Interaction of Cucurbit[7]uril with Oxime K027, Atropine,and Paraoxon: Risky or Advantageous Delivery System?

Antidotes against organophosphates often possess physicochemical properties that mitigate their passage across the blood–brain barrier. Cucurbit[7]urils may be successfully used as a drug delivery system for bisquaternary oximes and improve central nervous system targeting. The main aim of these studies was to elucidate the relationship between cucurbit[7]uril, oxime K027, atropine, and paraoxon to define potential risks or advantages of this delivery system in a complex in vivo system. For this reason, in silico (molecular docking combined with umbrella sampling simulation) and in vivo (UHPLC—pharmacokinetics, toxicokinetics; acetylcholinesterase reactivation and functional observatory battery) methods were used. Based on our results, cucurbit[7]urils affect multiple factors in organophosphates poisoning and its therapy by (i) scavenging paraoxon and preventing free fraction of this toxin from entering the brain, (ii) enhancing the availability of atropine in the central nervous system and by (iii) increasing oxime passage into the brain. In conclusion, using cucurbit[7]urils with oximes might positively impact the overall treatment effectiveness and the benefits can outweigh the potential risks.     

A Novel Insight into the Cardiotoxicity of Antineoplastic Drug Doxorubicin

Doxorubicin is a commonly used antineoplastic agent in the treatment of many types of cancer. Little is known about the interactions of doxorubicin with cardiac biomolecules. Serious cardiotoxicity including dilated cardiomyopathy often resulting in a fatal congestive heart failure may occur as a consequence of chemotherapy with doxorubicin. The purpose of this study was to determine the effect of exposure to doxorubicin on the changes in major amino acids in tissue of cardiac muscle (proline, taurine, glutamic acid, arginine, aspartic acid, leucine, glycine, valine, alanine, isoleucine, threonine, lysine and serine). An in vitro interaction study was performed as a comparison of amino acid profiles in heart tissue before and after application of doxorubicin. We found that doxorubicin directly influences myocardial amino acid representation even at low concentrations. In addition, we performed an interaction study that resulted in the determination of breaking points for each of analyzed amino acids. Lysine, arginine, β-alanine, valine and serine were determined as the most sensitive amino acids. Additionally we compared amino acid profiles of myocardium before and after exposure to doxorubicin. The amount of amino acids after interaction with doxorubicin was significantly reduced (p = 0.05). This fact points at an ability of doxorubicin to induce changes in quantitative composition of amino acids in myocardium. Moreover, this confirms that the interactions between doxorubicin and amino acids may act as another factor most likely responsible for adverse effects of doxorubicin on myocardium.     

Short-term power sources for tokamaks and other physical experiments

The Compass-D tokamak is being planned to move from UKAEA Culham (England) be and reinstalled in IPP Prague (Czech Republic). An overview of Compass-D energetics is described in short. The new power sources have to be designed. Alternative solutions of power sources have been investigated. Ignitrons and mechanical breakers can be replaced by modern high-power semiconductors. With respect to the need of accumulated energy, new technologies of energy storage - supercapacitors and high-speed flywheels, not applied up to now in similar fusion projects, are characterized in comparison with traditional ones - capacitors and big motor-flywheel generators. It is shown that these technologies enhance possibilities in arrangement of power supplies for tokamaks as well as for other high-power demanding experiments with pulse length from fraction to tens of seconds.     

Pool boiling heat transfer of carbon dioxide on a horizontal tube

Carbon dioxide is again becoming an important refrigerant. While the thermophysical properties are well known there is a lack of data on its heat transfer characteristics.

In this study, heat transfer coefficients for nucleate boiling of carbon dioxide are determined using a standard apparatus for the investigation of pool boiling based on a set-up from Karlsruhe [D. Gorenflo, J. Goetz, K. Bier. Vorschlag für eine Standard-Apparatur zur Messung des Wärmeübergangs beim Blasensieden. Wärme-und Stoffübertragung 16 (1982), 69–78; J. Goetz, Entwicklung und Erprobung einer Normapparatur zur Messung des Wärmeübergangs beim Blasensieden. Dissertation Universität Karlsruhe (1980).] and built at our institute. Electrically heated horizontal cylinders with an outer diameter of 16 mm and a length of 100 mm are used as heating elements. Measurements with constant heat flux are performed for different wall materials and surface roughnesses. The heat transfer is investigated within the pressure range of 0.53≤ p ≤1.43 MPa (0.072≤ p/p_c ≤0.190) and a temperature range of −56≤ t ≤−30 °C, respectively. Heat fluxes of up to 80,000 W m⁻² are applied.

The influences of wall material and roughness on the heat transfer coefficient are evaluated separately. The obtained coefficients are compared to generally accepted correlations and to experimental results of other authors, who used similar configurations with copper tubes and carbon dioxide. These are the only previous experimental data, which could be found. Results for copper, stainless steel and aluminium as wall materials are presented.     

Microporous membranes prepared from blends of polysulfone and sulfonated poly(2,6‐dimethyl‐1,4‐phenylene oxide)

Membranes were prepared from solutions containing Udel‐type polysulfone (PSf) and sulfonated poly(2,6‐dimethyl‐1,4‐phenylene oxide) (SPPO). Polymer solutions in 1‐methyl‐2‐pyrrolidone were cast on a nonwoven textile and precipitated in a water bath. The permeabilities and selectivities of the prepared membranes depended on the concentrations of both polymers in the casting solution. The higher the concentration of PSf, the lower were the permeabilities to water and average pore sizes of the membranes. On the other hand, a very small amount of SPPO in the casting solution (about 1–4 wt % relative to the casting solution weight) brought about a considerable increase in water permeabilities and had a small influence on the average pore sizes. The effects were most pronounced if SPPO with a degree of sulfonation of 20–40% was used. The considerable increase in water permeabilities was explained by separation of the PSf and SPPO phases during precipitation in water and by the concentration of hydrophilic SPPO on the surface of the membrane and its pores. The determinations of the oriented concentration potentials proved the presence of a negative surface charge in the membranes. © 2001 John Wiley & Sons, Inc. J Appl Polym Sci 81: 134–142, 2001     

Transient luminescence in organic light-emitting diodes explained by trap-assisted recombination of stored charges

We show that after voltage turn-off the recombination of the charges which are stored in the on-state may follow a trap-assisted mechanism instead of the Langevin formula in organic light-emitting diodes. A microscopic model based on this form of recombination is introduced, which not only fits the transient electroluminescence very well in the whole range of the off-state but also provides parameters quantitatively characterizing the stored charges in the on-state. In the last part, we briefly compare the work by Weichsel et al. [1] and our model, trying to constitute a comprehensive picture of the stored charges in OLEDs. As an OLED model system we have chosen a host/guest system co-doped with red and green phosphorescent emitters.     

Dual-phase polyphenylene oxide membranes with copolyimide branched modifiers

Poly(2,6-dimethyl-1,4-phenylene oxide) (PPO) membranes are attractive due to high permeability for gases; however, the selectivity of these membranes is insufficient. In this work, the gas selectivity was improved without significant loss of the permeability. For this purpose, PPO was modified via incorporation of the branched copolyimide filler–grafted copolyimide (PI-g-PMMA) with polymethyl methacrylate (PMMA) side chains. Two series of mixed self-supporting PPO/PI-g-PMMA films (with variation of the filler content) were prepared and studied as gas separation membranes. The length of the polymide (PI) chain and the density of PMMA grafting were the same in both series, however, in one series the grafted chains contained 50 MMA units, and in the other 150 units. The intermolecular interactions between the PPO matrix and the PI-g-PMMA fillers were investigated using viscometry, infrared (IR) spectroscopy, and scanning electron microscopy. The compatibility of the polymer components is limited; however, for both series, the contents of the respective filler are found, which ensures phase segregation only in a microscale. Therefore, the mechanical properties of the films allow their use as gas separation membranes. It is shown that the degree of the segregation as well as the mechanical and gas transport properties of the membranes depend on the length of the PMMA chains, and the membranes with filler-containing shorter branches (50 MMA units) show better selectivity.