Abstract
BackgroundMultiple therapeutic properties have been attributed to Cannabis sativa. However, further research is required to unveil the medicinal potential of Cannabis and the relationship between biological activity and chemical profile.ObjectivesThe primary objective of this study was to characterize the chemical profile and antioxidant properties of three varieties of Cannabis sativa available in Uruguay during progressive stages of maturation.MethodsFresh samples of female inflorescences from three stable Cannabis sativa phenotypes, collected at different time points during the end of the flowering period were analyzed. Chemical characterization of chloroform extracts was performed by 1H-NMR. The antioxidant properties of the Cannabis sativa extracts, and pure cannabinoids, were measured in a Cu2+-induced LDL oxidation assay.ResultsThe main cannabinoids in the youngest inflorescences were tetrahydrocannabinolic acid (THC-A, 242 ± 62 mg/g) and tetrahydrocannabinol (THC, 7.3 ± 6.5 mg/g). Cannabinoid levels increased more than twice in two of the mature samples. A third sample showed a lower and constant concentration of THC-A and THC (177 ± 25 and 1 ± 1, respectively). The THC-A/THC rich cannabis extracts increased the latency phase of LDL oxidation by a factor of 1.2–3.5 per μg, and slowed down the propagation phase of lipoperoxidation (IC50 1.7–4.6 μg/mL). Hemp, a cannabidiol (CBD, 198 mg/g) and cannabidiolic acid (CBD-A, 92 mg/g) rich variety, also prevented the formation of conjugated dienes during LDL oxidation. In fact, 1 μg of extract was able to stretch the latency phase 3.7 times and also to significantly reduce the steepness of the propagation phase (IC50 of 8 μg/mL). Synthetic THC lengthened the duration of the lag phase by a factor of 21 per μg, while for the propagation phase showed an IC50 ≤ 1 μg/mL. Conversely, THC-A was unable to improve any parameter. Meanwhile, the presence of 1 μg of pure CBD and CBD-A increased the initial latency phase 4.8 and 9.4 times, respectively, but did not have an effect on the propagation phase.ConclusionCannabis whole extracts acted on both phases of lipid oxidation in copper challenged LDL. Those effects were just partially related with the content of cannabinoids and partially recapitulated by isolated pure cannabinoids. Our results support the potentially beneficial effects of Cannabis sativa whole extracts on the initial phase of atherosclerosis.
Highlights
Cannabis has been used for medicinal purposes for centuries (Pain 2015)
The quantification of phytocannabinoids was performed from specific signals in the 1H-Nuclear Magnetic Resonance (NMR) spectra, which in deuterated chloroform appeared between 5.5–6.8 ppm (Fig. 3)
A progressive increase during maturation of tetrahydrocannabinolic acid (THC-A) was observed in the varieties SB, and Mag with R2 values of 0.89 and 0.46, respectively; while the increase of THC was only significant for SB (R2 = 0.79)
Summary
Cannabis has been used for medicinal purposes for centuries (Pain 2015). Current changing legal frameworks concerning cannabis (Gould 2015) must come together with scientific data to support the scope of therapeutic benefits and risks, providing rigorous knowledge to the medical community and decision makers.Inflammation is part of a protective response given by the immune system. Cannabis has been used for medicinal purposes for centuries (Pain 2015). Macrophages and neutrophils produce oxygen and nitrogen derived oxidants (Iles and Forman 2002). These molecules are involved in relevant signaling and defense processes (Brüne et al 2013), if inflammation persists, intracellular and extracellular molecules will become oxidized, leading to endothelial dysfunction and tissue damage (Mittal et al 2014). Multiple therapeutic properties have been attributed to Cannabis sativa. Further research is required to unveil the medicinal potential of Cannabis and the relationship between biological activity and chemical profile
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