La especie vegetal Cannabis sativa (Cannabaceae) posee importantes propiedades medicinales gracias a los componentes bioactivos que posee. El fitoestrógeno CBD se puede encontrar en la planta y debido a las características terapéuticas y estructurales de la molécula, lo convierte en un interesante andamio susceptible a numerosas modificaciones sintéticas, con el fin de mejorar su eficacia y potencia terapéutica. Este trabajo proporciona información sobre los distintos análogos sintéticos de CBD descubiertos en los últimos años (2010 - 2021). La búsqueda bibliográfica se realizó en distintas bases de datos, con distintas palabras clave. Dicha búsqueda se limitó a los años 2010 - 2021, y se consideraron revisiones, micro revisiones y meta-análisis de mayor impacto. Se recopilaron alrededor de 40 nuevos análogos sintéticos de CBD y fueron clasificados según el blanco estructural modificado. Estos compuestos poseen una importante bioactividad e incluso, muchos conservan la actividad de su precursor. Sin embargo, en muchos casos, el conocimiento de su mecanismo de acción aún se encuentra en estudio por lo que se necesitan numerosas investigaciones farmacológicas y medicinales.
SeO2 based samples are tested for the oxidation of α-pinene, in liquid phase employing ethanol as the solvent. Commercial SeO2 was tested under both reflux and under 6 atm O2 pressure. At conversion levels of approximately 40%, the yield to myrtenal was much higher in the latter (34.4%) than in the former case (18.0%) due to the high oxidant species availability. Besides the high yield attained at relatively short reaction time. A palladium promoted selenium dioxide supported catalyst (Pd/SeO2/SiO2) was prepared, characterized, and submitted to the catalytic test. Selenium dioxide (14.4%) was strongly fixed to the silica support. Upon the palladium introduction (0.98%), the reducibility of SeO2 is modified, which originates a selenium species activation towards the allylic oxidation. A 12% conversion level is attained over Pd/SeO2/SiO2 following 8 h of reaction time, employing ethanol as the solvent at 134 °C. The main product is myrtenal, being obtained with a selectivity of 62%. Over oxidation products are not detected. The palladium/selenium dioxide sample is easy to handle with and its recuperation following the reaction in liquid phase is possible.
We have previously demonstrated that the endocannabinoid system is dysregulated at synaptic terminals in the cerebral cortex of aged rats, characterized by reduced availability of the neuroprotective endocannabinoid 2-arachidonoylglycerol (2-AG) as a result of im-paired metabolic enzyme activity. This deficit was only partially compensated by canna-binoid receptor (CBR) ligand binding. Given that Δ9-tetrahydrocannabinol (THC) func-tions as a CBR ligand, the present study was designed to determine whether a full-spectrum cannabis extract with high THC content, its THC-free fraction, or pure THC could modulate the age-related dysregulation of 2-AG. Synaptosomes isolated from the cerebral cortex of adult and aged rats were incubated with a full-spectrum extract, a THC-free fraction, or pure THC, together with the corre-sponding radiolabeled substrates to assess 2-AG-metabolizing enzyme activity. Our re-sults demonstrate that the age-related decline in 2-AG bioavailability (a) is exacerbated by either the THC-free fraction or pure THC, primarily due to a significant reduction in 2-AG synthesis, and (b) is partially attenuated through inhibition of 2-AG hydrolysis when the extract contains THC. Consequently, a high-THC full-spectrum extract regulates 2-AG metabolism more effectively than THC alone. These findings support the concept that cannabis phytochemicals act synergistically (the entourage effect) and highlight the therapeutic potential of high-THC extracts for restoring reduced 2-AG levels in the aging brain.
Phytoestrogens are plant compounds which have generated considerable interests. A litany of health benefits including a lowered risk of osteoporosis, heart disease, breast cancer, and menopausal symptoms, are frequently attributed to phytoestrogens but without the knowledge of their side effects. Consequently, the question of whether or not phytoestrogens are beneficial or harmful to human health remains unresolved. Here, we investigate the effects of lipid extracts from the Solanaceae Nicotiana glauca on skeletal muscle cells, in relation to apoptosis. Previously, we evidenced the presence of molecules functional and structurally analogous to 17β-estradiol in extracts of Solanaceaes. We performed extraction and phytochemical screening as per the standard methods of Wagner (1984), using Dragendroff’s, Bornträger´s and Libermann-Burchard’s test. The effects of lipids extracts from N. glauca in C2C12 cells were analyzed by Mitotracker DAPI, TUNEL and immunofluorescence staining and Western blotting. Caspase activity was analyzed with a commercial kit. Opposite to the effects of 17β-estradiol, the crude extract from N. glauca and its sub-extracts obtained by partition, induced apoptosis in C2C12 cells. This apoptotic action involved caspase 3/7 activation. Also, we evidenced that the extracts from N. glauca trigger a rapid defense response in skeletal muscle through Akt and HSP27-phosphorylation. The data reported here, on the effects of lipid extracts from N. glauca on myoblasts suggest that the traditional use of this medicinal plant could affect the skeletal muscle homeostasis.
New triterpenic azines from lupeol exhibited neuroprotective effects in vitro , with 4c notably preventing 6-OHDA- and ferroptosis-induced dopaminergic cell death, highlighting its potential for Parkinson's disease.