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Cannabigerol (CBG) is one of the major phytocannabinoids present in Cannabis sativa L. that is attracting pharmacological interest because it is non-psychotropic and is abundant in some industrial hemp varieties. The aim of this work was to investigate in parallel the binding properties of CBG to cannabinoid CB1 (CB1R) and CB2 (CB2R) receptors and the effects of the compound on agonist activation of those receptors and of CB1–CB2 heteroreceptor complexes. Using [3H]-CP-55940, CBG competed with low micromolar Ki values the binding to CB1R and CB2R. Homogeneous binding in living cells, which is only technically possible for the CB2R, provided a 152 nM Ki value. Also interesting, CBG competed the binding of [3H]-WIN-55,212-2 to CB2R but not to CB1R (Ki: 2.7 versus >30 μM). The phytocannabinoid modulated signaling mediated by receptors and receptor heteromers even at low concentrations of 0.1–1 μM. cAMP, pERK, β-arrestin recruitment and label-free assays in HEK-293T cells expressing the receptors and treated with endocannabinoids or selective agonists proved that CBG is a partial agonist of CB2R. The action on cells expressing heteromers was similar to that obtained in cells expressing the CB2R. The effect of CBG on CB1R was measurable but the underlying molecular mechanisms remain uncertain. The results indicate that CBG is indeed effective as regulator of endocannabinoid signaling.

Cultivar influence on variability in olive oil phenolic profiles determined through an extensive germplasm survey ResumenDespite the evident influence of the cultivar on olive oil composition, few studies have been devoted to exploring the variability of phenols in a representative number of monovarietal olive oils. In this study, oil samples from 80 cultivars selected for their impact on worldwide oil production were analyzed to compare their phenolic composition by using a method based on LC-MS/MS. Secoiridoid derivatives were the most concentrated phenols in virgin olive oil, showing high variability that was significantly due to the cultivar. Multivariate analysis allowed discrimination between four groups of cultivars through their phenolic profiles: (i) richer in aglycon isomers of oleuropein and ligstroside; (ii) richer in oleocanthal and oleacein; (iii) richer in flavonoids; and (iv) oils with balanced but reduced phenolic concentrations. Additionally, correlation analysis showed no linkage among aglycon isomers and oleocanthal/oleacein, which can be explained by the enzymatic pathways involved in the metabolism of both oleuropein and ligstroside.

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