Synthesis and Biological Characterization of Monomeric and Tetrameric RGD-Cryptophycin Conjugates

The effective delivery of cytotoxic agents to tumor cells is a key challenge in anticancer therapy. Multivalent integrinspecific ligands are considered a promising tool to increase the binding affinity, selectivity, and internalization efficiency of small-molecule drug conjugates. Herein, we report the synthesis and biological evaluation of a multimeric conjugate containing the high-affinity integrin α_vβ₃ binding ligand RAFT-c(RGDfK)₄, a lysosomally cleavable Val-Cit linker, and cryptophycin-55 glycinate, a potent inhibitor of tubulin polymerization. In vitro cytotoxicity assays verified that the multimeric RGD-cryptophycin conjugate displays improved potency compared to the monomeric analogue in integrin α_vβ₃ overexpressing tumor cell lines, while significantly reduced activity was observed in the integrin-negative cell line.     

Structural feature of calf thymus deoxyribonucleic acid–ruthenium(III) interaction in aqueous solution by difference Fourier transformed infrared spectroscopy

Here is the report on the interaction of ruthenium(III) species with DNA in aqueous solution at pH 7.42 by Fourier transformed infrared difference spectroscopy. Under the physiological pH and molar ratio [Ruthenium]/[DNA]?=?1/80–1/20 direct binding to guanine-N7, adenine-N7, and surprising binding to exocyclic thymine-O2 was found. At low metal concentration no significant shift of the absorption bands was observed, only nonspecific electrostatic binding of ruthenium(III) with negatively charged phosphate groups occurred. The increase of ruthenium(III) concentration caused DNA double helix destabilization and direct binding of the metal cation to guanine-N7 and thymine-O2. At higher ruthenium(III) concentrations denaturation of the DNA helix is evident with no apparent binding of ruthenium(III) to adenine and cytosine. Helix opening allows migration of ruthenium(III) ions from phosphate to available nucleobases (guanine and thymine). No alteration of the sugar phosphate geometry was observed thus confirming that DNA remains in B conformation.     

Comparative study of the textural and structural properties of the aerogel and xerogel sulphated zirconia

Aerogel and xerogel sulphated zirconia with defined atomic ratio S/Zr = 0.5 and molar hydrolysis ratio h = nH₂O/nZrO₂ = 3 show different textural and structural properties after calcination at high temperatures. The aerogel obtained just after solvent evacuation develops only the tetragonal phase, whereas the xerogel dried in an oven is amorphous. Heating to a temperature above 833 K, leads to transition of the tetragonal phase to the monoclinic one for the two solids, due to sulphur loss but the tetragonal phase remains stable for the aerogel . Raman, Infrared and XPS spectroscopies show that the loss of the sulphur at high temperatures seems to be easier for the xerogel than for the aerogel.     

Speciation of239U and238Np produced by radiative neutron capture

Various simple and complex compounds of²³⁸U and²³⁷Np have been irradiated in a neutron flux. The chemical state of²³⁹U and²³⁸Np formed in (n, ) reactions has been determined as a function of the initial oxidation state of the actinide elements and of the nature of ligands. A scheme for the chemical reactions following neutron capture is proposed.     

Effect of gas pulsation on long slugs in horizontal gas–liquid pipe flow

Long liquid slugs reaching a length of several hundreds of pipe diameter may appear when transporting gas and liquid in horizontal or nearly horizontal pipelines. These long slugs may cause system vibration, separator flooding, and operational problems for the downstream processing facilities. Although mainly short hydrodynamic slugs have been observed in offshore gas and oil production fields over the past years, the appearance of the long slugs is becoming more common as many production fields are now more mature and reach end of field life, giving reduced production rates and reduced operational pressure.     

Methods for the numerical solution of the Benjamin‐Bona‐Mahony‐Burgers equation

L^∞‐error estimates for finite element for Galerkin solutions for the Benjamin‐Bona‐Mahony‐Burgers (BBMB) equation are considered. A priori bound and the semidiscrete Galerkin scheme are studied using appropriate projections. For fully discrete Galerkin schemes, we consider the backward Euler method and analyze the corresponding error estimates. For a second order accuracy in time, we propose a three‐level backward method. © 2008 Wiley Periodicals, Inc. Numer Methods Partial Differential Eq, 2008     

Effect of titanium based complex catalyst and carbon nanotubes on hydrogen storage performance of magnesium

Mg (MgH₂)-based composites, using carbon nanotubes (CNTs) and pre-synthesized titanium based complex (TCat) as the catalysts, were prepared by high energy ball milling technique. The use of both catalysts demonstrated markedly improved the hydrogen storage performance, e.g. a significant increase of hydrogen release rate and decrease of desorption temperature. The synthesized composites can absorb almost 6 wt% of hydrogen within 3 min at 200 °C and desorb 6 wt% hydrogen in 10 min at 310 °C. The influence of CNTs and TCat on desorption temperature was also investigated by using temperature programmed desorption (TPD). The TPD results reveal that the peak desorption temperature and the onset temperature can be lowered by 109 °C and 155 °C, respectively, compared to the non-catalyzed MgH₂. The reaction enthalpy and entropy of hydrogen desorption for the synthesized MgH₂-based composites are calculated by the van’t Hoff analysis to be 73.1 kJ/mol H₂ and 130.2 J/mol H₂ K, respectively.