Department of Physiology and Pharmacology "V. Erspamer", Sapienza University of Rome, P.le Aldo Moro 5, 00185 Rome, Italy.
Department of Biochemical Sciences, Sapienza University of Rome, P.le Aldo Moro 5, 00185 Rome, Italy.
Molecules. 2021 Nov 5;26(21):6688. doi: 10.3390/molecules26216688.
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.
麻类作物传统上被用作纤维、营养物质和具有医学价值的生物活性植物化学物质的来源。在本研究中，从分别于 6 月和 9 月采集的 Felina 32 大麻花序中获得了两种富含萜类的有机提取物 FOJ 和 FOS，研究了它们的体外抗癌特性。特别评估了它们在不同癌细胞系中的细胞毒性，并通过 GC/MS 分析鉴定出非致幻植物大麻素（大麻二酚和大麻色烯）和石竹烷倍半萜（β-石竹烯、β-石竹烯氧化物和α-葎草烯）之间可能存在的伴生效应。研究了大麻素 CB1 和 CB2 受体的调节作为一种机制假设。结果突出了 FOJ、FOS 和纯化合物在三阴性乳腺癌 MDA-MB-468 细胞中的显著细胞毒性作用，可能由 CB2 受体激活介导。大麻二酚是主要的细胞毒性成分，尽管低水平的石竹烷倍半萜和大麻色烯诱导增效作用；提取物中存在未知拮抗化合物也被强调。这些结果表明，Felina 32 大麻花序作为具有抗癌特性的生物活性植物复合物的来源具有一定的研究价值，并强调了考虑麻基提取物中可能存在的少量萜类物质（如石竹烷倍半萜）在伴生效应中的重要性。
