Molecular Imaging and Preclinical Studies of Radiolabeled Long-Term RGD Peptides in U-87 MG Tumor-Bearing Mice

The Arg–Gly–Asp (RGD) peptide shows a high affinity for α_vβ₃ integrin, which is overexpressed in new tumor blood vessels and many types of tumor cells. The radiolabeled RGD peptide has been studied for cancer imaging and radionuclide therapy. We have developed a long-term tumor-targeting peptide DOTA-EB-cRGDfK, which combines a DOTA chelator, a truncated Evans blue dye (EB), a modified linker, and cRGDfK peptide. The aim of this study was to evaluate the potential of indium-111(¹¹¹In) radiolabeled DOTA-EB-cRGDfK in α_vβ₃ integrin-expressing tumors. The human glioblastoma cell line U-87 MG was used to determine the in vitro binding affinity of the radiolabeled peptide. The in vivo distribution of radiolabeled peptides in U-87 MG xenografts was investigated by biodistribution, nanoSPECT/CT, pharmacokinetic and excretion studies. The in vitro competition assay showed that ¹¹¹In-DOTA-EB-cRGDfK had a significant binding affinity to U-87 MG cancer cells (IC₅₀ = 71.7 nM). NanoSPECT/CT imaging showed ¹¹¹In-DOTA-EB-cRGDfK has higher tumor uptake than control peptides (¹¹¹In-DOTA-cRGDfK and ¹¹¹In-DOTA-EB), and there is still a clear signal until 72 h after injection. The biodistribution results showed significant tumor accumulation (27.1 ± 2.7% ID/g) and the tumor to non-tumor ratio was 22.85 at 24 h after injection. In addition, the pharmacokinetics results indicated that the ¹¹¹In-DOTA-EB-cRGDfK peptide has a long-term half-life (T_1/2λz = 77.3 h) and that the calculated absorbed dose was safe for humans. We demonstrated that radiolabeled DOTA-EB-cRGDfK may be a promising agent for glioblastoma tumor imaging and has the potential as a theranostic radiopharmaceutical.     

Effect of the addition of fluoride on the conditional solubility of alumina in LiCl-KCl eutectic melt

Owing to its well-known high complexing power toward Al³⁺ ion, fluoride ion is able to increase the solubility of alumina in alkali chloride melts. To determine the extent of this effect, the formation of aluminium(III) fluoro-complexes was studied potentiometrically in LiCl-KCl eutectic at 470°. But the sodium fluoride addition appeared to produce not only the complexation effect but also a mineralization effect on alumina. So, the thermodynamical stability of alumina formed in this melt by precipitation from aluminium chloride with carbonate ion (oxide anion donor) depends on the fluoride ion concentration. These two effects explain the solubility variation of alumina in the LiCl-KCl eutectic + NaF mixtures. A pF^? - pO^2? diagram, which represents the stability area of the various aluminium (III) species is established, and leads to some conclusions concerning the electrowinning of aluminium from molten chloride melts.The cumulative formation constants of the aluminium(lII) fluoro-complexes (AlF^3?i_i) have been obtained, whose values are the following: 2.5 ± 0.4, 4.7 ± 0.6, 5.7 ± 0.5, 7.5 ± 0.4, 8.0 ± 0.5, 9.0 ± 0.6, respectively for i = 1, 2, 3, 4, 5 and 6. It has been shown that oxyfluoride species such as AlOF^1?j_i does not exist. The solubility products of gamma and alpha-alumina have been determined and are equal to 10^?42.9 and 10^?44.0 respectively (all the constants are given in the molality scale). They differ widely from the solubility product of the alumina obtained in the absence of fluoride ion, ie 10^?27.4.     

Verlauf der Hydrierung pflanzlicher Öle - Makrokinetische Einflüsse

Course of Hydrogenation of Vegetable Oils-Macrokinetic Influence. Hydrogenation of vegetable oils is a complicated process whose course is not only influenced by the nature and properties of the catalyst and of the oil, which is to be hardened, of the temperature and pressure, but also by physical-chemical processes as adsorption, desorption and diffusion. During exploration of microkinetic phenomena, especially the way of formation of hydrogen dispersion in the reaction mixture and its influence on the curse of hydrogenation were investigated. Tne velocity and the character of hydrogenation were investigated. The velocity and the character of hydrogenation are significantly influenced by material transfer whose data are essentially changed by the shape of the stirrer, the rotation velocity and the way of the hydrogen supply. By increase of the efficiency of the flushing of Ni-catalyst particles with hydrogen the reaction velocity increases nearly in one scale of magnitude. Simultaneously the selectivity in dependence on the way of stirring of the reaction mixture and the hydrogen distribution was expressed.     

A fuzzy constraint-based approach to data reconciliation in material flow analysis

Data reconciliation consists in modifying noisy or unreliable data in order to make them consistent with a mathematical model (herein a material flow network). The conventional approach relies on least-squares minimization. Here, we use a fuzzy set-based approach, replacing Gaussian likelihood functions by fuzzy intervals, and a leximin criterion. We show that the setting of fuzzy sets provides a generalized approach to the choice of estimated values, that is more flexible and less dependent on oftentimes debatable probabilistic justifications. It potentially encompasses interval-based formulations and the least squares method, by choosing appropriate membership functions and aggregation operations. This paper also lays bare the fact that data reconciliation under the fuzzy set approach is viewed as an information fusion problem, as opposed to the statistical tradition which solves an estimation problem.     

Electrochemical behaviour of indium ions in molten equimolar CaCl2–NaCl mixture at 550 ∘C

The stability of indium chloride and oxide as well as the electrochemical behaviour of indium ions have been studied in the equimolar CaCl2–NaCl melt at 550 C by X-ray diffraction (XRD) and different electrochemical techniques, using molybdenum and tungsten wires as working electrodes. Voltammetric and chronopotentiometric studies showed signals attributed to the presence of three oxidation states of indium, i.e. 0, i and iii. The standard potential of the redox couples, as well as the solubility products of indium oxides have been determined, showing that In(iii) ions are completely reduced to monovalent indium by the indium metal according to the reaction: In () + 2 In 3 In () and that In₂O is a strong oxide donor according to the reaction: In₂O(s) 2 In() + O^2- These results have allowed the construction of E-pO2– equilibrium diagrams summarising the properties of In–O compounds. The electrodeposition of indium was uncomplicated at Mo and W electrodes. Very good adherence of liquid indium to the electrode materials was observed, with the formation of Na–In alloys at highly reducing potentials, and there was no evidence of indium dissolution into the melt. Moreover, the voltammograms corresponding to the electrochemical In(iii)/In(i) exchange were well defined. The two electrochemical steps were found to be quasi-reversible, and the values of the kinetic parameters, ko and , for both reactions, as well as the diffusion coefficients, DIn(III) and DIn(I) were calculated.     

新型海藻糖酶抑制剂的合成及生物活性

本文合成了未见文献报道的七个化合物,其结构均得到核磁共振、红外光谱、质谱和元素分析的确证,并测试了其海藻糖酶抑制活性,生测结果表明此类化合物显示了一定的抑制作用。     

Energieinformatik

Due to the increasing importance of producing and consuming energy more sustainably, Energy Informatics (EI) has evolved into a thriving research area within the CS/IS community. The article attempts to characterize this young and highly dynamic field of research by describing current EI research topics and methods and provides an outlook of how the field might evolve in the future. It is shown that two general research questions have received the most attention so far and are likely to dominate the EI research agenda in the coming years: How to leverage information and communication technology (ICT) to (1) improve energy efficiency, and (2) to integrate decentralized renewable energy sources into the power grid. Selected EI streams are reviewed, highlighting how the respective research questions are broken down into specific research projects and how EI researchers have made contributions based on their individual academic background.     

Production of propylene glycol fatty acid monoesters by lipase-catalyzed reactions in organic solvents

Fatty acid monoesters of propylene glycol (1,2-propanediol) are good water-in-oil emulsifiers. These esters were synthesized enzymatically to overcome the problems associated with chemical processes. APseudomonas lipase was added to reaction mixtures containing propylene glycol and various acyl donors (fatty acids, fatty acid ethyl esters, fatty acid anhydrides and triglycerides) in organic solvents, and the mixtures were shaken at 30°C. The products were analyzed by gas chromatography. The yield of monoesters was affected by the acyl donors, organic solvents, temperature, water content, pH memory and reaction time. The anhydrous (lyophilized) enzyme and fatty acid anhydrides were best for monoester production. The optimum pH ranges were 4–5 and 8–10. The yields of propylene glycol monolaurate, monomyristate, monopalmitate, monostearate and monooleate with 50 mM fatty acid anhydrides as acyl donors were 97.2, 79.6, 83.7, 89.7 and 93.4 mM, respectively; those with 50 mM fatty acids as acyl donors were 37.3, 28.7, 28.7, 35.3 and 36.2 mM, respectively. The yields of propylene glycol monopalmitate, monostearate and monooleate with 50 mM triglycerides as acyl donors were 87.4, 65.1 and 83.2 mM, respectively.     

Engineering a pharmacologically superior form of leptin for the treatment of obesity

Leptin plays a central role in the homeostasis of body weight through its regulatory effects on appetite and energy expenditure, yet in trials as a therapeutic agent for the treatment of obesity in humans it has been disappointing. The poor clinical efficacy of leptin results from its short circulating half-life, low potency and poor solubility, necessitating large and frequent doses to obtain even modest clinical benefit. Engineered Fc-leptin immunofusins, consisting of the Fc fragment of an immunoglobulin gamma chain followed by leptin, exhibit improved pharmacological properties with very consistent and potent biological activities. Furthermore, in extending the circulating half-life of the protein in vivo from a few minutes for leptin to many hours for Fc-leptin, these proteins have the potential to reduce drastically the dosage and frequency of administration required to obtain clinical benefit. The results of this study show that the engineered leptin immunofusins described here have significantly enhanced pharmacological properties in comparison with the recombinant leptin that was used in clinical trials. As such, they could represent an important step towards a therapeutically superior form of leptin if the disappointing performance of leptin in early clinical trials was due to its poor pharmacological properties rather than any conceptual weakness in the strategy of using leptin for the treatment of obesity and its related disorders.