Scutellaria incarnata Vent. root extract and isolated phenylethanoid glycosides are neuroprotective against C2-ceramide toxicity.

ETHNOPHARMACOLOGICAL RELEVANCE: Neuronal death is a central process in neurodegenerative diseases and represents a therapeutic challenge for their prevention and treatment. Scutellaria incarnata Vent. roots are used traditionally in Colombia for central nervous system conditions including those affecting cognitive functions, but their chemistry and neuroprotective action remain to be explored to understand the scientific basis for their medicinal uses. In this study, S. incarnata roots are investigated to assess whether they have neuroprotective effects that could provide some explanation for their traditional use in neurodegenerative diseases. AIM OF THE STUDY: To evaluate the neuroprotective effect of S. incarnata roots and its chemical constituents against C2-ceramide-induced cell death in Cath.-a-differentiated (CAD) cells. MATERIALS AND METHODS: S. incarnata root ethanol extract was fractionated and compounds were isolated by column chromatography; their structures were elucidated by nuclear magnetic resonance spectroscopy, mass spectrometry and infrared spectroscopy. The cytotoxic and neuroprotective effects against C2-ceramide of S. incarnata root extract, fractions and isolated compounds were assessed in CAD cells. RESULTS: S. incarnata root extract and its n-butanol fraction were not cytotoxic but showed neuroprotective effects against C2-ceramide toxicity in CAD cells. The phenylethanoid glycosides incarnatoside (isolated for the first time) and stachysoside C (12.5, 25 and 50 µg/mL) from S. incarnata roots also protected CAD cells against C2-ceramide without inducing cytotoxic effects. CONCLUSION: The observed neuroprotective effects of S. incarnata root extract and isolated phenylethanoid glycosides in CAD cells provide an ethnopharmacological basis for the traditional use of this species in Colombia for central nervous system disorders.

Nanopartículas lipídicas a base de propóleos como transportadores de activos de interés cosmético: Desarrollo, caracterización y evaluación de seguridad / Propolis based lipid nanoparticles as carriers of cosmetic actives: Development, characterization and safety evaluation

En el ámbito cosmético, la tecnología a escala nanométrica resulta atractiva para el diseño de productos novedosos y funcionales. Así, para el caso de las nanopartículas lipídicas, se ha demostrado su capacidad para incrementar la estabilidad de moléculas activas y modificar su liberación. Como un aporte en la búsqueda de alternativas innovadoras para la preparación de este tipo de transportadores (carriers), el presente trabajo propone el aprovechamiento de las ceras provenientes de propóleos para la preparación de partículas lipídicas conteniendo extracto del árbol de té. Las partículas obtenidas presentan tamaños cercanos a 200 nm con polidispersidades inferiores a 0,1. Los valores de potencial zeta cercanos a cero sugieren un mecanismo de estabilización del sistema particulado vía efecto estérico. De otro lado, la incorporación del activo dentro de la estructura de las partículas es confirmada por DSC. En conjunto, los resultados evidencian la posibilidad de generar valor agregado a un producto de la colmena reconocido y valorado por sus propiedades biológicas. Además, ofrecen un material de partida que constituye una alternativa interesante para el desarrollo de productos cosméticos novedosos en los que podrían incorporarse moléculas activas.

In the cosmetic field, the technology at the nanometric scale is attractive for designing novel and functional products. In the case of lipid nanoparticles, the ability of these carriers for increasing the stability of active molecules and modifying their release has been demonstrated. As a contribution in the research of innovative alternatives for preparing these particles, this work proposes the use of the propolis waxes as starting material. In this way, lipid nanoparticles containing tea tree oil were prepared having particle sizes close to 200 nm with polydispersity indexes less than 0.1. The zeta potential values near to zero suggest the stabilization of the lipid nanoparticles via steric mechanisms. The incorporation of the active into the nanoparticle structure is confirmed by DSC. As a whole, the results are appealing in order to give added value to beehive product, recognized in Latin America for its biological properties. Furthermore, these results offer a new alternative of lipid material which is interesting for developing pioneering cosmetic products containing active molecules.

Actividad antiplasmódica in vitro de Piper holtonii (cordoncillo) / In vitro antiplasmodial activity of Piper holtonii (cordoncillo)

Introducción: especies vegetales del género Piper (Piperaceae) han sido usadas en la medicina tradicional en diferentes regiones del mundo, incluida Latinoamérica para el tratamiento de enfermedades tropicales como la malaria. Objetivo: evaluar la actividad antiplasmódica del extracto etanólico y las fracciones de diferente polaridad de Piper holtonii C.DC. Métodos: la actividad antiplasmódica del extracto etanólico de las partes aéreas de Piper holtonii y de las fracciones hexánica, clorofórmica, metanólica, butanólica y acuosa, se evaluó sobre un cultivo de Plasmodium falciparum cepa FCB-2. Se determinó la actividad hemolítica y se caracterizaron fitoquímicamente cada una de las fracciones. Resultados: el extracto etanólico y las fracciones de baja polaridad presentaron actividad promisoria con valores de CI50 inferiores a 25 µg/mL. Conclusiones: los resultados de la actividad biológica de Piper holtonii permiten sugerir que los metabolitos de baja y media polaridad están relacionados con la actividad antiplasmódica de esta especie.

Introduction: plant species of the genus Piper (Piperaceae) have been used in traditional medicine in various regions of the world. In Latin America they have been used to treat tropical diseases such as malaria. Objective: evaluate the antiplasmodial activity of the ethanolic extract and fractions of varying polarity of Piper holtonii C. DC. Methods: evaluation was conducted of the antiplasmodial activity of ethanolic extract from aerial parts of Piper holtonii and of hexane, chloroform, methanol, buthanol and aqueous fractions on a Plasmodium falciparum strain FCB-2 culture. Hemolytic activity was determined and phytochemical characterization of each fraction was performed. Results: both the ethanolic extract and the low-polarity fractions displayed promising activity, with CI50 values below 25 µg/mL. Conclusions: results concerning the biological activity of Piper holtonii suggest that low- and medium-polarity metabolites are related to antiplasmodial activity in this species.

Triterpenos e flavonóides isolados de flores de Laseguea erecta (Apocynaceae) / Triterpenes and flavonoids isolate from the flowers of Laseguea erecta (Apocynaceae)

Das flores de Laseguea erecta isolaram-se o lupeol, ácido ursólico e os flavonóides quercetina (3,5,7,3',4'-pentaidroxiflavona) e 3-O-ß-L-arabinopiranosil quercetina. Esta é o primeiro estudo sobre metabólitos especiais em flores desse gênero. As estruturas foram determinadas através da análise dos dados espectrais de IV, RMN de 1H e 13C (1D e 2D) e comparação com valores registrados na literatura.

From the flowers of Laseguea erecta were isolated the lupeol, ursolic acid, quercetin (3,5,7,3',4'-pentahydroxyflavone) and 3-O-ß-L-arabinopyranosylquercetin. This is the first phytochemical study of this genera flowers'. The structures were established by the IR, 1H and 13C NMR (1D, 2D) spectral data analysis and by comparison with literature data.