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

<i>Cannabis sativa</i> 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...

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Autores principales:	Silvia Di Giacomo, Alessia Mariano, Marco Gullì, Caterina Fraschetti, Annabella Vitalone, Antonello Filippi, Luisa Mannina, Anna Scotto d’Abusco, Antonella Di Sotto
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	hemp inflorescences phytocannabinoids cannabidiol cannabichromene β-caryophyllene β-caryophyllene oxide Organic chemistry QD241-441
Acceso en línea:	https://doaj.org/article/b4845da87d0d446d875061557c81b1fc
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spelling	oai:doaj.org-article:b4845da87d0d446d875061557c81b1fc2021-11-11T18:38:33ZRole of Caryophyllane Sesquiterpenes in the Entourage Effect of Felina 32 Hemp Inflorescence Phytocomplex in Triple Negative MDA-MB-468 Breast Cancer Cells10.3390/molecules262166881420-3049https://doaj.org/article/b4845da87d0d446d875061557c81b1fc2021-11-01T00:00:00Zhttps://www.mdpi.com/1420-3049/26/21/6688https://doaj.org/toc/1420-3049<i>Cannabis sativa</i> 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.Silvia Di GiacomoAlessia MarianoMarco GullìCaterina FraschettiAnnabella VitaloneAntonello FilippiLuisa ManninaAnna Scotto d’AbuscoAntonella Di SottoMDPI AGarticlehemp inflorescencesphytocannabinoidscannabidiolcannabichromeneβ-caryophylleneβ-caryophyllene oxideOrganic chemistryQD241-441ENMolecules, Vol 26, Iss 6688, p 6688 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	hemp inflorescences phytocannabinoids cannabidiol cannabichromene β-caryophyllene β-caryophyllene oxide Organic chemistry QD241-441
spellingShingle	hemp inflorescences phytocannabinoids cannabidiol cannabichromene β-caryophyllene β-caryophyllene oxide Organic chemistry QD241-441 Silvia Di Giacomo Alessia Mariano Marco Gullì Caterina Fraschetti Annabella Vitalone Antonello Filippi Luisa Mannina Anna Scotto d’Abusco Antonella Di Sotto Role of Caryophyllane Sesquiterpenes in the Entourage Effect of Felina 32 Hemp Inflorescence Phytocomplex in Triple Negative MDA-MB-468 Breast Cancer Cells
description	<i>Cannabis sativa</i> 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.
format	article
author	Silvia Di Giacomo Alessia Mariano Marco Gullì Caterina Fraschetti Annabella Vitalone Antonello Filippi Luisa Mannina Anna Scotto d’Abusco Antonella Di Sotto
author_facet	Silvia Di Giacomo Alessia Mariano Marco Gullì Caterina Fraschetti Annabella Vitalone Antonello Filippi Luisa Mannina Anna Scotto d’Abusco Antonella Di Sotto
author_sort	Silvia Di Giacomo
title	Role of Caryophyllane Sesquiterpenes in the Entourage Effect of Felina 32 Hemp Inflorescence Phytocomplex in Triple Negative MDA-MB-468 Breast Cancer Cells
title_short	Role of Caryophyllane Sesquiterpenes in the Entourage Effect of Felina 32 Hemp Inflorescence Phytocomplex in Triple Negative MDA-MB-468 Breast Cancer Cells
title_full	Role of Caryophyllane Sesquiterpenes in the Entourage Effect of Felina 32 Hemp Inflorescence Phytocomplex in Triple Negative MDA-MB-468 Breast Cancer Cells
title_fullStr	Role of Caryophyllane Sesquiterpenes in the Entourage Effect of Felina 32 Hemp Inflorescence Phytocomplex in Triple Negative MDA-MB-468 Breast Cancer Cells
title_full_unstemmed	Role of Caryophyllane Sesquiterpenes in the Entourage Effect of Felina 32 Hemp Inflorescence Phytocomplex in Triple Negative MDA-MB-468 Breast Cancer Cells
title_sort	role of caryophyllane sesquiterpenes in the entourage effect of felina 32 hemp inflorescence phytocomplex in triple negative mda-mb-468 breast cancer cells
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/b4845da87d0d446d875061557c81b1fc
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Role of Caryophyllane Sesquiterpenes in the Entourage Effect of Felina 32 Hemp Inflorescence Phytocomplex in Triple Negative MDA-MB-468 Breast Cancer Cells

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