15 resultados para TRISCHELATED RUTHENIUM(II)
em Consorci de Serveis Universitaris de Catalunya (CSUC), Spain
Resumo:
A photoactivated ruthenium(II) arene complex has been conjugated to two receptor-binding peptides, a dicarba analogue of octreotide and the Arg-Gly-Asp (RGD) tripeptide. These peptides can act as"tumor-targeting devices" since their receptors are overexpressed on the membranes of tumor cells. Both ruthenium-peptide conjugates are stable in aqueous solution in the dark, but upon irradiation with visible light, the pyridyl-derivatized peptides were selectively photodissociated from the ruthenium complex, as inferred by UV-vis and NMR spectroscopy. Importantly, the reactive aqua species generated from the conjugates, [(η6-p-cym)Ru(bpm)(H2O)]2+, reacted with the model DNA nucleobase 9-ethylguanine as well as with guanines of two DNA sequences, 5′dCATGGCT and 5′dAGCCATG. Interestingly, when irradiation was performed in the presence of the oligonucleotides, a new ruthenium adduct involving both guanines was formed as a consequence of the photodriven loss of p-cymene from the two monofunctional adducts. The release of the arene ligand and the formation of a ruthenated product with a multidentate binding mode might have important implications for the biological activity of such photoactivated ruthenium(II) arene complexes. Finally, photoreactions with the peptide-oligonucleotide hybrid, Phac-His-Gly-Met-linker-p5′dCATGGCT, also led to arene release and to guanine adducts, including a GG chelate. The lack of interaction with the peptide fragment confirms the preference of such organometallic ruthenium(II) complexes for guanine over other potential biological ligands, such as histidine or methionine amino acids.
Resumo:
A straightforward methodology for the synthesis of conjugates between a cytotoxic organometallic ruthenium(II) complex and amino- and guanidinoglycosides, as potential RNA-targeted anticancer compounds, is described. Under microwave irradiation, the imidazole ligand incorporated on the aminoglycoside moiety (neamine or neomycin) was found to replace one triphenylphosphine ligand from the ruthenium precursor [(η6-p-cym)RuCl(PPh3)2]+, allowing the assembly of the target conjugates. The guanidinylated analogue was easily prepared from the neomycin-ruthenium conjugate by reaction with N,N′-di-Boc-N″-triflylguanidine, a powerful guanidinylating reagent that was compatible with the integrity of the metal complex. All conjugates were purified by semipreparative high-performance liquid chromatography (HPLC) and characterized by electrospray ionization (ESI) and matrix-assisted laser desorptionionization time-of-flight (MALDI-TOF) mass spectrometry (MS) and NMR spectroscopy. The cytotoxicity of the compounds was tested in MCF-7 (breast) and DU-145 (prostate) human cancer cells, as well as in the normal HEK293 (Human Embryonic Kidney) cell line, revealing a dependence on the nature of the glycoside moiety and the type of cell (cancer or healthy). Indeed, the neomycinruthenium conjugate (2) displayed moderate antiproliferative activity in both cancer cell lines (IC50 ≈ 80 μM), whereas the neamine conjugate (4) was inactive (IC50 ≈ 200 μM). However, the guanidinylated analogue of the neomycinruthenium conjugate (3) required much lower concentrations than the parent conjugate for equal effect (IC50 = 7.17 μM in DU-145 and IC50 = 11.33 μM in MCF-7). Although the same ranking in antiproliferative activity was found in the nontumorigenic cell line (3 2 > 4), IC50 values indicate that aminoglycoside-containing conjugates are about 2-fold more cytotoxic in normal cells (e.g., IC50 = 49.4 μM for 2) than in cancer cells, whereas an opposite tendency was found with the guanidinylated conjugate, since its cytotoxicity in the normal cell line (IC50 = 12.75 μM for 3) was similar or even lower than that found in MCF-7 and DU-145 cancer cell lines, respectively. Cell uptake studies performed by ICP-MS with conjugates 2 and 3 revealed that guanidinylation of the neomycin moiety had a positive effect on accumulation (about 3-fold higher in DU-145 and 4-fold higher in HEK293), which correlates well with the higher antiproliferative activity of 3. Interestingly, despite the slightly higher accumulation in the normal cell than in the cancer cell line (about 1.4-fold), guanidinoneomycinruthenium conjugate (3) was more cytotoxic to cancer cells (about 1.8-fold), whereas the opposite tendency applied for neomycinruthenium conjugate (2). Such differences in cytotoxic activity and cellular accumulation between cancer and normal cells open the way to the creation of more selective, less toxic anticancer metallodrugs by conjugating cytotoxic metal-based complexes such as ruthenium(II) arene derivatives to guanidinoglycosides.
Resumo:
A straightforward methodology for the synthesis of conjugates between a cytotoxic organometallic ruthenium(II) complex and amino- and guanidinoglycosides, as potential RNA-targeted anticancer compounds, is described. Under microwave irradiation, the imidazole ligand incorporated on the aminoglycoside moiety (neamine or neomycin) was found to replace one triphenylphosphine ligand from the ruthenium precursor [(η6-p-cym)RuCl(PPh3)2]+, allowing the assembly of the target conjugates. The guanidinylated analogue was easily prepared from the neomycin-ruthenium conjugate by reaction with N,N′-di-Boc-N″-triflylguanidine, a powerful guanidinylating reagent that was compatible with the integrity of the metal complex. All conjugates were purified by semipreparative high-performance liquid chromatography (HPLC) and characterized by electrospray ionization (ESI) and matrix-assisted laser desorption-ionization time-of-flight (MALDI-TOF) mass spectrometry (MS) and NMR spectroscopy. The cytotoxicity of the compounds was tested in MCF-7 (breast) and DU-145 (prostate) human cancer cells, as well as in the normal HEK293 (Human Embryonic Kidney) cell line, revealing a dependence on the nature of the glycoside moiety and the type of cell (cancer or healthy). Indeed, the neomycin-ruthenium conjugate (2) displayed moderate antiproliferative activity in both cancer cell lines (IC50 ≈ 80 μM), whereas the neamine conjugate (4) was inactive (IC50 ≈ 200 μM). However, the guanidinylated analogue of the neomycin-ruthenium conjugate (3) required much lower concentrations than the parent conjugate for equal effect (IC50 = 7.17 μM in DU-145 and IC50 = 11.33 μM in MCF-7). Although the same ranking in antiproliferative activity was found in the nontumorigenic cell line (3 2 > 4), IC50 values indicate that aminoglycoside-containing conjugates are about 2-fold more cytotoxic in normal cells (e.g., IC50 = 49.4 μM for 2) than in cancer cells, whereas an opposite tendency was found with the guanidinylated conjugate, since its cytotoxicity in the normal cell line (IC50 = 12.75 μM for 3) was similar or even lower than that found in MCF-7 and DU-145 cancer cell lines, respectively. Cell uptake studies performed by ICP-MS with conjugates 2 and 3 revealed that guanidinylation of the neomycin moiety had a positive effect on accumulation (about 3-fold higher in DU-145 and 4-fold higher in HEK293), which correlates well with the higher antiproliferative activity of 3. Interestingly, despite the slightly higher accumulation in the normal cell than in the cancer cell line (about 1.4-fold), guanidinoneomycin-ruthenium conjugate (3) was more cytotoxic to cancer cells (about 1.8-fold), whereas the opposite tendency applied for neomycin-ruthenium conjugate (2). Such differences in cytotoxic activity and cellular accumulation between cancer and normal cells open the way to the creation of more selective, less toxic anticancer metallodrugs by conjugating cytotoxic metal-based complexes such as ruthenium(II) arene derivatives to guanidinoglycosides.
Resumo:
Vegeu el resum a l'inici del document del fitxer adjunt.
Resumo:
We describe fractal tessellations of the complex plane that arise naturally from Cannon-Thurston maps associated to complete, hyperbolic, once-punctured-torus bundles. We determine the symmetry groups of these tessellations.
Resumo:
"Vegeu el resum a l'inici del document del fitxer adjunt."
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Este capítulo repasa los distintos factores que influyen en la refrigeración del invernadero, como son la reducción de radiación solar, la evapotranspiración del cultivo, la ventilación y la evaporación de agua. Dichos factores están ligados entre sí por las ecuaciones del balance de energía y de humedad, de modo que al cambiar uno (por ejemplo, la radiación que llega al cultivo si se sombrea el invernadero) pueden cambiar los otros, por ejemplo la tasa de transpiración. Se presenta un balance simplificado de energía y humedad y se resuelven las ecuaciones para ver el efecto de los distintos sistemas de refrigeración en dos climas representativos, costero y continental. Después se discuten los equipos de sombro, ventilación mecánica y refrigeración por evaporación.
Resumo:
Estudi de la història de gènere del segle XIX i la seva aplicació a la figura de la reina Isabel II. A través de la publicística de l’època, els Fullets Bonsoms, descobrim la trajectòria sobre l’opinió i la imatge de les dones, i concretament, l’opinió creada al voltant de la reina Isabel II en diferents períodes del seu regnat (1833-1868). La imatge de la dona del segle XIX era la de l’àngel de la llar, la dona com a esposa i mare, que tenia com a principal missió el matrimoni, la maternitat i la domesticitat. A conseqüència, ha de rebre una educació en consonància amb el seu destí i es considera que per naturalesa no està capacitada per al món laboral. En aquest context, comença a néixer una consciència feminista de la mà d’Emilia Pardo Bazán o Concepción Arenal. Isabel II va ser proclamada reina amb només tres anys i es va convertir en el símbol de l’esperança i la llibertat dels espanyols: en l’iris de pau i llibertat. Però l’inestabilitat política, les camarilles, la corrupció, la vida privada i pública de la reina, entre d’altres factors van crear la imatge d’una reina lasciva, ingrata i cruel dels últims anys del seu regnat. La revolució antidinàstica coneguda com La Gloriosa va conduir a Isabel II al destronament i l’exili.
Resumo:
The demand for computational power has been leading the improvement of the High Performance Computing (HPC) area, generally represented by the use of distributed systems like clusters of computers running parallel applications. In this area, fault tolerance plays an important role in order to provide high availability isolating the application from the faults effects. Performance and availability form an undissociable binomial for some kind of applications. Therefore, the fault tolerant solutions must take into consideration these two constraints when it has been designed. In this dissertation, we present a few side-effects that some fault tolerant solutions may presents when recovering a failed process. These effects may causes degradation of the system, affecting mainly the overall performance and availability. We introduce RADIC-II, a fault tolerant architecture for message passing based on RADIC (Redundant Array of Distributed Independent Fault Tolerance Controllers) architecture. RADIC-II keeps as maximum as possible the RADIC features of transparency, decentralization, flexibility and scalability, incorporating a flexible dynamic redundancy feature, allowing to mitigate or to avoid some recovery side-effects.
Resumo:
Es va realitzar el II Workshop en Tomografia Computeritzada (TC) a Monells. El primer dia es va dedicar íntegrament a la utilització del TC en temes de classificació de canals porcines, i el segon dia es va obrir a altres aplicacions del TC, ja sigui en animals vius o en diferents aspectes de qualitat de la carn o els productes carnis. Al workshop hi van assistir 45 persones de 12 països de la UE. The II workshop on the use of Computed Tomography (CT) in pig carcass classification. Other CT applications: live animals and meat technology was held in Monells. The first day it was dedicated to the use of CT in pig carcass classification. The segond day it was open to otehr CT applications, in live animals or in meat and meat products quality. There were 45 assistants of 12 EU countries.
Resumo:
El grupo de olivo de la SECH se formó en el año 2005 con la vocación de favorecer la integración y la discusión de los investigadores que trabajan en temas relacionados con el olivar, las almazaras y la calidad del fruto, tanto del aceite de oliva como de la aceituna de mesa. Para favorecer este debate, en octubre de 2006, se realizaron las I Jornadas en Córdoba, y en ellas se abordaron tres temas: nuevas tendencias en la elección vegetal, plantaciones superintensivas y sistemas de manejo del suelo. En las II Jornadas que se van a realizar en Tarragona se debatirán distintos temas como el material vegetal, algún enfoque de la olivicultura sostenible, tecnología de almazaras y calidad del aceite de oliva.
Resumo:
La Revolución Energética Cubana (REC) surge de las necesidades de resolver la situación social y económica de Cuba, sumergida en una crisis energética con constantes apagones que limitaban por completo el desarrollo del país. La REC (2006) es un conjunto de medidas basadas en los principios de la autosuficiencia energética, el ahorro y uso racional de la energía, y el incremento de la eficiencia en todos los aspectos. En el presente trabajo se realiza el análisis de la sostenibilidad socio-ambiental de la REC en la Universidad Central Marta Abreu de las Villas (UCLV), ubicada en Santa Clara (Cuba). La valoración se ha efectuado mediante el análisis de los impactos ambientales y sociales en dos estudios paralelos que se complementan aplicando la técnica de conmensurabilidad débil. El conjunto de los programas de la REC han propiciado mejoras en el suministro eléctrico y en el ahorro energético, disminuyendo en un 30% las emisiones de CO2, a pesar del incremento en la actividad docente y en la flota de equipos, en la universidad. Las medidas adoptadas han incidido en la calidad de la docencia, las condiciones de vida, la concienciación y la participación de la población, dando lugar a un impacto social positivo. De esta manera, el balance global de la REC se califica de positivo ya que ha permitido el desarrollo de la UCLV sin incrementar los impactos ambientales, por lo que se puede considerar un paso en el camino hacia la sostenibilidad socio-ambiental.
Resumo:
Treball de recerca realitzat per una alumna d'ensenyament secundari i guardonat amb un Premi CIRIT per fomentar l'esperit científic del Jovent l'any 2009. El tema d’aquest treball de recerca és la premsa satírica a Catalunya durant la Segona República, centrat en l’anàlisi del setmanari 'El Be Negre’, i, a través d’aquesta publicació, l’objectiu és conèixer i veure com va tractar la premsa satírica determinats esdeveniments d’aquest període. La motivació de la recerca ve donada per l’interés en el periodisme i la història. El treball es divideix en dues grans parts; la primera d’aproximació al marc històric, i la segona, d’anàlisi de la revista. La primera part, consta d’un resum històric del període de la Segona República tan a nivell espanyol com català, d’un breu resum de les principals publicacions de l’època, tan diaris catalans com castellans i d’ideologies molt diverses, d’una breu història de la premsa satírica de Catalunya, des de mitjan segle XIX fins a la II República, i, finalment, una extensa documentació sobre el Be Negre (origen i influencies, redactors i ninotaires, seccions, funcionament, relació del setmanari amb diferents forces polítiques i sindicals). La segona part del treball, el cos central, es basa en l’anàlisi de la revista el Be Negre, a partir dels seus articles i acudits, que tracten alguns dels esdeveniments més rellevants de la Segona República.
Resumo:
Aquest treball és una primera aproximació al magmàtic món del teatre societari barceloní de principis de segle XX. Vol ser una radiografia, primer, en forma d’estat de la qüestió general, i després, en forma d’anàlisi de dos casos concrets, el CADCI i l’Ateneu Obrer del districte II, de tots els aspectes que engloba el fet teatral en aquests espais: des dels repertoris al funcionament de les companyies, passant per la recepció, el paper del públic o la importància del teatre com a eina política i de transmissió generacional del coneixement. Tot això en el context d’uns anys de crisi del món teatral, en general, i del teatre català, en particular.