23 research outputs found
Elementos multimedia para el desarrollo de las prácticas de Biotecnología Farmacéutica II (BFII)a través del campus virtual. Evaluación mediante indicadores de calida
El objetivo general propuesto para este Proyecto de Innovación Docente (PID) fue desarrollar elementos multimedia para articular de manera clara y coherente las prácticas de Biotecnología Farmacéutica II (BFII, Asignatura de 4º curso de Grado en Farmacia) a través del campus virtual. De esta forma las prácticas se pueden desarrollar de manera autónoma dentro y fuera del aula, teniendo la supervisión y seguimiento de forma más o menos puntual del docente a través de una tutorización con apoyo tecnológico (clases y actividades presenciales y on-line)
Desarrollo y elaboración de recursos didácticos on line para fomentar el autoaprendizaje interactivo y la autoevaluación en Química Farmacéutica con el apoyo del Campus Virtual
En este Proyecto de Innovación Docente se ha pretendido de manera general optimizar las alternativas ofrecidas en el Campus Virtual, mediante el diseño, elaboración y evaluación de actividades didáticas on-line que permitan que el Aula Virtual se convierta en un apoyo activo en el proceso enseñanza-aprendizaje en la asignatura de Química Farmacéutica II. Se ha llevado a cabo la elaboración de cuestionarios interactivos de autoevaluación que permitan al alumno conocer la adecuación de los conocimientos adquiridos, y al docente poder realizar un seguimiento rápido de cada alumno
Biocatalyzed Synthesis of Glycostructures with Anti-infective Activity
Molecules containing carbohydrate moieties play essential roles in fighting a variety of bacterial and viral infections. Consequently, the design of new carbohydrate-containing drugs or vaccines has attracted great attention in recent years as means to target several infectious diseases.
Conventional methods to produce these compounds face numerous challenges because their current production technology is based on chemical synthesis, which often requires several steps and uses environmentally unfriendly reactants, contaminant solvents, and inefficient protocols. The search for sustainable processes such as the use of biocatalysts and eco-friendly solvents is of vital importance. Therefore, their use in a variety of reactions leading to the production of pharmaceuticals has increased exponentially in the last years, fueled by recent advances in protein engineering, enzyme directed evolution, combinatorial biosynthesis, immobilization techniques, and flow biocatalysis. In glycochemistry and glycobiology, enzymes belonging to the families of glycosidases, glycosyltransferases (Gtfs), lipases, and, in the case of nucleoside and nucleotide analogues, also nucleoside phosphorylases (NPs) are the preferred choices as catalysts.
In this Account, on the basis of our expertise, we will discuss the recent biocatalytic and sustainable approaches that have been employed to synthesize carbohydrate-based drugs, ranging from antiviral nucleosides and nucleotides to antibiotics with antibacterial activity and glycoconjugates such as neoglycoproteins (glycovaccines, GCVs) and glycodendrimers that are considered as very promising tools against viral and bacterial infections.
In the first section, we will report the use of NPs and N-deoxyribosyltransferases for the development of transglycosylation processes aimed at the synthesis of nucleoside analogues with antiviral activity. The use of deoxyribonucleoside kinases and hydrolases for the modification of the sugar moiety of nucleosides has been widely investigated.
Next, we will describe the results obtained using enzymes for the chemoenzymatic synthesis of glycoconjugates such as GCVs and glycodendrimers with antibacterial and antiviral activity. In this context, the search for efficient enzymatic syntheses represents an excellent strategy to produce structure-defined antigenic or immunogenic oligosaccharide analogues with high purity. Lipases, glycosidases, and Gtfs have been used for their preparation.
Interestingly, many authors have proposed the use Gtfs originating from the biosynthesis of natural glycosylated antibiotics such as glycopeptides, macrolides, and aminoglycosides. These have been used in the chemoenzymatic semisynthesis of novel antibiotic derivatives by modification of the sugar moiety linked to their complex scaffold. These contributions will be described in the last section of this review because of their relevance in the fight against the spreading phenomenon of antibiotic resistance. In this context, the pioneering in vivo synthesis of novel derivatives obtained by genetic manipulation of producer strains (combinatorial biosynthesis) will be shortly described as well.
All of these strategies provide a useful and environmentally friendly synthetic toolbox. Likewise, the field represents an illustrative example of how biocatalysis can contribute to the sustainable development of complex glycan-based therapies and how problems derived from the integration of natural tools in synthetic pathways can be efficiently tackled to afford high yields and selectivity. The use of enzymatic synthesis is becoming a reality in the pharmaceutical industry and in drug discovery to rapidly afford collections of new antibacterial or antiviral molecules with improved specificity and better metabolic stability
Aprender jugando: aplicación de juegos interactivos para el aprendizaje de la Química en Ciencias Farmacéuticas
Aplicación de la dinámica de los juegos interactivos en las prácticas de Química Orgánica del Grado en Farmacia mediante la utilización de nuevas tecnologías y herramientas on line
Herramientas de Aprendizaje para el Diseño 3D de Estructuras y Procesos Químicos mediante Programas Informáticos Gratuitos/Libres
El objetivo propuesto en este proyecto de innovación docente fue el diseño, elaboración y evaluación de videos tutoriales on-line sobre el manejo de programas informáticos libres/gratuitos para el dibujo de moléculas químicas de interés farmacéutico, nomenclatura, cálculo de fórmulas y el diseño espacial de estructuras tridimensionales, que permitan que el alumno del Grado en Farmacia aprenda el manejo de programas siendo este un apoyo para la realización de su TFG y la defensa de mismo (Póster). Por otro lado, también se planteó el facilitar y animar a que los alumnos de cuarto y quinto curso del Grado en Farmacia presenten comunicaciones en el Congreso de Investigación para Estudiantes Pregraduados de Ciencias de la Salud celebrado todos los años en la UCM
Aprendizaje de las prácticas de laboratorio de Química Farmacéutica del Grado en Farmacia y Doble Grado en Farmacia y Nutrición a través del aula virtual
Depto. de Química en Ciencias FarmacéuticasFac. de FarmaciaFALSEsubmitte
Liver fibrosis secondary to bile duct injury: correlation of Smad7 with TGF-β and extracellular matrix proteins
<p>Abstract</p> <p>Background</p> <p>Liver fibrosis is the result of continuous liver injury stemming from different etiological factors. Bile duct injury induces an altered expression of TGF-β, which has an important role in liver fibrosis because this cytokine induces the expression of target genes such as collagens, PAI-1, TIMPs, and others that lead to extracellular matrix deposition. Smad7 is the principal inhibitor that regulates the target gene transcription of the TGF-β signaling. The aim of the study was to determine whether Smad7 mRNA expression correlates with the gene expression of <it>TGF-β, Col I</it>, <it>Col III</it>, <it>Col IV</it>, or <it>PAI-1 </it>in liver fibrosis secondary to bile duct injury (BDI).</p> <p>Results</p> <p>Serum TGF-β concentration was higher in BDI patients (39 296 pg/ml) than in liver donors (9008 pg/ml). Morphometric analysis of liver sections showed 41.85% of tissue contained fibrotic deposits in BDI patients. mRNA expression of Smad7, Col I, and PAI-1 was also significantly higher (<it>P </it>< 0.05) in patients with BDI than in controls. Smad7 mRNA expression correlated significantly with TGF-β concentration, Col I and Col III expression, and the amount of fibrosis.</p> <p>Conclusion</p> <p>We found augmented serum concentration of TGF-β and an increase in the percentage of fibrotic tissue in the liver of BDI patients. Contrary to expected results, the 6-fold increase in <it>Smad7 </it>expression did not inhibit the expression of <it>TGF-β, collagens</it>, and <it>PAI-1</it>. We also observed greater expression of Col I and Col III mRNA in BDI patients and significant correlations between their expression and TGF-β concentration and Smad7 mRNA expression.</p
Inglés
The use of mechanochemistry in carbohydrate chemistry is currently a growing field in which many new developments are being made because of its potential application in green methodologies. Ball milling (BM) is a promising eco-friendly technique with excellent characteristics that allows mostly solvent-free, faster and energy-efficient reactions. In this context, we provide in this perspective review a critical summary and discussion of the main known synthetic methods for carbohydrates based on mechanochemistry. The combination of the promising properties of mechanochemistry with carbohydrate reactions can be advantageous for setting strategies aligned with the green chemistry principles.Ministerio de Economía, Comercio y Empresa (España)Depto. de Química en Ciencias FarmacéuticasFac. de FarmaciaTRUEpu
Current challenges and future perspectives in sustainable mechanochemical transformations of carbohydrates
The use of mechanochemistry in carbohydrate chemistry is currently a growing field in which many new developments are being made because of its potential application in green methodologies. Ball milling (BM) is a promising eco-friendly technique with excellent characteristics that allows mostly solvent-free, faster and energy-efficient reactions. In this context, we provide in this perspective review a critical summary and discussion of the main known synthetic methods for carbohydrates based on mechanochemistry. The combination of the promising properties of mechanochemistry with carbohydrate reactions can be advantageous for setting strategies aligned with the green chemistry principles.Ministerio de Economía, Comercio y Empresa (España)Depto. de Química en Ciencias FarmacéuticasFac. de FarmaciaTRUEpu