Scotto d'Abusco, Anna; Di Sotto, Antonella. - In: MOLECULES. - ISSN 1420-3049. - 26:21(2021), p. 6688. [10.3390/molecules26216688]
File allegati a questo prodotto
File Dimensione Formato  
Di Giacomo_Role_2021.pdf

accesso aperto

Tipologia: Versione editoriale (versione pubblicata con il layout dell'editore)
Licenza: Creative commons
Dimensione 2.69 MB
Formato Adobe PDF
2.69 MB Adobe PDF Visualizza/Apri PDF

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11573/1587489
Citazioni
  • ???jsp.display-item.citation.pmc??? 6
  • Scopus 8
  • ???jsp.display-item.citation.isi??? 8
social impact