Synthesis of IAN-type N,N-Ligands via Dynamic Kinetic Asymmetric Buchwald-Hartwig Amination

The Pd-catalyzed coupling of racemic heterobiaryl bromides, triflates, or nonaflates with aryl/alkyl primary amines using QUINAP as the ligand provides the corresponding axially chiral heterobiaryl amines with excellent yields and enantioselectivities. Reactivity and structural studies of neutral and cationic oxidative addition intermediates support a dynamic kinetic asymmetric amination mechanism based on the labilization of the stereogenic axis in the latter and suggest that coordination of the amine to the Pd center is the stereodetermining step.Ministerio de Ciencia e Innovación CTQ2013-48164-C2-1-P, CTQ2013-48164-C2-2-P, RYC-2013-12585 for A.R.European FEDER FundsJunta de Andalucía 2012/FQM 1078

Magnetómetro para medida de campos electromagnéticos débiles en la banda ELF

Número de publicación: ES2557702 A1 (27.01.2016) Número de Solicitud: Consulta de Expedientes OEPM (C.E.O.) P201400462 (28.05.2014)La invención comprende un sistema para la medición de campos electromagnéticos débiles, en la banda de frecuencias comprendida entre 1 a 100 Hz, donde se localizan señales derivadas de la resonancia natural que ocurre entre la tierra y la ionosfera, las resonancias de Schumann. El sistema está compuesto por un núcleo de material ferromagnético (1) y un conjunto de bobinas separadas entre sí (2), conectadas mediante cables unifilares (8). Un cable de par trenzado (3) conecta el sensor a un sistema electrónico de medida (4) compuesto por un amplificador diferencial (5) al que se acoplan cada par trenzado, en una bifurcación coaxial con las mallas comunes (20), (21) mediante conectores coaxiales (22), (23) y con salida a un convertidor analógico digital (6). La geometría, estructura y materiales del sistema, le confieren sus propiedades de sensibilidad y ancho de banda.Universidad de Almerí

Red-Emitting Tetracoordinate Organoboron Chelates: Synthesis, Photophysical Properties, and Fluorescence Microscopy

Seven tetracoordinate organoboron fluorophores with heterobiaryl N,O- or N,N-chelate ligands were prepared and photophysically characterized (in toluene). The electronic variation of the heteroaromatic moiety provided a means for the fine-tuning of the UV/vis absorption and emission spectra. In the most interesting cases, the spectra were red-shifted to maximum absorbance at wavelengths longer than 500 nm and emission maxima between 620 and 660 nm. The pronounced intramolecular charge-transfer character of the dyes yielded large Stokes shifts (3500-5100 cm), while maintaining appreciable fluorescence quantum yields of up to 0.2 for emission maxima longer than 600 nm. The lipophilic character of the dyes enabled their application as stains of vesicle substructures in confocal fluorescence microscopy imaging.Ministerio de Economía y Competitividad CTQ2014-54729 - C2 - 1 - P for U.P., CTQ2013 - 48164 - C2 - 1 - P , CTQ2013 - 48164 - C2 - 2 - P for A.R., CTQ2013 - 41339 - P, CTQ2015 - 71896 - REDT for E.P.I., Ramón y Cajal contract RYC - 2013 - 12585 for A.R.FEDER FundJunta de Andalucía 2012/FQM - 2140 for U.P., 2009/FQM - 4537 and 2012/FQM - 1078 for A.R

Application of directly brewed compost extract improves yield and quality in baby leaf lettuce grown hydroponically

The aim of this work was to study whether the application of a directly brewed compost extract (added in the nutrient solution or by microsprinkler) could be used to improve the yield and quality of baby leaf red lettuce growing in a floating system, and to control the incidence of Pythium irregulare. Its e_ect on the quality of fresh-cut red lettuce was also studied. For this, two experiments were carried out over two growing cycles (winter–spring and autumn). The results showed that the use of compost extract added to the nutrient solution improved baby leaf lettuce growth and quality, reducing the nitrate content and enhancing the content of potentially health-promoting compounds such as phenols and flavonoids and the antioxidant capacity. Microbial quality was maintained during storage and the compost extract had no negative e_ect on the microbial load of the final product. In addition, application of the compost decreased the population of P. irregulare in the water. It is concluded that the application of directly brewed compost extract is of potential use in a sustainable soilless production system for baby leaf red lettuce, since it improves the yield and quality of the product and is able to control the incidence of P. irregulare.This work was supported by projects AGL2017-84085-C3-3-R and AGL2017-84085-C3-1-R from the Ministerio de Economía y Competitividad of Spain

Meta-heurística ACO (Ant Colony Optimization) para la resolución de problemas en líneas de producción

La meta -heurística ACO (Ant Colony Optimization) es un procedimiento heurístico para la resolución de problemas de optimización di screta basado en el comportamiento de las hormigas. Sus principales características son: (1) la utilización de "feed -back" positivo, (2) computación distribuida (la estructura de estos algoritmos permite su paralelización de forma muy simple y natural), y (3) el uso de heurísticas Greedy constructivas (ayuda a encontrar soluciones aceptables en las primeras etapas del proceso de exploración). En este artículo se presenta la aplicación de dichas meta -heurísticas a la resolución de problemas de producción co mo equilibrado de líneas de montaje o la secuenciación de unidades en un sistema que no permite esperasPostprint (published version

Structural stabilization of botulinum neurotoxins by tyrosine phosphorylation

AbstractTyrosine phosphorylation of botulinum neurotoxins augments their proteolytic activity and thermal stability, suggesting a substantial modification of the global protein conformation. We used Fourier-transform infrared (FTIR) spectroscopy to study changes of secondary structure and thermostability of tyrosine phosphorylated botulinum neurotoxins A (BoNT A) and E (BoNT E). Changes in the conformationally-sensitive amide I band upon phosphorylation indicated an increase of the α-helical content with a concomitant decrease of less ordered structures such as turns and random coils, and without changes in β-sheet content. These changes in secondary structure were accompanied by an increase in the residual amide II absorbance band remaining upon H-D exchange, consistent with a tighter packing of the phosphorylated proteins. FTIR and differential scanning calorimetry (DSC) analyses of the denaturation process show that phosphorylated neurotoxins denature at temperatures higher than those required by non-phosphorylated species. These findings indicate that tyrosine phosphorylation induced a transition to higher order and that the more compact structure presumably imparts to the phosphorylated neurotoxins the higher catalytic activity and thermostability

Synthesis of IAN-type N,N-Ligands via Dynamic Kinetic Asymmetric Buchwald-Hartwig Amination

The Pd-catalyzed coupling of racemic heterobiaryl bromides, triflates, or nonaflates with aryl/alkyl primary amines using QUINAP as the ligand provides the corresponding axially chiral heterobiaryl amines with excellent yields and enantioselectivities. Reactivity and structural studies of neutral and cationic oxidative addition intermediates support a dynamic kinetic asymmetric amination mechanism based on the labilization of the stereogenic axis in the latter and suggest that coordination of the amine to the Pd center is the stereodetermining step.Peer Reviewe

Role of the transient receptor potential vanilloid 1 in inflammation and sepsis

The transient receptor potential vanilloid 1 (TRPV1) is a thermoreceptor that responds to noxious temperatures, as well as to chemical agonists, such as vanilloids and protons. In addition, its channel activity is notably potentiated by proinflammatory mediators released upon tissue damage. The TRPV1 contribution to sensory neuron sensitization by proalgesic agents has signaled this receptor as a prime target for analgesic and anti-inflammatory drug intervention. However, TRPV1 antagonists have notably failed in clinical and preclinical studies because of their unwanted side effects. Recent reports have unveiled previously unrecognized anti-inflammatory and protective functions of TRPV1 in several diseases. For instance, this channel has been suggested to play an anti-inflammatory role in sepsis. Therefore, the use of potent TRPV1 antagonists as a general strategy to treat inflammation must be cautiously considered, given the deleterious effects that may arise from inhibiting the population of channels that have a protective function. The use of TRPV1 antagonists may be limited to treating those pathologies where enhanced receptor activity contributes to the inflamed state. Alternatively, therapeutic paradigms, such as reduction of inflammatory-mediated increase of receptor expression in the cell surface, may be a better strategy to prevent abrogation of the TRPV1 subpopulation involved in anti-inflammatory and protective processes

N-type inactivation of the potassium channel KcsA by the Shaker B "ball" Peptide: Mapping the inactivating peptide-binding epitope

10 pags, 6 figsThe effects of the inactivating peptide from the eukaryotic Shaker B K + channel (the ShB peptide) on the prokaryotic KcsA channel have been studied using patch clamp methods. The data show that the peptide induces rapid, N-type inactivation in KcsA through a process that includes functional uncoupling of channel gating. We have also employed saturation transfer difference (STD) NMR methods to map the molecular interactions between the inactivating peptide and its channel target. The results indicate that binding of the ShB peptide to KcsA involves the ortho and meta protons of Tyr 8, which exhibit the strongest STD effects; the C4H in the imidazole ring of His16; the methyl protons of Val4, Leu 7, and Leu10 and the side chain amine protons of one, if not both, the Lys18 and Lys19 residues. When a noninactivating ShB-L7E mutant is used in the studies, binding to KcsA is still observed but involves different amino acids. Thus, the strongest STD effects are now seen on the methyl protons of Val4 and Leu10, whereas His16 seems similarly affected as before. Conversely, STD effects on Tyr8 are strongly diminished, and those on Lys18 and/or Lys19 are abolished. Additionally, Fourier transform infrared spectroscopy of KcsA in presence of 13C-labeled peptide derivatives suggests that the ShB peptide, but not the ShB-L7E mutant, adopts a β-hairpin structure when bound to the KcsA channel. Indeed, docking such a β-hairpin structure into an open pore model for K+ channels to simulate the inactivating peptide/channel complex predicts interactions well in agreement with the experimental observations. © 2008 by The American Society for Biochemistry and Molecular Biology, Inc.This work was supported by Spanish Ministerio de Educación y Ciencia Grants CTQ2005-00360/BQU (to J. L. N.) and BFU2005-00749 (to J. M. G.-R.);FIPSE Experiment 36557/06 (to J. L. N.) and Grant BANCAJA-UMH IP/UR/01;and Consellería de Empresa, Universidad y Ciencia de la Generalitat Valenciana Grant GV07/017 (to J. A. E.)

Promising composts as growing media for the production of baby leaf lettuce in a floating system

The floating system is a successful strategy for producing baby leaf vegetables. Moreover, compost from agricultural and agri-food industry wastes is an alternative to peat that can be used as a component of growing media in this cultivation system. In this study, we experimented with three composts containing tomato (Solanum lycopersicum L.), leek (Allium porrum L.), grape (Vitis vinifera L.), and/or olive (Olea europaea L.) mill cake residues, which were used as the main component (75/25 volume/volume) of three growing media (GM1, GM2 and GM3) to evaluate their e_ect on the growth and quality of red baby leaf lettuce (Lactuca sativa L.). We used a commercial peat substrate as a control treatment (100% volume) and in mixtures (25% volume) with the composts. The plants were cultivated over two growing cycles, in spring and summer, and harvested twice in each cycle when the plants had four to five leaves. We found that the percentage of seed germination was significantly higher in plants grown in peat than in those grown in compost growing media. The yield was a_ected by the growing media in the summer cycle, and we obtained the highest value with GM1. Furthermore, the second cut was more productive than the first one for all the growing media in both cycles. The lettuce quality was also a_ected by the growing media. In general, the total phenolic content and antioxidant capacity in the leaves was higher in plants grown in the compost growing media, particularly in the second cut, but the nitrate content in the leaves was greater in some of the compost treatments compared with the peat treatment. In addition, an in vitro suppressive activity study demonstrated that the interaction between di_erent fungi and bacteria observed through metagenomics analysis could contribute to the e_ectiveness of the compost in controlling Pythium irregulare. The use of compost as a component of the growing media in the production of baby leaf vegetables in a floating system does not only favor the crop yield and producto quality, but also shows suppressive e_ects against P. irregulare.This research was funded by the Spanish Ministry of Economy and Competitiveness: Reference project: AGL2017-84085-C3-1-R, AGL2017-84085-C3-2-R, AGL2017-84085-C3-3-R