960 resultados para Benzoyl glycine


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En el cultivo de soja, una vez que el número de vainas quedó fijado, la ocurrencia de defoliaciones puede disminuir el rendimiento al afectar el peso de las semillas; sin embargo, la magnitud del efecto de las defoliaciones tardías sobre el rendimiento es altamente variable. El objetivo general de la tesis fue obtener una aproximación cuantitativa para estimar las pérdidas del rendimiento en genotipos de soja con número y peso potencial de semillas contratantes ante defoliaciones tardías, basada en el entendimiento de las bases funcionales que definen el crecimiento de las semillas. Se realizaron tres experimentos en parcelas con manipulaciones de la fuente (0, 33, 67 y 100 por ciento de defoliación)y los destinos (desvainado de 0 y 40 por ciento de vainas)15 y 20 días después de R5. El índice de área foliar (IAF)y el porcentaje de radiación fotosintéticamente activa interceptada (porcentaje RFAi), medidos luego de los tratamientos, se usaron como estimadores de la fuente remanente y para calcular la relación Fuente/Destino (F/D)establecida. Estos atributos permitieron cuantificar adecuadamente las mermas en rendimiento y los cambios en el peso de las semillas, siendo el nivel de destinos sólo importante bajo nula o leve defoliación. La respuesta a la disponibilidad de fuente se manifestó principalmente en posiciones distales del tallo principal, y se debió a cambios en la tasa de crecimiento de la semilla más que a la duración del llenado efectivo. Las defoliaciones no alteraron el patrón de desecamiento de las semillas, a excepción de la defoliación total, que lo aceleró. El contenido máximo de agua se asoció con el peso final de los granos en cada uno de los tratamientos de defoliación. La removilización aparente de reservas no se incrementó ante la reducción de la relación F/D y se redujo con una defoliación total. No se encontraron evidencias que sugieran un rol moderador de las reservas para sostener el peso de las semillas, sin embargo existió una respuesta diferencial de los genotipos y entre años en el nivel de removilización. Puede concluirse que defoliaciones tardías reducen el rendimiento de soja debido a reducciones en la tasa de crecimiento de las semillas, que no fueron compensadas por removilización, por lo que podría estimarse la caída del rendimiento mediante la cuantificación de la fuente remanente luego de una defoliación.

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La maleza altamisa (Artemisia annua L.)interfiere con el cultivo de soja por competencia y alelopatía, moduladas por estreses bióticos y abióticos (e.g. densidad, herbicida). Los aleloquímicos de altamisa (e.g. artemisinina, aceite esencial)pueden afectar directamente el crecimiento del cultivo o, indirectamente, a través de Bradyrhizobium japonicum (bacteria fijadora de N). Comprender los efectos de las interacciones en el sistema soja-altamisa es agroecológicamente relevante para diseñar prácticas que optimicen la producción y minimicen el uso de insumos. El objetivo de esta tesis fue analizar las interferencias competitivas y alelopáticas entre soja-altamisa y su impacto sobre la nodulación y el rendimiento del cultivo ante cambios en la densidad de plantas y dosis de herbicida. La metodología incluyó ensayos en: (i)parcelas a campo con distintas combinaciones de densidades cultivo-maleza y niveles de alelopatía y de herbicida, (ii)macetas a campo con distintas fuentes de aleloquímicos (biomasa seca y verde de altamisa, artemisinina pura)y suelos (arcilloso y arenoso)y (iii)laboratorio con distintos tipos y niveles de aleloquímicos. (i)Altas densidades de altamisa junto con altos niveles de aleloquímicos en el suelo no redujeron el crecimiento y rendimiento de soja y promovieron la nodulación con o sin aplicación de dosis subletales de herbicida. (ii)El rendimiento fue mayor en presencia de aleloquímicos y sustrato arcilloso. La relación entre el rendimiento y el peso de los nódulos fue positiva y los mayores valores se registraron con biomasa seca de altamisa. (iii)La artemisinina y el aceite esencial provocaron un efecto sinérgico negativo sobre el crecimiento de B. japonicum. El efecto neto de las interacciones competitivas, alelopáticas y de mutualismo generadas entre soja y altamisa dependen no solo del ambiente explorado sino del nivel de organización estudiado. En condiciones de campo (parcelas y macetas), la interacción alelopática fue positiva o neutra, mientras que en laboratorio resultó negativa.

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p.127-132

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After thermal treatment of a mixture of glucose and glycine for 2 h at 125 degreesC, about 60% of the starting material was converted into nonsoluble, black pigments, whereas 40% of the mixture was still water-soluble. Dialysis of the latter fraction revealed 30.4% of low molecular weight compounds (LMWs; MW <10 000 De) and 10.0% high-molecular weight products [HMWs; MW greater than or equal to 10000 Dal. The water-soluble Maillard reaction products (MRPs) were separated by gel permeation chromatography and ultrafiltration, revealing that 60% of the water-soluble products of the total carbohydrate/amino acid mixture had MWs <1 000 Da and consisted mainly of non-coloured reaction products. MRPs with MWs between 1000 and 30000 Da were Found in comparatively low yields (about 1.3%). In contrast, about 31.1% of the MRPs exhibited MWs > 30000 Da, amongst which 14.5% showed MWs > 100000 Da, thus indicating an oligomerisation of LMWs to melanoidins under roasting conditions. To investigate the physiological effects of these MRPs, xenobiotic enzyme activities were analysed in intestinal Caco-2 cells. For Phase-I NADPH-cytochrome c-reductase, the activity in the presence of the LMW and HMW fraction was decreased by 13% and 22%: respectively. Phase-II glutathione-S-transferase activity decreased by 15% and 18%, respectively, after incubation with the LMW and the HMW fractions. Considering the different yields, 30% and 10%, respectively, of the LMW and the HMW fractions, the total amount of the LMW fraction present in the glucose-glycine mixture is more active in modulating three enzyme activities than that of the HMW fraction.

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The properties of melanoidins prepared from glucose and glycine (GG) were investigated by a three step purification protocol consisting of dialysis, gel filtration at high ionic strength and ion metal affinity chromatography. The high molecular weight fraction obtained in the GG system is responsible for 80% of the total brown colour and its antioxidative ability was about 1/4 of that of Trolox measured by the inhibition of linoleic acid oxidation. GG melanoidins have good affinity towards Cu (II) (32% bound to the resin) while it is much lower towards Pb (II) (10%) and Fe (II) (5%). Capillary zone electrophoresis analysis suggests that GG melanoidins are positively charged, although no signal was observed analysing melanoidins by matrix-assisted laser desorption-ionisation time-of-flight mass spectrometry (MALDI-TOF/MS).

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Mixtures of glycine, glucose, and starch were extrusion cooked using sodium hydroxide at 0, 3, and 6 g/L of extruder water feed, 18% moisture, and 120, 150, and 180 degreesC target die temperatures, giving extrudates with pH values of 5.6, 6.8, and 7.4. Freeze-dried equimolar solutions of glucose and glycine were heated either dry or after equilibration to similar to 13% moisture at 180 degreesC in a reaction-tube system designed to mimic the heating profile in an extruder. Volatile compounds were isolated onto Tenax and analyzed by gas chromatography-mass spectrometry. For the extrudates, total yields of volatiles increased with decreasing pH at 180 degreesC, reached a maximum at pH 6.S at 150 degreesC, and increased with increasing pH at 120 degreesC. Amounts increased with temperature at all pH values. Pyrazines were the most abundant class for all sets of conditions (54-79% of total volatiles). Pyrroles, ketones, furans, oxazoles, and pyridines were also identified. Yields of volatiles from the reaction-tube samples increased by > 60% in the moist system. Levels of individual classes also increased in the presence of moisture, except pyrazines, which decreased similar to3.5-fold. Twenty-one of the compounds were common to the reaction-tube samples and the extrudates.

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Collagen-related peptide is a selective agonist for the platelet collagen receptor Glycoprotein VI. The triple helical peptide contains ten GPO triplets/strand (single letter amino acid nomenclature, where O is hydroxyproline) and so over-represents GPO compared with native collagen sequence. To investigate the ability of Glycoprotein VI to recognize GPO triplets in a setting more representative of the collagens, we synthesized a set of triple helical peptides containing fewer GPO triplets, varying their number and spacing within an inert (GPP)(n) backbone. The adhesion of recombinant human Glycoprotein VI ectodomain, like that of human platelets, to these peptides increased with their GPO content, and platelet adhesion was abolished by the specific anti-Glycoprotein VI-blocking antibody, 10B12. Platelet aggregation and protein tyrosine phosphorylation were induced only by cross-linked peptides and only those that contained two or more GPO triplets. Such peptides were less potent than cross-linked collagen-related peptide. Our data suggest that both the sequences GPOGPO and GPO center dot center dot center dot center dot center dot center dot center dot center dot center dot GPO represent functional Glycoprotein VI recognition motifs within collagen. Furthermore, we propose that the (GPO)(4) motif can support simultaneous binding of two glycoprotein VI molecules, in either a parallel or anti-parallel stacking arrangement, which could play an important role in activation of signaling.

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Cathepsins are known to have many important physiological roles and provide a viable target for inhibition. Fluorobenzoyl dipeptide derivatives were synthesized and tested for biological activity in an effort to find an efficient inhibitor of the cysteine protease cathepsin L. Thirty-six novel inhibitors (1-36) were synthesized from protected amino acids via the standard DCC/HOBt coupling protocol, containing a benzyl ester or a nitrile as an electrophilic warhead. The activity of the inhibitors was evaluated against cathepsin L and IC50 values calculated. Modification of both amino acids and terminal groups afforded compounds with single digit micromolar inhibition. Results utilizing the benzoyl-L-leucine-glycine nitrile backbone are comparable to that for the commercially available inhibitor 39.

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Homology modeling was used to build 3D models of the N-methyl-D-aspartate (NMDA) receptor glycine binding site on the basis of an X-ray structure of the water-soluble AMPA-sensitive receptor. The docking of agonists and antagonists to these models was used to reveal binding modes of ligands and to explain known structure-activity relationships. Two types of quantitative models, 3D-QSAR/CoMFA and a regression model based on docking energies, were built for antagonists (derivatives of 4-hydroxy-2-quinolone, quinoxaline-2,3-dione, and related compounds). The CoMFA steric and electrostatic maps were superimposed on the homology-based model, and a close correspondence was marked. The derived computational models have permitted the evaluation of the structural features crucial for high glycine binding site affinity and are important for the design of new ligands.

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An approach for evaluation of binding selectivity was suggested and exemplified using glycine/NMDA and AMPA receptors. For analyzing the pairwise selectivity, we propose to use the difference between biological activities (expressed as -log Ki) of ligands with respect to different receptor subtypes as a dependent variable for building comparative molecular field analysis (CoMFA) models. The resulting fields (which will be referred to as the "selectivity fields") indicate the ways of increasing selectivity of binding, inhibition, etc. As an example, CoMFA of a set of pyrazolo[1,5-c]quinazolines and triazolo[1,5-c]quinazolines was used for considering the binding selectivity with respect to glycine/NMDA and AMPA receptors. In addition, the mapping of these fields onto the molecular models of the corresponding receptors makes it possible to reveal the reasons for experimentally observed selectivity as well as to suggest additional ways of increasing selectivity.

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Herein we report the discovery and SAR of a novel series of non-MPEP site metabotropic glutamate receptor 5 (mGlu(5)) positive allosteric modulators (PAMs) based on an aryl glycine sulfonamide scaffold. This series represents a rare non-MPEP site mGlu(5) PAM chemotype.