Aminolysis of Aziridines Catalyzed by Samarium Iodides

Abstract  

Samarium diiodide is an efficient catalyst for the aminolysis of either activated or non activated aziridines with aromatic amines. A variety of N-diprotected β-diamines has been prepared including new products. The comparison of the N-protecting groups of aziridines in reactions catalyzed by samarium diiodide or by samarium iodobinaphtholate indicates that N-Boc protection leads to the best results.     

Comparison of antimicrobial resistance of Campylobacter jejuni isolated from humans, chickens, raw milk, and environmental water in Québec

This study compares the occurrence of antimicrobial resistance to erythromycin, ciprofloxacin, and tetracycline among 384 Campylobacter jejuni isolates from humans (245), fresh whole retail chickens (56), raw milk (33), and environmental water (41) collected between 2000 and 2003 in Québec, Canada. Resistance to ciprofloxacin was significantly more frequent in human isolates acquired abroad than in those acquired locally (50 versus 5.9%; P < 0.001); ciprofloxacin resistance was almost absent in water, chicken, and raw milk isolates. In contrast, resistance to erythromycin was significantly more common in chicken than in locally acquired human isolates (16 versus 3.0%, respectively; P < 0.001); no erythromycin resistance was found among water, raw milk, and human isolates acquired abroad. Resistance to tetracycline was significantly more common in chicken and human isolates acquired locally (58.9 and 45.8%, respectively) than in raw milk and water isolates (9.1 and 7.3%, respectively, P < 0.001). Tetracycline resistance was also observed in 44.4% of human isolates acquired abroad. No human isolate was resistant to both ciprofloxacin and erythromycin, but one chicken isolate was resistant to all three antimicrobial agents. Our results suggest that from 2000 to 2003 in Québec, antimicrobial resistance remained stable among locally acquired C. jejuni human clinical isolates and might even have decreased. However, the high erythromycin resistance rate observed among chicken isolates is concerning because of the risk of transmission of such isolates to humans. Additional studies are needed to monitor trends in antimicrobial resistance among food, environment, and human C. jejuni isolates as well as antibiotic use in animals.     

Coating carbon nanotubes with a polystyrene-based polymer protects against pulmonary toxicity

Background  

carbon nanotubes (CNT) can have adverse effects on health. Therefore, minimizing the risk associated with CNT exposure is of crucial importance. The aim of this work was to evaluate if coating multi-walled CNT (MWCNT) with polymers could modify their toxicity, thus representing a useful strategy to decrease adverse health effects of CNT. We used industrially-produced MWCNT uncoated (NT1) or coated (50/50 wt%) with acid-based (NT2) or polystyrene-based (NT3) polymer, and exposed murine macrophages (RAW 264.7 cell line) or Balb/c mice by intratracheal administration. Biological experiments were performed both in vitro and in vivo, examining time- and dose-dependent effects of CNT, in terms of cytotoxicity, expression of genes and proteins related to oxidative stress, inflammation and tissue remodeling, cell and lung tissue morphology (optical and transmission electron microscopy), and bronchoalveolar lavage fluid content analysis.     

The development of a silica nanoparticle-based label-free DNA biosensor

A silica nanoparticle-based DNA biosensor capable of detecting Bacillus anthracis bacteria through the use of unlabelled ss-oligonucleotides has been developed. The biosensor makes use of the optical changes that accompany a nanoparticle-immobilized cationic conjugated polymer (polythiophene) interacting with single-stranded vs. hybridized oligonucleotides, where a fluorescence signal appears only when hybridized DNA is present (i.e. only when the ss-oligonucleotide interacting with the polymer has hybridized with its complement). In order to enhance the sensitivity of the biosensor, two different nanoparticle architectures were developed and used to elucidate how the presence of neighboring fluorophores on the nanoparticle surface affects F?rster-resonant energy transfer (FRET) between the polythiophene/oligonucleotide complex (FRET donor) and the fluorophores (FRET acceptors). We demonstrate that the silica nanoparticle-based FRET platform lowers the limit of detection at least 10-fold in comparison to the polythiophene itself, and allows the detection of ～2 × 10(-12) moles of ss-oligonucleotide in a 100 μL sample with a standard fluorimeter (i.e. has a limit of detection of ～2 nM ssDNA). Such nanoparticle-based biosensor platforms are beneficial because of the robustness and stability inherent to their covalent assembly and they provide a valuable new tool that may allow for the sensitive, label-free detection (the target DNA that produces the fluorescence signal is unlabelled) without the use of polymerase chain reaction.     

Irreversible changes in protein conformation due to interaction with superparamagnetic iron oxide nanoparticles

The understanding of the interactions between nanomaterials and proteins is of extreme importance in medicine. In a biological fluid, proteins can adsorb and associate with nanoparticles, which can have significant impact on the biological behavior of the proteins and the nanoparticles. We report here on the interactions of iron saturated human transferrin protein with both bare and polyvinyl alcohol coated superparamagnetic iron oxide nanoparticles (SPIONs). The exposure of human transferrin to SPIONs results in the release of iron, which changes the main function of the protein, which is the transport of iron among cells. After removal of the magnetic nanoparticles, the original protein conformation is not recovered, indicating irreversible changes in transferrin conformation: from a compact to an open structure.     

Effects of the nature of the doping salt and of the thermal pre-treatment and sintering temperature on Spark Plasma Sintering of transparent alumina

A slurry of α-Al₂O₃ was doped with Mg, Zr and La nitrates or chlorides, in various amounts in the range 150-500 wt ppm and then freeze-dried to produce nanosized doped powder (∼150 nm). The powder was sintered by SPS to yield transparent polycrystalline alpha alumina. The influence of the nature of the doping element and the starting salt, the thermal treatment before sintering and the sintering temperature on the transparency of the ceramics were investigated. The transparency of the ceramics of nanosized Al₂O₃ was shown to depend mainly on the way the powder was prepared, the nature of the doping salt also had an effect. Finally, a high real inline transmittance, reaching 48.1% was achieved after optimization.     

Unique hue data for colour appearance models. Part I: Loci of unique hues and hue uniformity

Psychophysical experiments were conducted to assess unique hues on a CRT display for a large sample of colour‐normal observers (n = 185). These data were then used to evaluate the most commonly used colour appearance model, CIECAM02, by transforming the CIEXYZ tristimulus values of the unique hues to the CIECAM02 colour appearance attributes, lightness, chroma and hue angle. We report two findings: (1) the hue angles derived from our unique hue data are inconsistent with the commonly used Natural Color System hues that are incorporated in the CIECAM02 model. We argue that our predicted unique hue angles (derived from our large dataset) provide a more reliable standard for colour management applications when the precise specification of these salient colours is important. (2) We test hue uniformity for CIECAM02 in all four unique hues and show significant disagreements for all hues, except for unique red which seems to be invariant under lightness changes. Our dataset is useful to improve the CIECAM02 model as it provides reliable data for benchmarking. © 2010 Wiley Periodicals, Inc. Col Res Appl, 2011     

Synthesis and Evaluation of a Series of Bis(pentylpyridinium) Compounds as Antifungal Agents

A series of bis(4‐pentylpyridinium) compounds with a variety of spacers between the pyridinium headgroups was synthesised, and the antifungal activity of these compounds was investigated. Lengthening the alkyl spacer between the pentylpyridinium headgroups from 12 to 16 methylene units resulted in increased antifungal activity against C. neoformans and C. albicans, but also resulted in increased hemolytic activity and cytotoxicity against mammalian cells. However, inclusion of an ortho‐substituted benzene ring in the centre of the alkyl spacer resulted in decreased cytotoxicity and hemolytic activity, while maintaining antifungal potency. Replacement of the alkyl and aromatic‐containing spacers by more hydrophilic ethylene glycol groups resulted in a loss of antifungal activity. Some of the compounds inhibited fungal PLB1 activity, but the low correlation of this inhibition with antifungal potency indicates PLB1 inhibition is unlikely to be the predominant mode of antifungal action of this class of compounds, with preliminary studies suggesting they may act via disruption of fungal mitochondrial function.     

MA‐NOTMP: A Triazacyclononane Trimethylphosphinate Based Bifunctional Chelator for Gallium Radiolabelling of Biomolecules

In the past few years, gallium‐68 has demonstrated significant potential as a radioisotope for positron emission tomography (PET), and the optimization of chelators for gallium coordination is a major goal in the development of radiopharmaceuticals. Methylaminotriazacyclononane trimethylphosphinate (MA‐NOTMP), a new C‐functionalized triazacyclononane derivative with phosphinate pendant arms, presents excellent coordination properties for ⁶⁸Ga (low ligand concentration, labelling at low pH even at room temperature). A “ready‐to‐be‐grafted” bifunctional chelating agent (p‐NCS‐Bz‐MA‐NOTMP) was prepared to allow ⁶⁸Ga labelling of sensitive biological vectors. Conjugation to a bombesin_(7–14) derivative was performed, and preliminary in vitro experiments demonstrated the potential of MA‐NOTMP in the development of radiopharmaceuticals. This new chelator is therefore of major interest for labelling sensitive biomolecules, and further in vivo experiments will soon be performed.