Structure−Activity Relationships of Cinnamate Ester Analogues as Potent Antiprotozoal Agents

Protozoal infections are still a global health problem, threatening the lives of millions of people around the world, mainly in impoverished tropical and sub-tropical regions. Thus, in view of the lack of efficient therapies and increasing resistances against existing drugs, this study describes the antiprotozoal potential of synthetic cinnamate ester analogues and their structure-activity relationships. In general, Leishmania donovani and Trypanosoma brucei were quite susceptible to the compounds in a structure-dependent manner. Detailed analysis revealed a key role of the substitution pattern on the aromatic ring and a marked effect of the side chain on the activity against these two parasites. The high antileishmanial potency and remarkable selectivity of the nitro-aromatic derivatives suggested them as promising candidates for further studies. On the other hand, the high in vitro potency of catechol-type compounds against T. brucei could not be extrapolated to an in vivo mouse model.     

Radiolabeling,Preparation, and Bioevaluation of 99mTc-Azathioprine as a Potential Targeting Agent for Solid Tumor Imaging

Radiochemistry - Azathioprine, an antitumor agent, was labeled with 99mTc using stannous chloride dihydrate as a reducing agent. Factors such as the amounts of the reducing agent and substrate, pH,...     

Long-Term Changes in the Course of Ice Phenomena on the Oder River along the Polish–German Border

Ice phenomena are a major component of the hydrological regime of east-central and northern European rivers. However, their occurrence disturbs inland water transportation, particularly affecting the major rivers of the Central European Plain that are part of Europe’s international waterways. The Oder is one of these rivers, and is located on the boundary between the much warmer and the much colder part of the temperate climatic zone. This makes the course of ice phenomena on the river difficult to predict. The main purpose of this work is to document and analyse the dynamic of changes occurring for over 60 years (1956–2015) in the ice phenomena of a river that demonstrates a transitional ice regime. It was found that the duration of all ice phenomena decreased (by up to 0.58 days·year^?1) and so did the duration of ice cover (by up to 0.46 days·year^?1). The rates and trends of the two parameters were, however, different in different parts of the lower stretch of the river. This fact is especially important in the context of climate changes whose characteristics include an increased incidence of extreme weather situations, both meteorological and hydrological. There was also found to be a strong correlation (R² from 0.69 to 0.81) between the duration of ice phenomena and the mean air temperature in winter (December to February) and a much weaker correlation between the duration of ice phenomena and the NAO index (R² from 0.42 to 0.48). Such a little correlation of ice phenomena with NAO is likely to result from the pollution of the Oder River (in particular in the second half of the twentieth century) and icebreaking operations on the river.

     

Improving weld formability by a novel dual-rotation bobbin tool friction stir welding

A novel dual-rotation bobbin tool friction stir welding (DBT-FSW) was developed, in which the upper shoulder (US) and lower shoulder (LS) have different rotational speeds. This process was tried to weld 3.2 mm thick aluminum-lithium alloy sheets. The metallographic analysis and torque measurement were carried out to characterize the weld formability. Experimental results show that compared to conventional bobbin tool friction stir welding, the DBT-FSW has an excellent process stability, and can produce the defect-free joints in a wider range of welding parameters. These can be attributed to the significant improvement of material flow caused by the formation of a staggered layer structure and the unbalanced force between the US and LS during the DBT-FSW process.     

The Influence of Magnetron Sputtering Conditions on the Structure of Zr–Pd Coatings

Technical Physics Letters - Using the method of DC magnetron sputtering, nonstructured amorphous metal coatings of Zr75Pd25 composition were obtained with an average deposition rate of 1.3 nm/s at...     

Tribological behaviour of a 3Y-TZP/Ta ceramic-metal biocomposite against ultrahigh molecular weight polyethylene (UHMWPE)

This study aims to evaluate the tribological behaviour of 3Y-TZP/Ta (20 vol%) ceramic-metal composites and 3Y-TZP monolithic ceramic prepared by spark plasma sintering (SPS) against ultrahigh molecular weight polyethylene (UHMWPE). According to the results of pin (UHMWPE)-on-flat wear test under dry conditions, the UHMWPE – 3Y-TZP/Ta system exhibited lower volume loss and friction coefficient than the UHMWPE – monolithic ceramic combination due to the presence of an autolubricating layer that provides sufficient lubrication for reducing the friction. Owing to the lubrication of the liquid media, under wet conditions obtained using simulated body fluid (SBF), similar behaviour is observed in both cases. Additionally, the ceramic and biocomposite materials were subjected to a low temperature degradation (LTD) process (often referred to as “ageing”) to evaluate the changes in the tribological behaviour after this treatment. In this particular case, the wear properties of the UHMWPE-biocomposite system were found to be less influenced by ageing in contrast to the case of the UHMWPE-zirconia monolithic material. In addition to their exceptional mechanical performance, 3Y-TZP/Ta composites also showed high resistance to low temperature degradation and good tribological properties, making them promising candidates for biomedical applications, especially for orthopaedic implants.     

Reoptimization framework and policy analysis for maritime inventory routing under uncertainty

We study a maritime inventory routing problem, in which shipments between production and consumption nodes are carried out by a fleet of vessels. The vessels have specific capacities and can be chartered under different agreements. The inventory levels of all consumption nodes and some production nodes should be maintained within specified bounds; for the remaining production nodes, orders should be picked up within pre-defined time windows. We propose a discrete-time mixed-integer programming model. In the face of new information and uncertainty, this optimization model has to be re-solved, as the horizon is rolled forward. We discuss how to account for different sources of uncertainty. We present a rolling-horizon reoptimization framework that allows us to study different policies that impact the quality of the implemented solution, so we can identify the optimal set of policies.     

Chromophore-Free Sealing and Repair of Soft Tissues Using Mid-Infrared Light-Activated Biosealants

Poor strength, infection, leakage, long procedure times, and inflammation limit the efficacy of common tissue sealing devices in surgeries and trauma. Light-activated sealing is attractive for tissue sealing and repair, and can be facilitated by the generation of local heat following absorption of nonionizing laser energy by chromophores. Here, the inherent ability of biomaterials is exploited to absorb nonionizing, mid-infrared (midIR) light in order to engender rapid photothermal sealing and repair of soft tissue wounds. In this approach, the biomaterial simultaneously acts as a photothermal convertor as well as a biosealant, which dispenses the need for exogeneous light-absorbing nanoparticles or dyes. Biomechanical recovery, mathematical modeling, histopathology analyses, tissue strain mapping using digital imaging correlation, and visualization of the biosealant-tissue interface using hyperspectral imaging indicate superior performance of midIR sealing in live mice compared to conventional sutures and glue. The midIR-biosealant approach demonstrates rapid sealing of soft tissues, improves cosmesis, lowers potential for scarring, obviates safety concerns because of the nonionizing light used, and allows adoption of a wide diversity of biomaterials. Taken together, the studies demonstrate a novel advance both in biomaterials for surgical sealing along with the use of nonionizing midIR light, with high potential for clinical translation.