In Vitro Activity of Monofunctional Pt-II Complex Based on 8-Aminoquinoline against Human Glioblastoma

A new cationic Pt(II) complex bearing 8-aminoquinoline as chelating ligand (called Pt-8AQ) was evaluated against two human carcinomas, one mesothelioma, and three glioblastoma cell lines. The in vitro comparison to the clinically approved CisPt showed a minor activity of Pt-8AQ against carcinoma and mesothelioma, whereas a significant activity of Pt-8AQ was observed on the proliferation of the three glioblastoma cell lines (U87-MG IC50 = 3.68 ± 0.69 µM; U373-MG IC50 = 11.53 ± 0.16 µM; U138-MG IC50 = 8.05 ± 0.23 µM) that was higher than that observed with the clinically approved CisPt (U87-MG IC50 = 7.27 + 1.80 µM; U373-MG IC50 = 22.69 ± 0.05 µM; U138-MG IC50 = 32.1 ± 4.44 µM). Cell cycle analysis proved that Pt-8AQ significantly affected the cell cycle pattern by increasing the apoptotic cells represented by the sub G0/G1 region related with a downregulation of p53 and Bcl-2. Moreover, an NMR investigation of Pt-8AQ interaction with 9-EtG, GSH, and Mets7 excluded DNA as the main target, suggesting a novel mechanism of action. Our study demonstrated the high stability of Pt-8AQ after incubation at 37 °C and a significant antineoplastic activity on glioblastomas. These features also make Pt-8AQ a good candidate for developing a new selective advanced cell chemotherapy approach in combination with MSCs.

Tracking reservoir dynamics across a complete caldera cycle at Rabaul, Papua New Guinea

<p>Caldera-forming eruptions are some of the most devastating events on Earth; however, the volcanoes that produce these eruptions frequently have much more minor activity. Knowing if a restless caldera is currently primed for a large eruption, therefore, has important implications for hazard assessment and risk management. Many calderas, including Rabaul in Papua New Guinea, show cycles of activity with multiple caldera-forming eruptions interspersed with more minor activity. We present data that spans an entire cycle, from one caldera-forming eruption to the next and estimate the storage conditions for each eruption. The last complete caldera cycle of Rabaul started at ~10.5 ka, with the eruption of the dacitic Vunabugbug Ignimbrite. Following the Vunabugbug, little volcanic activity was preserved until ~4.4 ka, suggesting either a period quiescence or destruction and burial during the subsequent caldera-forming eruptions of the region. From 4.4 ka, there is an increase in the volume and SiO<sub>2</sub> contents of volcanic deposits that are preserved, which culminated in the eruption of the dacitic Memorial Ignimbrite at ~4.1 ka. The Memorial Ignimbrite was smaller than the Vunabugbug Ignimbrite and Rabaul Pyroclastics and may not have formed a caldera; however, it does appear to have altered the plumbing system and allowed deeper, hotter basalts to reach the surface. Following the eruption of these basalts, the system gradually evolves towards more silicic magmas, until the eruption of the dacitic Rabaul Pyroclastics at ~1.4 ka. After the Rabaul Pyroclastics hotter, more mafic magmas can again reach the surface, both as more mafic lava flows and as hybrid andesites that contain crystal cargos transported from deeper in the system.</p><p>Two-pyroxene, clinopyroxene–liquid and plagioclase–liquid thermobarometers suggest that the dacites, including those erupted during the caldera-forming eruptions, were stored at pressures of ~1 kbar (~4 km depth) and at temperatures of ~930 °C. There is a tight relationship between the temperature and the SiO<sub>2</sub> content of the magmas, with the basalts erupted after the large ignimbrites recording temperatures of up to 1100 °C. Some of the more mafic magmas also record deeper storage, at pressures of 3–4 kbar (11–15 km). Plagioclase–liquid pairs suggest melt H<sub>2</sub>O contents of ~2.8 wt.% for the dacites, although some of the more mafic magmas have slightly higher melt H<sub>2</sub>O contents (3.2–4.0 wt.%)—this may be because the basalts were saturated and stored at greater pressures. Magnetite–liquid pairs record relatively constant oxygen fugacities of ~1.2 log units above the FMQ buffer.</p><p>At Rabaul it would take on the order of a few millennia to differentiate or accumulate enough dacitic magma to produce a large explosive eruption. The eruption of highly evolved, crystal-poor, cold, hydrous magmas geochemically similar to those erupted prior to the Memorial Ignimbrite and Rabaul Pyroclastics may provide a warning of an impending large explosive eruption.</p>

Catalytic Activation of a Carbon–Chloride Bond by Dicationic Tellurium-Based Chalcogen Bond Donors

Noncovalent interactions such as halogen bonding (XB) and chalcogen bonding (ChB) have gained increased interest over the last decade. Whereas XB-based organocatalysis has been studied in some detail by now, intermolecular ChB catalysis only emerged quite recently. Herein, bidentate cationic tellurium-based chalcogen bond donors are employed in the catalytic chloride abstraction of 1-chloroisochroman. While selenium-based ChB catalysts showed only minor activity in this given benchmark reaction, tellurium-based variants exhibited strong activity, with rate accelerations of up to 40 relative to non-chalogenated reference compounds. In general, the activity of the catalysts improved with weaker coordinating counterions, but tetrafluoroborate took part in a fluoride transfer side reaction. Catalyst stability was confirmed via a fluoro-tagged variant.

Diurnal feeding strategies of the Ferruginous Duck (Aythya nyroca) in Lake Tonga (Northeastern Algeria)

Although the Ferruginous Duck (Aythya nyroca) has thoroughly been studied, the foraging behaviour of this species is still not completely known. In the present paper we studied the diurnal feeding behaviour of ducks. We monitored the annual cycle of birds through two fieldtrips per month. The instantaneous behaviour of birds was recorded in regular 30-minute intervals from 7 a.m. to 4:30 p.m., amounting a total of 456 observation hours. Food searching activity corresponds to a quarter of the total diurnal time budget of the Ferruginous Duck. Foraging behaviour was classified into five categories dominated by the “diving”, which is almost 45.61% of the total search time. Foraging activities at the water surface considered to be secondary activities, including feeding by “bill”, “neck and head”, and “beak and head” in a rate of 19.86%, 14.53%, and 13.98%, respectively. The “toggle” remains a minor activity and represents only 5.99% of foraging time. The feeding behaviour of this species correlated to several environmental parameters (rainfall, temperature and wind velocity), and linked to the group size of ducks visiting the lake. Regarding the food intensity, our results show the highest values for “bill and head” behaviour. “Diving” has the longest feeding interval (16.16±14.1 minutes), while foraging by “bill” has the shortest (0.69 ± 0.48 minutes).

One-pot multicomponent nitro-Mannich reaction using a heterogeneous catalyst under solvent-free conditions

An environmentally-friendly, one-pot multicomponent reaction of various aldehydes, amines and nitroalkanes for the synthesis of β-nitroamines is here described. Amberlyst A-21 supported CuI was found to be a highly efficient novel heterogeneous catalyst for the three-component nitro-Mannich reaction between aldehydes, amines and nitroalkanes. The developed protocol is performed in a solvent-free medium to produce a variety of β-nitroamines in good to excellent yields within short reaction times. The catalyst can be easily prepared and recovered. It has been tested up to eight times with only a minor activity loss.

Foraging behavior, environmental parameters and nests development of Melipona colimana Ayala (Hymenoptera: Meliponini) in temperate climate of Jalisco, México

Melipona colimana Ayala is an endemic species inhabiting temperate forests of pine and oak of south of Jalisco in Mexico. During a year, it was recorded every 15 days foraging activity, environmental parameters and the development of colonies of M. colimana in its wild habitat. For five minutes every hour from 7:00 to 21:00, the bees that entered and left the hive and bringing pollen and resin were registered. Every hour the relative humidity, temperature, wind speed and light intensity was recorded and related to foraging activity. Additionally, the weight of the colonies recently transferred to wooden boxes, the number of brood combs, honey pots and pollen were registered. The time of beginning and ending of the foraging activity differs from the reports of stingless bees of tropical weather and the same happens with the pollen collection. The environmental parameters that affect other tropical stingless bees in the foraging activity also affect M. colimana in temperate climate. It was determined that the major activity season and the presence of more pollen pots in the colony is from November through February, for what it could be the best time of the year for the division and obtainance of new colonies, while the critical period of minor activity and pollen flow was during rainy season. These data may be useful for the future sustainable use of this species in temperate climate.

The Glycoside Hydrolase Family 8 Reducing-End Xylose-Releasing Exo-oligoxylanase Rex8A from Paenibacillus barcinonensis BP-23 Is Active on Branched Xylooligosaccharides

ABSTRACTA GH8 family enzyme involved in xylan depolymerization has been characterized. The enzyme, Rex8A, is a reducing-end xylose-releasing exo-oligoxylanase (Rex) that efficiently hydrolyzes xylooligosaccharides and shows minor activity on polymeric xylan. Rex8A hydrolyzes xylooligomers of 3 to 6 xylose units to xylose and xylobiose in long-term incubations. Kinetic constants of Rex8A were determined on xylotriose, showing aKmof 1.64 ± 0.03 mM and akcatvalue of 118.8 s−1. Besides linear xylooligosaccharides, the enzyme hydrolyzed decorated xylooligomers. The catalytic activity on branched xylooligosaccharides, i.e., the release of xylose from the reducing end, is a newly described trait of xylose-releasing exo-oligoxylanases, as the exo-activity on these substrates has not been reported for the few of these enzymes characterized to date. Modeling of the three-dimensional (3D) structure of Rex8A shows an (α/α)6barrel fold where the loops connecting the α-helices contour the active site. These loops, which show high sequence diversity among GH8 enzymes, shape a catalytic cleft with a −2 subsite that can accommodate methyl-glucuronic acid decorations. The hydrolytic ability of Rex8A on branched oligomers can be crucial for the complete depolymerization of highly substituted xylans, which is indispensable to accomplish biomass deconstruction and to generate efficient catalysts.IMPORTANCEA GH8 family enzyme involved in xylan depolymerization has been characterized. The Rex8A enzyme fromPaenibacillus barcinonensisis involved in depolymerization of glucuronoxylan, a major component of the lignocellulosic substrates. The study shows that Rex8A is a reducing-end xylose-releasing exo-oligoxylanase that efficiently hydrolyzes xylose from neutral and acidic xylooligosaccharides generated by the action of other xylanases also secreted by the strain. The activity of a Rex enzyme on branched xylooligosaccharides has not been described to date. This report provides original and useful information on the properties of a new example of the rarely studied Rex enzymes. Depolymerization of highly substituted xylans is crucial for biomass valorization as a platform for generation of biofuels, chemicals, and solvents.

Casino Markets: A Study of Tourist and Local Patrons

This paper compares the socio-demographic characteristics and motivations of tourists from Alberta who visit casinos while travelling, with Albertans who patronise local casinos; and tourists from Alberta for whom a casino visit was a major trip activity versus those for whom it was a minor activity. Data were collected from 900 residents of Alberta's two major metropolitan areas who had visited a casino in the previous 12 months. Findings demonstrate that tourist patrons are more likely to be female, to have a university education and to have management or professional occupations. They are also more likely to be motivated by social or communal goals and less likely to be motivated by risk seeking than local patrons. Those tourists for whom casino gaming is a major trip activity are more strongly motivated by risk-taking and the wish to escape their regular lives than are tourists for whom gaming is a minor trip activity. Differences also exist in terms of several key travel profile dimensions.