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Context: Salvia semiatrata Zucc. (Lamiaceae) is a species used as a tranquilizer and to relieve pain in folk medicine in Santiago Huauclilla, Oaxaca, Mexico. Objective: To evaluate the antinociceptive and anxiolytic-like effects of S. semiatrata extracts and identify a bioactive metabolite. Materials and methods: The extracts were obtained by maceration of S. semiatrata aerial parts using solvents in increasing polarity (hexane, ethyl acetate and methanol). A neo-clerodane diterpene was extracted from the ethyl acetate fraction using open column chromatography. Identification of this metabolite was performed by crystallography, 1 H NMR, 13 C NMR, ATR-IR, ECD, MS and elemental analysis. The antinociceptive activity was explored using the writhing and formalin tests. Whereas, the anxiolyticlike responses were analysed in the open-field, hole-board and plus-maze tests. All the treatments were administered using oral gavage in male CD1 mice and explored 30 min after administration of the individual extracts (300 mg/kg) or the compound 1 (0.1, 1 or 10 mg/kg). Results: All the extracts produced significant reduction in the nociceptive and anxiety-like behaviour compared to mice treated with the vehicle (0.5% tween 80 in saline solution). The spectroscopic analysis corroborated the presence of the neo-clerodane diterpene 7-keto-neoclerodan-3,13-dien-18,19:15,16diolide (1), as partial responsible of the antinociceptive and anxiolytic-like effects, which produced a dose-dependent response in the writhing test with an ED 50 ¼4.15 mg/kg. Discussion and conclusions: These results reinforce the medicinal properties of S. semiatrata in folk medicine, where participation of a neo-clerodane diterpene was evidenced in the inhibitory central nervous system activity of this species.

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Background: Amyloid-β (Aβ) fibrils induce cognitive impairment and neuronal loss, leading to onset of Alzheimer’s disease (AD). The inhibition of Aβ aggregation has been proposed as a therapeutic strategy for AD. Pristine C60 has shown the capacity to interact with the Aβ peptide and interfere with fibril formation but induces significant toxic effects in vitro and in vivo. Objective: To evaluate the potential of a series of C60 multiadducts to inhibit the Aβ fibrillization. Methods: A series of C60 multiadducts with four to six diethyl malonyl and their corresponding disodium-malonyl substituents were synthesized as individual isomers. Their potential on Aβ fibrillization inhibition was evaluated in vitro, in cellulo, and silico. Antioxidant activity, acetylcholinesterase inhibition capacity, and toxicity were assessed in vitro. Results: The multiadducts modulate Aβ fibrils formation without inducing cell toxicity, and that the number and polarity of the substituents play a significant role in the adducts efficacy to modulate Aβ aggregation. The molecular mechanism of fullerene-Aβ interaction and modulation was identified. Furthermore, the fullerene derivatives exhibited antioxidant capacity and reduction of acetylcholinesterase activity. Conclusion: Multiadducts of C60 are novel multi-target-directed ligand molecules that could hold considerable promise as the starting point for the development of AD therapies.

Antecedentes: Salvia purpurea Cav., comúnmente conocida como “salvia moradita”, es una planta medicinal usada en Oaxaca, Veracruz y Chiapas por sus propiedades analgésica, antiinflamatoria y antidiarreica. Sin embargo, no existen evidencias científicas que soporten su potencial para el alivio del dolor. Hipótesis: Terpenos y compuestos fenólicos son responsables de la actividad antinociceptiva de extractos de S. purpurea. Especie estudiada: Salvia purpurea Cav. (Lamiaceae). Lugar de estudio y año: Salvia purpurea se colectó en Santiago Huauclilla, Oaxaca, en octubre de 2017. Métodos: La toxicidad aguda (Dosis letal media, DL50) de los extractos de acetona, metanol y acuoso de S. purpurea se determinó mediante el protocolo de la OCDE (2001). Los extractos se administraron vía oral (p.o.) en un rango de dosis de 3 a 300 mg/kg para evaluar el efecto antinociceptivo utilizando las pruebas de estiramiento abdominal y formalina en ratones.  El análisis por HPLC se realizó para identificar la naturaleza de los metabolitos presentes en los extractos activos en comparación con sus respectivos estándares. Resultados: La toxicidad aguda de todos los extractos fue calculada como DL50 > 2000 mg/kg, p.o. El efecto antinociceptivo fue significativo en todas las dosis probadas y en forma no dependiente de la dosis para todos los extractos y en ambas pruebas. El análisis fitoquímico permitió identificar a compuestos de naturaleza terpénica y fenólica. Conclusiones: Los resultados del presente estudio refuerzan el uso como analgésico y antiinflamatorio de S. purpurea en la Medicina Tradicional Mexicana, donde terpenos y compuestos fenólicos participan en dichas actividades.