One-pot synthesis and in vivo biological evaluation of new pyrimidine privileged scaffolds as potent anti-inflammatory agents

Research on Chemical Intermediates - A simple methodology has been developed for the synthesis of diverse members of multifunctionalized 4-hydroxy-2-methyl-6-(phenyl)pyrimidine-5-carbonitrile...     

Quantification of fexofenadine in human plasma by liquid chromatography coupled to electrospray tandem mass spectrometry using mosapride as internal standard

A rapid high-performance liquid chromatography/positive ion electrospray tandem mass spectrometry method was developed and validated for the quantification of fexofenadine in human plasma using mosapride as internal standard. Following solid-phase extraction, the analytes were separated using an isocratic mobile phase on a reverse-phase column and analyzed by MS/MS in the multiple reaction monitoring mode using the respective [M+H]+ ions, m/z 502/466 for fexofenadine and m/z 422/198 for the IS. The method exhibited a linear dynamic range of 1-500 ng/mL for fexofenadine in human plasma. The lower limit of quantification was 1 ng/mL with a relative standard deviation of less than 5% for fexofenadine. Acceptable precision and accuracy were obtained for concentrations over the standard curve range. The total chromatographic run time of 2 min for each sample made it possible to analyze more than 400 human plasma samples per day. The validated method has been successfully used to analyze human plasma samples for application in pharmacokinetic, bioavailability or bioequivalence studies.     

Structure-based engineering of strictosidine synthase: auxiliary for alkaloid libraries

The highly substrate-specific strictosidine synthase (EC 4.3.3.2) catalyzes the biological Pictet-Spengler condensation between tryptamine and secologanin, leading to the synthesis of about 2000 monoterpenoid indole alkaloids in higher plants. The crystal structure of Rauvolfia serpentina strictosidine synthase (STR1) in complex with strictosidine has been elucidated here, allowing the rational site-directed mutation of the active center of STR1 and resulting in modulation of its substrate acceptance. Here, we report on the rational redesign of STR1 by generation of a Val208Ala mutant, further describing the influence on substrate acceptance and the enzyme-catalyzed synthesis of 10-methyl- and 10-methoxystrictosidines. Based on the addition of strictosidine to a crude strictosidine glucosidase preparation from Catharanthus cells, a combined chemoenzymatic approach to generating large alkaloid libraries for future pharmacological screenings is presented.     

Quantitative determination of macroelement and microelement content of fresh and processed bamboo shoots by wavelength dispersive X-ray fluorescence spectrometry

Bamboo shoots are considered as healthy and nutritional food as they supply proteins, dietary fiber, phenols, phytosterols, vitamins, and minerals in considerable quantities and capture a novel place in the spectrum of plant foods. Besides nutrients and bioactive compounds, shoots also contain antinutrient (cyanogen) that needs to be removed by adequate processing prior to consumption. This study was undertaken to investigate the effects of fermentation, brine preservation, and boiling on levels of mineral elements in shoots of Dendrocalamus hamiltonii using wavelength dispersive X-ray fluorescence (WD-XRF) spectrometry. WD-XRF spectrometry is a method that causes the least destruction to the raw plant material as no harsh chemicals are used and gives the most accurate results. Fermentation process resulted in significant increase in the levels of Rb (9%), S (11%), Mg (12%), Zn (46%), Ca (56%), and Fe (87%); however, Na (18.79 g/100 g, dry weight), Cl (24.73 g/100 g, dry weight), and Br (20.0 mg/100 g, dry weight) content increased drastically after brine preservation. Boiling increased the levels of Fe by 139% but did not affect the Rb (20.0 mg/100 g, dry weight) and Zn content (10.2 mg/100 g, dry weight) of the shoots. In general, fermentation, which led to the lowest loss of mineral elements, appears the best method in enhancement and retention of the mineral content in bamboo shoots and holds the prospect at industrial and society levels.     

Classical model for diffusion and thermalization of heavy quarks in a hot medium: memory and out-of-equilibrium effects

We consider a simple model for the diffusion of heavy quarks in a hot bath,modeling the latter by an ensemble of oscillators distributed according to either a thermal distribution or to an out-of-equilibrium distribution with a saturation scale.In this model it is easy to introduce memory effects by changing the distribution of oscillators:we model them by introducing a Gaussian distribution,dN/dω.which can be deformed continuously from a δ-function,giving a Markov dissipation, to a broad kernel with memory.Deriving the equation of motion of the heavy quark in the bath,we remark how dissipation comes out naturally as an effect of the back-reaction of the oscillators on the bath.Moreover,the exact solution of this equation allows to define the thermalization time as the time necessary to remove any memory of the initial conditions.We find that the broadening of the dissipative kernel,while keeping the coupling fixed,lowers the thermalization time.We also derive the fluctuation-dissipation theorem for the bath,and use it to estimate the kinematic regime in which momentum diffusion of the heavy quark dominates over drift.We find that diffusion is more important as long as K_0/ε is small,where K_0 and ε denote the initial energy of the heavy quark and the average energy of the bath,respectively.     

Phase transition in Na2SO4: all five polymorphic transformations in DSC

In this investigation, we have characterized the Na₂SO₄ using differential scanning calorimetry (DSC). It is well known that Na₂SO₄ exhibits five polymorphs. However, the experimental evidence for all five polymorphs has never been observed in DSC. In this investigation, the five polymorphic transformations have been observed in heating cycle. Furthermore, the transition I–II is observed, which is not reversible. In addition, phase transition temperature for V→IV and IV→III transition appears to be much closed and may get unnoticed.     

Optical studies of two dimensional gratings in fused silica, GE 124, and Foturan glasses fabricated using femtosecond laser pulses

Herein we present results on the femtosecond laser direct writing and optical characterization studies of two dimensional gratings in fused silica, GE 124, and Foturan^™ glasses. Varieties of structures were achieved with varying input energy and spatial orientation of the samples. Various characterization techniques including fluorescence spectroscopy, micro-Raman spectroscopy, and laser confocal microscopy were employed to analyze the structural and physical modifications at the focal volume resulting in change of refractive index. Diffraction efficiencies of 9–12% were observed from the grating structures. A broad-band emission was observed in the laser-modified region of the Foturan glass. The obtained results are analyzed in the light of recent work in similar glasses and exploring the applications of such structures in the fields of photonics.