Rutin is the rutinose conjugate of quercetin. It presents several biological activities and is the major flavonoid in the hydroalcoholic extract of the calyces of Physalis peruviana L. It also shows hypoglycemic activity after oral administration. The aim of this work was to study the matrix effects of the extract from P. peruviana calyces on the pharmacokinetics of rutin and its metabolites in Wistar rats, using non-compartmental and population pharmacokinetic analyses. A pharmacokinetic study was performed after intravenous and oral administration of different doses of pure rutin and the extract. In the non-compartmental analysis, it was found that rutin from the extract exhibited higher distribution and clearance, as well as an 11-fold increase in the bioavailability of its active metabolites. A population pharmacokinetic model was also carried out with two compartments, double absorption and linear elimination, in which the extract and the doses were the covariates involved. This model correctly described the differences observed between rutin as a pure compound and rutin from the extract, including the dose dependency.
Objectives The objective of this work was to evaluate the anti-inflammatory activity of the aqueous extract, fractions and major compounds, which are isolated and identified from Passiflora edulis f. edulis (purple passion fruit) leaves extract. Methods For the isolation of the major compounds, reversed-phase chromatography and normal phase countercurrent chromatography were used. The separation was followed by thin layer chromatography and HPLC-DAD-ELSD. One-dimensional and two-dimensional NMR and ESI-TOF-MS/MS were used for structural elucidation. The anti-inflammatory activity was evaluated on a TPA multiple dose model of skin chronic inflammation in mice. Additionally, myeloperoxidase (MPO) and nitric oxide synthase (NOS) activity assays were performed as possible mechanisms of action studies. Key findings and conclusions The study of the butanolic fraction mainly showed the presence of saponins and flavonoids. Three minor flavonoids were detected; and three known saponins, cyclopassiflosides IX, XI and III were isolated and identified. This is the first unequivocal report of the presence of these compounds in P. edulis f. edulis leaves. The most favourable results of anti-inflammatory activity were obtained for the flavonoid-rich fraction. All the fractions and isolated compounds evaluated, presented high percentages of inhibition of nitric oxide synthase activity.
El presente libro es fruto de la investigación interdisciplinaria entorno a los fines medicinales de las hojas de Passiflora ligularis (granadilla), realizada entre los grupos de investigación Principios Bioactivos de Plantas Medicinales, del Departamento de Farmacia, y Estudio y Aprovechamiento de Productos Naturales Marinos y Frutas de Colombia, del Departamento de Química, ambos de la Universidad Nacional de Colombia; y el Grupo de Investigación en Fitoquímica de la Pontificia Universidad Javeriana, con apoyo del Ministerio de Ciencia, Tecnología e Innovación de Colombia. A lo largo de estas páginas se resumen algunos de los resultados y avances más destacados de estos grupos de investigación en cuanto a la caracterización química de las hojas de esta especie. Además, se da énfasis a los flavonoides y saponinas; al estudio in silico, in vitro e in vivo de su actividad farmacológica, principalmente como hipoglicemiante y antinflamatorio; y al desarrollo de metodologías analíticas precisas, exactas y reproducibles que permitan la completa caracterización del extracto optimizado obtenido como un ingrediente activo promisorio para el desarrollo de productos fitoterapéuticos (etapa actualmente en progreso). Esta publicación pretende la divulgación técnica y científica de los resultados de varios años de estudio con el fin de dar valor agregado a los cultivos de Passiflora ligularis, una planta de gran interés comercial debido a sus frutos, cuyas hojas en la actualidad son simplemente un subproducto de su cosecha, a causa del desconocimiento de su potencial terapéutico y de la posibilidad de convertirse en una materia prima para la obtención de productos fitoterapéuticos estables, seguros y eficaces.
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