Introducción. El fraccionamiento fitoquímico de Valeriana pavonii, especie vegetal nativa utilizada tradicionalmente en Colombia con fines tranquilizantes, condujo al aislamiento e identificación de la isovaleramida, uno de los principios responsables de su actividad sobre el sistema nervioso central como anticonvulsivo. Objetivo. Reportar la identificación de la isovaleramida, metabolito de V. pavonii activo sobre el sistema nervioso central. Materiales y métodos. La purificación de la isovaleramida se realizó mediante técnicas cromatográficas. Su estrucutra se determinó por experimentos de resonancia magnética y espectrometría de masas. Se emplearon las pruebas de convulsión máxima inducida eléctricamente en ratones como ensayo farmacológico in vivo y el ensayo in vitro de unión al sitio de las benzodiacepinas sobre el receptor GABA-A. Resultados. En el modelo de convulsión máxima inducida eléctricamente en ratones, la isovaleramida, aislada de la fracción más activa de V. pavonii, confirió un índice de protección de 90% en una dosis de 100 mg/kg, por vía oral, comparable al agente de referencia utilizado: fenitoína sódica (20 mg/kg, por vía oral, 100%) y superior al control (vehículo, 20%). En el ensayo in vitro, la isovaleramida presentó un 42% de inhibición del sitio de unión de flunitracepam con tritio. Conclusión. La isovaleramida es uno de los principios activos anticonvulsivos de V. pavonii, por primera vez reportado en esta especie. Estos resultados dan soporte al uso tradicional de V. pavonii y a su interés como fuente de principios útiles en terapéutica.
Context: Treatments for neurodegenerative diseases generate multiple adverse effects and do not reverse the progressive damage of the disease. It is a priority to find alternatives from medicinal plants as a source of molecules with neuroprotective potential. Caenorhabditis elegans as an in vivo screening model allows evaluating and selecting molecules with neuroprotective activity. Aims: To carry out a systematic review between the years 2010-2021, on traditionally used plant resources with potential neuroprotective activity evaluated in C. elegans. Methods: The review was carried out in 4 stages according to the PRISMA methodology. 1. Research question approach and objectives to define the thematic axes and create the search algorithm. 2. Search of ScienceDirect, Scopus, PubMed, Web of Science, Ebsco, Taylor and Francis and Scielo databases, 3. Selection of articles according to inclusion and exclusion criteria. 4. Organization of information relevant to the review. Results: The search yielded 122 articles, defining 12 base articles for the construction of the review. The extracts in dichloromethane, butanol, ethanolic and aqueous stand out; as well as iridoid and flavonoid type biocompounds. Antioxidant activity was the most cited. Among the neuroprotective effects in C. elegans transgenic strains, the increase in the percentage of survival of nematodes, reduction of paralysis, inhibition of protein aggregation and regulation of genes associated with stress stand out. Conclusions: The identification of bioactive molecules and extracts obtained from medicinal plants of traditional use with neuroprotective potential, is favored by the use of C. elegans as a model for the study of neurodegenerative diseases.
Context: Valeriana pavonii Poepp. & Endl. (Caprifoliaceae), is a plant used in traditional medicine as a tranquilizer in Colombia. Valerian extracts have been widely used since ancient times for their sedative and anxiolytic properties; however, the way its active metabolites, including iridoids, interact on their respective targets is not fully understood. Aims: To isolate and identificate active iridoid esters from V. pavonii. Perform in vitro inhibition assays and computational analyses to study their possible interaction on the benzodiazepine site of the GABAA receptor. Methods: Two compounds were obtained from dichloromethane and petroleum ether fractions of V. pavonii, respectively, by chromatographic techniques. The structural elucidation was performed by NMR and spectroscopic analyses. In vitro inhibition assays of the binding of 3H-flunitrazepam (3H-FNZ) for the benzodiazepine binding site of the GABAA receptor (BDZ-bs of the GABAA receptor) were carried out. Results: Two iridoid esters, hydrine-type valepotriates (compounds 1 and 2), were reported for the first time in V. pavonii. Both iridoids, 1 and 2, inhibited the binding of 3H-FNZ on the BDZ-bs of the GABAA receptor (40% at 300 µM). Docking studies and MMGBSA calculations revealed that these compounds exhibited molecular interactions with crucial residues of the benzodiazepine site, similar to those observed for drugs like flunitrazepam, diazepam, and flumazenil. Conclusions: These findings contribute to understanding the in vivo activity of extracts of Valeriana pavonni on the central nervous system, which showed promising effects, especially as anticonvulsants, sedative-hypnotics, and antidepressants, through the modulation of the GABAergic system by hydrine-type valepotriates and its derivatives.
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