Antimicrobial activity of a monomer and its polymer based on quinolone

An acryl monomer containing the quinolone moiety was synthesized and then polymerized with azobisisobutyronitrile in a dimethylformamide solution. The resulting polymer as well as the corresponding monomer exhibited an excellent antibacterial activity. The poly(acrylated quinolone) (PQ) was compounded with other ordinary synthetic polymers such as low‐density polyethylene (LDPE), poly(butylene succinate) (PBS), poly(methyl methacrylate) (PMMA), maleated polypropylene (PPMA), and polycaprolactone (PCL). The polymer blends reduced the viable cell number significantly on contact during the shake flask test even when the PQ content was as low as 1 wt %. © 2003 Wiley Periodicals, Inc. J Appl Polym Sci 90: 1797–1801, 2003     

Anti-Inflammatory Effect of Very High Dose Local Vessel Wall Statin Administration: Poly(L,L-Lactide) Biodegradable Microspheres with Simvastatin for Drug Delivery System (DDS)

Atherosclerosis involves an ongoing inflammatory response of the vascular endothelium and vessel wall of the aorta and vein. The pleiotropic effects of statins have been well described in many in vitro and in vivo studies, but these effects are difficult to achieve in clinical practice due to the low bioavailability of statins and their first-pass metabolism in the liver. The aim of this study was to test a vessel wall local drug delivery system (DDS) using PLA microstructures loaded with simvastatin. Wistar rats were fed high cholesterol chow as a model. The rat vessels were chemically injured by repeated injections of perivascular paclitaxel and 5-fluorouracil. The vessels were then cultured and treated by the injection of several concentrations of poly(L,L-lactide) microparticles loaded with the high local HMG-CoA inhibitor simvastatin (0.58 mg/kg) concentration (SVPLA). Histopathological examinations of the harvested vessels and vital organs after 24 h, 7 days and 4 weeks were performed. Microcirculation in mice as an additional test was performed to demonstrate the safety of this approach. A single dose of SVPLA microspheres with an average diameter of 6.4 μm and a drug concentration equal to 8.1% of particles limited the inflammatory reaction of the endothelium and vessel wall and had no influence on microcirculation in vivo or in vitro. A potent pleiotropic (anti-inflammatory) effect of simvastatin after local SVPLA administration was observed. Moreover, significant concentrations of free simvastatin were observed in the vessel wall (compared to the maximum serum level). In addition, it appeared that simvastatin, once locally administered as SVPLA particles, exerted potent pleiotropic effects on chemically injured vessels and presented anti-inflammatory action. Presumably, this effect was due to the high local concentrations of simvastatin. No local or systemic side effects were observed. This approach could be useful for local simvastatin DDSs when high, local drug concentrations are difficult to obtain, or systemic side effects are present.     

G-Quadruplex in Gene Encoding Large Subunit of Plant RNA Polymerase II: A Billion-Year-Old Story

G-quadruplexes have long been perceived as rare and physiologically unimportant nucleic acid structures. However, several studies have revealed their importance in molecular processes, suggesting their possible role in replication and gene expression regulation. Pathways involving G-quadruplexes are intensively studied, especially in the context of human diseases, while their involvement in gene expression regulation in plants remains largely unexplored. Here, we conducted a bioinformatic study and performed a complex circular dichroism measurement to identify a stable G-quadruplex in the gene RPB1, coding for the RNA polymerase II large subunit. We found that this G-quadruplex-forming locus is highly evolutionarily conserved amongst plants sensu lato (Archaeplastida) that share a common ancestor more than one billion years old. Finally, we discussed a new hypothesis regarding G-quadruplexes interacting with UV light in plants to potentially form an additional layer of the regulatory network.     

Tandem Chemoselective 1,2‐/1,4‐Migration of the Thio Group in Keto Thioesters: An Efficient Approach to Substituted Butenolides

We report herein an efficient and mechanistically unique tandem chemoselective 1,2‐/1,4‐migration of the thio group in keto thioesters that provides substituted butenolides in moderate to excellent yields. Thus, α‐keto thioesters in the presence of stabilized phosphonate carbanions undergo tandem 1,2‐sulfur migration; whereas 1,4‐migration of the thio group has been achieved with the same thioesters after the treatment with Wittig reagents followed by BF₃⋅OEt₂‐catalyzed tandem reaction. The crossover experiments and the isolation of intermediates reveal a stepwise mechanism for both of these transformations.

     

Features of compacting hydrogen-doped granules of a VT5-1kt titanium alloy

The effect of hydrogen on consolidation of granules of the VT5-1kt alloy, as well as the structure, mechanical characteristics, and fracture micromechanism of a compact produced by the hot-isostatic-pressing technique, is studied. It is established that hydrogen doping allows obtainment of a compact of the VT5-1kt alloy of 100% density with a high complex of properties in the course of a few minutes at such temperature-strength conditions in which the consolidation of granules is not realized. It is shown that the process of consolidation of hydrogenated granules proceeds more effectively in the (α + β) region.     

InP based semiconductor structures for radiation detection

We report the preparation of semi-insulating InP single crystals of p-type conductivity and intentionally undoped p-type epitaxial layers for radiation detection. We focus on (i) the growth of InP single crystals doped with copper by the Czochralski technique and their subsequent temperature annealing to convert them to a semi-insulating (SI) state of p-type conductivity, and (ii) the growth of thick (>10 μm) p-type InP layers by liquid phase epitaxy with an admixture of Pr and Dy. Grown layers and single crystals were examined by low-temperature photoluminescence spectroscopy, capacitance-voltage and temperature dependent Hall measurements. An efficient purification due to rare earth (RE) admixture has been observed and layers grown with the addition of Pr and Dy exhibit the change of electrical conductivity from n to p at certain RE concentration in the melt. Dominant acceptors responsible for conductivity conversion have been identified. Three types of detection structures exploiting the Schottky or Schottky like contacts on pure and SI p-type InP or exploiting the p–n junction were designed.     

Structure and properties of 6061 + 26 mass% Si aluminum alloy produced via coupled rapid solidification and KOBO-extrusion of powder

Experiments on mechanical consolidation of rapidly solidified (RS) powder of 6061 + 26 mass% Si alloy were performed using the oscillating-die extrusion method. The RS powder was wrapped in thin-wall 6061-alloy cup 35 mm in diameter and vacuum-compressed by means of 100 ton press. Bars 8 mm in diameter were extruded with cross-section reduction of λ = 19 without any preheating of the charge. Tubes with a diameter/wall thickness of 14 mm/1 mm and cross-section reduction of λ = 33 were also manufactured with success. TEM/STEM observations revealed a very fine structure of as-extruded material and bimodal distribution of quasi-spherical silicon particles. Statistical analysis revealed a silicon fine fraction of 0.1–0.7 μm and a coarse fraction 2.1–2.5 μm in diameter. Examination by means of TEM did not reveal any significant changes in the morphology of the silicon particles, even when a high extrusion ratio and the material annealing after deformation were used. Hot compression tests on as-extruded rods (λ = 19) and preliminary annealed samples were performed at a constant true strain rate of 5 × 10^?3 s^?1 within the temperature range of 293–823 K. High strength of the material and relatively high ductility of samples deformed by compression up to ?_t ? 0.4 were observed. The maximum flow stress value for as-extruded material was reduced with deformation temperature from ～390 to ～3.5 MPa for 293 and 823 K, respectively. Annealing of the samples at 773 K/30 min was found to reduce the maximum flow stress by 30–40%. Tensile strengths of similar as-cast alloys and materials manufactured by means of other powder metallurgy methods were shown for the purpose of comparison.     

Nucleation and growth of the electrodeposited iron layers in the presence of an external magnetic field

The effect of an uniform magnetic field with a flux density up to 1 T and different configurations relative to the electrode surface on the electrocrystallization of Fe on polycrystalline Au(1 1 1) from acidic sulphate electrolyte has been investigated. It was found, irrespective of the applied parameters, that the deposition proceeds through successive nucleation and growth steps. The first one related to 2D growth was followed by a second nucleation and 3D diffusion controlled growth. At potential of −1500 and −1550 mV_MSE nucleation proceeds via a progressive mode, while at −1650 mV_MSE it follows an instantaneous mode. A strong influence of the parallel-to-electrode magnetic field on the nucleation processes was found for the progressive mode, which leads to the increase of the growth rate and as a consequence to retardation of the nucleation rate of the 3D step. Additionally, in this configuration at a sufficiently high magnetic flux density a third nucleation step could be observed (3D), which was found to be also affected by a magnetic field. No effect of a perpendicular-to-electrode magnetic field on the nucleation has been observed. The effects of a magnetic field on the nucleation and growth processes are discussed with respect to the magnetohydrodynamic effect (MHD) and confirmed by rotating disc electrode (RDE) experiments.     

Structure and properties of hot-rolled strips obtained from titanium chips without chip remelting

Introduction of hydrogen technology provided hot-rolling fabrication of thin strips from chips of VT1-0 titanium alloy without chip remelting. It is established that the plasticity of strips made from this alloy largely depends on the presence of excess dispersed particles in the structure. It is assumed that they are the sparingly soluble oxides formed during the destruction in the course of pressure treatment of the oxide film retained on the chip surface. After homogenization, which can be combined with vacuum annealing for hydrogen removal, the structure and mechanical properties of the strips obtained by hydrogen technology correspond to the characteristics of semifinished products fabricated by ingot technology.