Platinum(II) Complexes Bearing Triphenylphosphine and Chelating Oximes: Antiproliferative Effect and Biological Profile in Resistant Cells

Platinum(II) complexes of the type [Pt(Cl)(PPh₃){(κ²-N,O)-(1{C(R)=N(OH)-2(O)C₆H₄})}] with R=Me, H, ( 1 and 2 ) were synthesized and characterized. Single-crystal X-ray diffraction confirmed the proposed (SP4-3) configuration for 1 . Study of the antiproliferative activity, performed on a panel of human tumor cell lines and on mesothelial cells, highlighted complex 2 as the more effective. In particular, it showed a remarkable cytotoxicity in ovarian carcinoma cells (A2780) and interestingly, a significant antiproliferative effect on cisplatin resistant cells (A2780cis). Investigation into the intracellular mechanism of action demonstrated that 2 had a lower ability to platinate DNA than did cisplatin, which was taken as reference, and a notably higher uptake in resistant cells. A significant accumulation in mitochondria, along with the ability to induce concentration-dependent mitochondrial membrane depolarization and intracellular reactive oxygen species production, allowed us to propose a mitochondrion-mediated pathway as responsible for the interesting cytotoxic profile of complex 2 .     

α-Triazolylboronic Acids: A Promising Scaffold for Effective Inhibitors of KPCs

Boronic acids are known reversible covalent inhibitors of serine β-lactamases. The selectivity and high potency of specific boronates bearing an amide side chain that mimics the β-lactam's amide side chain have been advanced in several studies. Herein, we describe a new class of boronic acids in which the amide group is replaced by a bioisostere triazole. The boronic acids were obtained in a two-step synthesis that relies on the solid and versatile copper-catalyzed azide–alkyne cycloaddition (CuAAC) followed by boronate deprotection. All of the compounds show very good inhibition of the Klebsiella pneumoniae carbapenemase KPC-2, with K_i values ranging from 1 nM to 1 μM, and most of them are able to restore cefepime activity against K. pneumoniae harboring bla_KPC-2. In particular, compound 1 e , bearing a sulfonamide substituted by a thiophene ring, proved to be an excellent KPC-2 inhibitor (K_i=30 nM); it restored cefepime susceptibility in KPC-Kpn cells (MIC=0.5 μg/mL) with values similar to that of vaborbactam (K_i=20 nM, MIC in KPC-Kpn 0.5 μg/mL). Our findings suggest that α-triazolylboronates might represent an effective scaffold for the treatment of KPC-mediated infections.     

Mixture design applied for the development of films based on starch,polyvinyl alcohol,and glycerol

Starch and polyvinyl alcohol (PVA) are biodegradable materials with potentiality to replace the conventional polymers in some applications. The aim of this work was to produce biodegradable films of PVA, cassava starch, and glycerol by thermoplastic extrusion using a mixture design to evaluate the effects of each component in the blend properties. Six formulations were prepared using a twin‐screw extruder coupled with a calender. All the materials were visually homogeneous and presented good processability. Mechanical properties were dependent on both the relative humidity conditioning and the formulation; higher relative humidities detracted the mechanical properties, which was associated to plasticizer effect of the water. Furthermore, the mechanical properties were better when higher concentrations of PVA were used, resulting in films with lower opacity, lower water vapor permeability, and higher thermal stability, according to TGA. Biodegradable materials based on starch, PVA, and glycerol have adequate mechanical and processing properties for commercial production. © 2015 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2015 , 132, 42697.     

Promising curaua fiber‐reinforced polyester composite for high‐impact ballistic multilayered armor

A typical multilayered armor system (MAS) is composed of a harder front ceramic tile, which is able to erode heavy ammunition, such as the 7.62 mm bullet, followed by a second layer to further reduce the impact energy. Aramid fabric is a common choice for the second layer. In the present work, polyester matrix composites reinforced with 10 to 30 vol% of curaua fibers, despite having much lower strength and stiffness than aramid fabric, displayed similar trauma indentation in a standard clay witness simulating the human body. Impedance matching and scanning electron microscopy analyses suggest effective energy absorption through ceramic fragment capture by curaua composites. Additionally, because of the high cost of aramid fabric, a full MAS with curaua fiber composite is much cheaper than a MAS composed of aramid fabric. Taking into consideration, both the economical and environmental advantages of natural fibers, it is concluded that curaua fiber‐reinforced polyester composite could replace aramid fabric as the second layer in MASs for personal ballistic protection. POLYM. ENG. SCI., 57:947–954, 2017. © 2016 Society of Plastics Engineers     

Evaluation of tritium diffusion through the Neutral Beam Injector calorimeter panel

The Neutral Beam Test Facility (NBTF) to be realized in Padoa will test the Neutral Beam Injection (NBI), one of the Heating and Current Drive Systems foreseen for ITER. The NBI is based on the acceleration of hydrogen or deuterium negative ions up to 1 MeV. This work has been aimed at assessing the tritium release from the NBTF in order to provide data for the safety analysis. In particular, the diffusion of the tritium through the neutral beam target material (the CuCrZr alloy calorimeter panels) has been assessed by using literature data of the diffusion coefficient. The tritium generated inside the calorimeter panels moves into both the vacuum and water side: the tritium diffusion flux has been evaluated during the beam-on (200 °C) and the beam-off (20 °C) phases of the NBTF experiments consisting of an interim campaign and a final test. The penetration depth of the tritium through the 2 mm thick CuCrZr alloy material has been also evaluated by using a Monte-Carlo code. As main result, the assessed diffusion flux of tritium during both the beam-on and the beam-off phases are modest. In fact, at the end of the interim campaign (100 days), about the 96% of the all generated tritium (626.5 MBq) exits the calorimeter while the residual tritium inventory (25 MBq) leaves the copper alloy with a diffusion time of about 1 month. At the end of the final test (14 days) about the 99% of the total generated tritium (1.023 × 10⁴ MBq) leaves the copper alloy and the remaining tritium inventory (152.2 MBq) is released by about 32 days. In both the interim campaign and the final test, more than the 99% of the total tritium is transferred into the vacuum side of the calorimeter panel while negligible tritium amounts enter the cooling water system thus showing a very low impact on the environment.     

Effect of Vacuum and Modified Atmosphere Packaging on the Shelf-life of Liquid-smoked Swordfish (Xiphias gladius) Slices

ABSTRACT: Swordfish fillets, dry-salted and treated with liquid smoke, were sliced and packed in vacuum conditions and under modified atmosphere (MA) (5% O₂,45% CO₂, 50% N₂) and stored at chilled temperature (4°C) to determine the effect of different packaging on shelf-life. Sensory attributes, total volatile basic nitrogen (TVB-N), pH, lipid oxidation by thiobarbituric acid test, and microbiological counts were monitored during 45 d of storage. The TVB-N increased to levels recommended by European regulation at the time of sensory rejection, resulting as the most reliable parameter of quality decay. Lipid oxidation was low and microbial counts could not be correlated with quality decay. Sensory rejection (at least 50% of the assessors scoring =5 in a scale from 1 to 9) was sooner for MA-packed samples (12d) than for vacuum-packed ones (42d).     

Systematic Review on Tumor Microenvironment in Glial Neoplasm: From Understanding Pathogenesis to Future Therapeutic Perspectives

Despite the multidisciplinary management in the treatment of glioblastomas, the average survival of GBM patients is still 15 months. In recent years, molecular biomarkers have gained more and more importance both in the diagnosis and therapy of glial tumors. At the same time, it has become clear that non neoplastic cells, which constitute about 30% of glioma mass, dramatically influence tumor growth, spread, and recurrence. This is the main reason why, in recent years, scientific research has been focused on understanding the function and the composition of tumor microenvironment and its role in gliomagenesis and recurrence. The aim of this review is to summarize the most recent discovery about resident microglia, tumor-associated macrophages, lymphocytes, and the role of extracellular vesicles and their bijective interaction with glioma cells. Moreover, we reported the most recent updates about new therapeutic strategies targeting immune system receptors and soluble factors. Understanding how glioma cells interact with non-neoplastic cells in tumor microenvironment is an essential step to comprehend mechanisms at the base of disease progression and to find new therapeutic strategies for GBM patients. However, no significant results have yet been obtained in studies targeting single molecules/pathways; considering the complex microenvironment, it is likely that only by using multiple therapeutic agents acting on multiple molecular targets can significant results be achieved.     

Effect of cavosurface angle beveling on the exposure angle of enamel prisms in different cavity sizes

The quality of the micromechanical retention between the enamel prisms exposed through acid etching and adhesive system can be influenced by the relationship between the angle of the exposed enamel prisms and the external surface/restorative material. Therefore, the aim of the present study was to determine the influence of the enamel cavosurface beveling in different cavity sizes on the angle relation between enamel prisms and the restorative material. For this research, 30 human permanent molars were used and divided into three groups according the isthmus aperture of class I cavities (1/4, 1/3, and 1/2 of the intercuspal distance). Cavosurface angle beveling was performed in each tooth buccal or palatal/lingual side, and a resin composite restoration was placed. Each restored tooth was sectioned in buccal/palatal direction followed by analysis in scanning electron microscope. Means of the angles observed between enamel prisms and the restorative material were registered and statistically analyzed by Kruskal‐Wallis test. Results showed higher mean angle values for beveled groups when comparing with the values observed in the unbeveled margins (p < .05) regardless of the isthmus aperture, being 1/4 (beveled = 48.36°; unbeveled = 20.71°), 1/3 (beveled = 39.75°; unbeveled = 29.15°), and 1/2 (beveled = 37.02°; unbeveled = 26.34°). It was also observed that in some unbeveled cavities, there were the presence of laterally exposed enamel prisms (0°), mainly in more conservative cavities. It was concluded that the presence of higher angles values occurred in the samples with beveled margins, without presence of laterally exposed enamel prisms.     

Performance Evaluation of Packet Mobile Communications through Level Crossing Analysis

In this paper the performance of a packet mobile radio network is studied inthe presence of shadow fading outage intervals.Under quite general assumptions for the medium access protocol,the probability mass function of the sequence of packets that may be lostdue to an outage interval is derived. It is seen that long sequences of lostpackets are likely to occur for typical values of the mobile speed andshadowing correlation parameters.For delay constrained sources, e.g., voice, the analysis is mainly focused atderiving the probability function of the sequence of dropped packetsand the probability of dropping. For data sources, the delay statistic isalso derived. In the latter case, the effect of finite buffer length isaddressed. Simulation is used to verify the accuracy of approximations introduced in the analysis.