Structure‐Based Optimization of the Terminal Tripeptide in Glycopeptide Dendrimer Inhibitors of Pseudomonas aeruginosa Biofilms Targeting LecA

The galactopeptide dendrimer GalAG2 ((β‐Gal‐OC₆H₄CO‐Lys‐Pro‐Leu)₄(Lys‐Phe‐Lys‐Ile)₂Lys‐His‐Ile‐NH₂) binds strongly to the Pseudomonas aeruginosa (PA) lectin LecA, and it inhibits PA biofilms, as well as disperses already established ones. By starting with the crystal structure of the terminal tripeptide moiety GalA‐KPL in complex with LecA, a computational mutagenesis study was carried out on the galactotripeptide to optimize the peptide–lectin interactions. 25 mutants were experimentally evaluated by a hemagglutination inhibition assay, 17 by isothermal titration calorimetry, and 3 by X‐ray crystallography. Two of these tripeptides, GalA‐KPY (dissociation constant (K_D)=2.7 μM ) and GalA‐KRL (K_D=2.7 μM ), are among the most potent monovalent LecA ligands reported to date. Dendrimers based on these tripeptide ligands showed improved PA biofilm inhibition and dispersal compared to those of GalAG2 , particularly G2KPY ((β‐Gal‐OC₆H₄CO‐Lys‐Pro‐Tyr)₄(Lys‐Phe‐Lys‐Ile)₂Lys‐His‐Ile‐NH₂). The possibility to retain and even improve the biofilm inhibition in several analogues of GalAG2 suggests that it should be possible to fine‐tune this dendrimer towards therapeutic use by adjusting the pharmacokinetic parameters in addition to the biofilm inhibition through amino acid substitutions.     

Acid–base sensor based on sol–gel encapsulation of bromothymol blue in silica: application for milk spoilage detection

Journal of Sol-Gel Science and Technology - In this work, silica capsules containing bromothymol blue (BTB) were synthesized by a modified Stöber sol–gel method. These silica capsules...     

Polarization-insensitive nonlinear optical loop mirror demultiplexer with twisted fiber

We experimentally demonstrate reduction of the polarization sensitivity of a nonlinear optical loop mirror (NOLM) from 5 to 0.5 dB by use of 550 m of twisted dispersion-shifted fiber with a twist rate of 8 turns/m (24 turns/beat length). The twisting of the fiber induces circular birefringence and equates the parallel-and the orthogonal-polarization nonlinear phase-shift terms. Experimental results show that the polarization sensitivity monotonically decreases from 5 dB for nontwisted fiber to 0.5 dB for fiber that is twisted at a rate of 8 turns/m, and the twist rate should be more than 4 turns/m (>10 turns/beat length) for emulation of circularly polarized fiber. The minimum polarization sensitivity occurs when the control-pulse polarization is aligned with one of the eigenmodes of the twisted fiber. With the fiber twisted at a rate of 8 turns/m in the NOLM, the nonlinear transmission is 23% at a switching energy of 4 pJ/pulse. Simulations confirm the observed behavior and show that the remaining polarization sensitivity results from energy transfer between orthogonal modes of the signal pulse.     

Heavy-ion friction force from a gas-kinetic model

A friction force is derived from the two-body collisions of projectile nucleons with target nucleons in the overlap region of their densities. We treat the diffuse surfaces of the heavy ions as Fermi gases. A certain average of the resulting friction force turns put to be identical in structure with the phenomenological Tsang-Swiatecki linear force. In our approach, the strength coefficient of the latter force can be calculated from the free two-nucleon scattering cross section without adjustable parameters. We obtain a strength which agrees well with the value found by Siwek-Wilczyńska and Wilczyński from an empirical fit.     

Transfer reactions induced by 17, 18O on 12, 13C at c.m. energies between 12.6 TO 14.0 MeV

Angular distributions for one-neutron and many-nucleon transfer reactions were measured in the systems ^{17, 18}O and ^{12, 13}C at c.m. energies between 12.6 to 14.0 MeV. All the cross sections were analyzed in terms of the full-recoil finite-range DWBA model. For multi-nucleon transfer processes an inert cluster transfer was assumed. The sensitivity of DWBA calculations to various parameter sets is discussed, and the effect of the no-recoil approximation on the phase and magnitude of the transfer amplitude is studied. For one-neutron transfer reactions the forward part of the angular distributions was reproduced reasonably well by the DWBA model, yielding satisfactory spectroscopic information. The rise of the cross section at the backward angles was not reproduced by the DWBA model. Possible contributions of cluster-exchange and compound-nucleus reactions are discussed. For multi-nucleon transfer reactions poorer fits were obtained, particularly in the ¹⁸O+¹²C system.     

Microscale Synthetic Schlieren

We develop the axisymmetric Synthetic Schlieren technique to study the wake of a microscale sphere settling through a density stratification. A video-microscope was used to magnify and image apparent displacements of a micron-sized random-dot pattern. Due to the nature of the wake, density gradient perturbations in the horizontal greatly exceed those in the vertical, requiring modification of previously developed axisymmetric techniques. We present results for 780 and 383 μm spheres, and describe the limiting role of noise in the system for a 157 μm sphere. This technique can be instrumental in understanding a range of ecological and environmental oceanic processes on the microscale.

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Stereoselective total synthesis of aminoiminohexitols via carbamate annulation

New methodology for the preparation of a variety of aminoiminohextitols is described. Key in the synthesis is the application of a diastereoselective Strecker reaction and the extension of our carbamate annulation methodology to protected and functionalized alkenylamines. Insight into the effects that the substitution patterns of the alkenylamines have on the diastereoselectivity of the iodocyclization and carbamate annulation is discussed. An evaluation of the glycosidase inhibitory activity of the aminoiminohexitols and derivatives is also presented, with the previously undisclosed D-talo isomer showing good selective inhibition of β-D-glucosidase.     

Chemical composition of the essential oil of Pituranthos scoparius

The essential oils obtained by hydro distillation of the aerial parts of Pituranthos scoparius were collected from different regions of Algeria and gave various yields ranging from 0.6 up to 2.8% (v/w). These samples were analyzed by GC and GC-MS showing the occurrence of monoterpene hydrocarbons and some oxygenated compounds. The major components were alpha-pinene (4.4-35.8%), limonene (0.8-66.5%), bornyl acetate (tr-9.6%), myristicin (tr-31.1) and dill apiole (0.4-47.3%). The aerial parts of P. scoparius could be either very rich or very poor in limonene, myristicin or dill apiole. Cluster analysis shows differences in essential oil compositions of samples coming from the different area collected.