A new naphthalene derivative with anti-amyloidogenic activity as potential therapeutic agent for Alzheimer's disease.

The aggregation of ß-amyloid peptides is associated to neurodegeneration in Alzheimer's disease (AD) patients. Consequently, the inhibition of both oligomerization and fibrillation of ß-amyloid peptides is considered a plausible therapeutic approach for AD. Herein, the synthesis of new naphthalene derivatives and their evaluation as anti-ß-amyloidogenic agents are presented. Molecular dynamic simulations predicted the formation of thermodynamically stable complexes between the compounds, the Aß1-42 peptide and fibrils. In human microglia cells, these compounds inhibited the aggregation of Aß1-42 peptide. The lead compound 8 showed a high affinity to amyloid plaques in mice brain ex vivo assays and an adequate log Poct/PBS value. Compound 8 also improved the cognitive function and decreased hippocampal ß-amyloid burden in the brain of 3xTg-AD female mice. Altogether, our results suggest that 8 could be a novel therapeutic agent for AD.

Amylovis-201 enhances physiological memory formation and rescues memory and hippocampal cell loss in a streptozotocin-induced Alzheimer's disease animal model.

Alzheimer's disease is the most common neurodegenerative disease, and its treatment is lacking. In this work, we tested Amylovis-201, a naphthalene-derived compound, as a possible therapeutic candidate for the treatment of AD. For this purpose, we performed three experiments. In the first and third experiment, animals received a bilateral administration of streptozotocin and, starting 24 h after injection, a daily dose of Amylovis-201 (orally), for 17 days or for the whole time of the experiment respectively (28 days), after which learning and memory, as well as the number of hippocampal dentate gyrus cells, were assessed. In the second experiment, healthy animals received a single dose of Amylovis-201, 10 min or 5 h after the learning section to assess whether this substance could promote specific mechanisms involved in memory trace formation. Our data show that, administration of a single dose of Amylovis-201, 10 min after the end of training, but not at 5 h, produces a prolongation in memory duration, probably because it modulates specific mechanisms involved in memory trace consolidation. Furthermore, daily administration of Amylovis-201 to animals with bilateral intracerebroventricular injection of STZ produces a reduction in the loss of the hippocampus dentate gyrus cells and an improvement in spatial memory, probably because Amylovis-201 can interact with some of the protein kinases of the insulin signaling cascade, also involved in neural plasticity, and thereby halt or reverse some of the effects of STZ. Taking to account these results, Amylovis-201 is a good candidate for the therapeutic treatment of AD.

Thalassia testudinum, una planta marina con potencialidades de uso terapéutico / Thalassia testudinum, a sea plant with great therapeutical potentialities

Introducción: las plantas medicinales son todas aquellas que contienen un principio activo o más, los cuales, administrados con la dosis adecuada, producen un efecto curativo a las enfermedades del hombre y los animales. El hecho de contener más de un principio activo hace que una planta medicinal pueda servir para tratar diferentes afecciones o trastornos. Objetivo: analizar los beneficios y las potencialidades terapéuticas de la planta marina Thalassia testudinum a partir de una revisión de la información existente y los principales resultados de las investigaciones realizadas sobre este organismo marino. Desarrollo: los productos naturales con propiedades terapéuticas han sido muy utilizados en la medicina tradicional. Indudablemente, los extractos de plantas de origen terrestre han representado hasta el presente una de las fuentes de mayor interés para la obtención de fitofármacos. Sin embargo, una fuente útil aún no explorada lo suficiente son los organismos marinos, que al evolucionar y vivir en condiciones ecológicas únicas y como resultado de su gran diversidad taxonómica en relación con la de los organismos terrestres, pueden sintetizar moléculas que no tienen equivalencia con las encontradas hasta el presente en estos últimos. Eso puede derivar en la obtención de estructuras químicas novedosas con efectos farmacológicos sui generis, tal es el caso de la fenograma marina Thalassia testudinum...(AU)

Introduction: medicinal plants are those which contain one or more active principles that have a curative effect upon some illnesses which affect men and animals, whenever it is adequately administered. When one plant contains more than one active principle, it can be used to treat different ailments or body disorders. Objective: to analyze the benefits and therapeutic potentialities of the sea plant Thalassia testudinum based on the existent information and in the main results of research works about this sea organism. Development: natural products with therapeutic properties have been widely used in traditional medicine. Undoubtedly, the extracts from ground origin trees have so far represented one of the most interesting sources for phytodrugs. Nevertheless, sea organisms are a useful source which has not been fully explored. As they live and evolve in unique ecologic conditions, and as a result of their great taxonomic diversity in relation to that of ground organisms, they can synthesize molecules that are not equivalent to those of ground organisms found until now. This can derive in obtaining new chemical structures with sui generis pharmacological effects as in the case of the marine phenogram Thalassia testudinum. From this plant, poliphelonic structure-rich extract has been obtained, which show therapeutic potentialities associated to the great variety of beneficial effects that have been described in the studies such as anti-inflammatory, cytoprotective, antioxidative and neuroprotective properties. All the aforementioned turns this new developing product into a possible phytodrug. Conclusions: the sea organisms represent a new source to obtain new phytodrugs and nutritional supplements of great use in human health and nutrition(AU)

Thalassia testudinum, una planta marina con potencialidades de uso terapéutico / Thalassia testudinum, a sea plant with great therapeutical potentialities

Introducción: las plantas medicinales son todas aquellas que contienen un principio activo o más, los cuales, administrados con la dosis adecuada, producen un efecto curativo a las enfermedades del hombre y los animales. El hecho de contener más de un principio activo hace que una planta medicinal pueda servir para tratar diferentes afecciones o trastornos. Objetivo: analizar los beneficios y las potencialidades terapéuticas de la planta marina Thalassia testudinum a partir de una revisión de la información existente y los principales resultados de las investigaciones realizadas sobre este organismo marino. Desarrollo: los productos naturales con propiedades terapéuticas han sido muy utilizados en la medicina tradicional. Indudablemente, los extractos de plantas de origen terrestre han representado hasta el presente una de las fuentes de mayor interés para la obtención de fitofármacos. Sin embargo, una fuente útil aún no explorada lo suficiente son los organismos marinos, que al evolucionar y vivir en condiciones ecológicas únicas y como resultado de su gran diversidad taxonómica en relación con la de los organismos terrestres, pueden sintetizar moléculas que no tienen equivalencia con las encontradas hasta el presente en estos últimos. Eso puede derivar en la obtención de estructuras químicas novedosas con efectos farmacológicos sui generis, tal es el caso de la fenograma marina Thalassia testudinum...

Introduction: medicinal plants are those which contain one or more active principles that have a curative effect upon some illnesses which affect men and animals, whenever it is adequately administered. When one plant contains more than one active principle, it can be used to treat different ailments or body disorders. Objective: to analyze the benefits and therapeutic potentialities of the sea plant Thalassia testudinum based on the existent information and in the main results of research works about this sea organism. Development: natural products with therapeutic properties have been widely used in traditional medicine. Undoubtedly, the extracts from ground origin trees have so far represented one of the most interesting sources for phytodrugs. Nevertheless, sea organisms are a useful source which has not been fully explored. As they live and evolve in unique ecologic conditions, and as a result of their great taxonomic diversity in relation to that of ground organisms, they can synthesize molecules that are not equivalent to those of ground organisms found until now. This can derive in obtaining new chemical structures with sui generis pharmacological effects as in the case of the marine phenogram Thalassia testudinum. From this plant, poliphelonic structure-rich extract has been obtained, which show therapeutic potentialities associated to the great variety of beneficial effects that have been described in the studies such as anti-inflammatory, cytoprotective, antioxidative and neuroprotective properties. All the aforementioned turns this new developing product into a possible phytodrug. Conclusions: the sea organisms represent a new source to obtain new phytodrugs and nutritional supplements of great use in human health and nutrition