Selective recognition of a saccharide-type tumor marker with natural and synthetic ligands: a new trend in cancer diagnosis

It is well known that saccharides and their glycoconjugates can have an important influence on various serious pathologic stages such as cancer. They can regulate tumor proliferation, invasion, hematogenous metastasis, and angiogenesis. These facts clearly show the importance of cancer saccharide recognition. In medicine, sensor analysis is one of the best methods for recognition and determination of biologically important analytes. The development and study of sensors for saccharide tumor markers can open a new way for their detection. Therefore, this review is focused on recognition of saccharide-based cancer markers by natural or synthetic selective ligands working as bio- and chemosensors. The design and application of these ligands for cancer diagnosis is a useful direction of research. Moreover, it also opens the possibility of using these agents for the targeted drug transport required for advanced anticancer therapy.     

Acetylcholinesterase-Inhibiting Activity of Salicylanilide <em>N</em>-Alkylcarbamates and Their Molecular Docking

A series of twenty-five novel salicylanilide N-alkylcarbamates were investigated as potential acetylcholinesterase inhibitors. The compounds were tested for their ability to inhibit acetylcholinesterase (AChE) from electric eel (Electrophorus electricus L.). Experimental lipophilicity was determined, and the structure-activity relationships are discussed. The mode of binding in the active site of AChE was investigated by molecular docking. All the discussed compounds expressed significantly higher AChE inhibitory activity than rivastigmine and slightly lower than galanthamine. Disubstitution by chlorine in C'_(3,4) of the aniline ring and the optimal length of hexyl-undecyl alkyl chains in the carbamate moiety provided the most active AChE inhibitors. Monochlorination in C'₍₄₎ exhibited slightly more effective AChE inhibitors than in C'₍₃₎. Generally it can be stated that compounds with higher lipophilicity showed higher inhibition, and the activity of the compounds is strongly dependent on the length of the N-alkyl chain.     

Transformation of 4‐oxo‐4H‐[1]‐benzopyran‐3‐carboxaldehydes into pyrazolo[3,4‐B]pyridines

Reaction of 6‐methyl‐4‐oxo‐4H‐[1]‐benzopyran‐3‐carboxaldehyde 1 with 5‐amino‐3‐methyl‐1‐phenylpyrazole 2 in alcoholic reaction media in the presence of 4‐toluenesulfonic acid as catalyst afforded 5‐(2‐hydroxy‐5‐methylbenzoyl)‐3‐methyl‐1‐phenyl‐1H‐pyrazolo[3,4‐b]pyridine 3 and 2‐methoxy‐6‐methyl‐3‐(3‐methyl‐1‐phenylpyrazol‐5‐ylaminomethylene)chroman‐4‐one 7 . We explain the mechanism of formation of both products on the basis of kinetic study of individual reaction steps.     

Study of Interaction between Metallothionein and CdTe Quantum Dots

Quantum dots (QDs) belong to a new class of fluorescent agent for biochemical, medicinal or other purposes. However, QDs based on cadmium or other metals can be risky for an organism. As one of the mechanism how to detoxify cadmium-based QDs expression of metallothioneins (MT) can be considered. Due to high affinity of metallothionein to cadmium(II) ions, we attempted to develop an approach for studying of possible interaction with QDs. We prepared QDs with CdTe core and studied the interaction with MT, which we isolated from livers of Cd-administered rabbits. To study the interaction, we used the mixture of both components MT (3.6 μM): CdTe QDs (0, 0.34, 0.68, 1.02, 1.36, 1.7, 2.04 and 2.47 μM). The mixtures were studied by spectrophotometry within the range from 200 to 750 nm with detected maxima at 260 and 505 nm. Same mixtures were also analysed by differential pulse voltammetry Brdicka reaction, which supported data from spectrophotometry. Subsequently, we used fast protein liquid chromatography for purification of protein–quantum dot conjugates. We obtained the different chromatograms for (1) Apo MT, (2) CdTe QDs and (3) MT–QD complex. We also collected the fractions and subsequently analysed them on the content of Cd and MT, which confirmed the formation of CdTe QDs–MT complex.     

A comparison of classical 90Sr separation methods with selective separation using molecular recognition technology products AnaLig? SR-01 gel, 3M Empore? Strontium Rad Disk and extraction chromatography Sr?Resin

We studied the use of an extraction chromatography for determination of ⁹⁰Sr in contaminated water samples. The aim of our work was to compare selected products from the point of view of the strontium chemical yields and analysis time. Three commercial products, 3M Empore? Strontium Rad Disk, AnaLig^® Sr-01 gel, Sr^®Resin, and two classical methods, liquid?Cliquid extraction with tributhylphosphate and carbonate co-precipitation, were tested for the separation of ⁹⁰Sr. The water sample from nuclear power plant A1 Jaslovske Bohunice was used for radiochemical analysis of ⁹⁰Sr volume activity. Samples were traced with ⁸⁵Sr to monitor strontium chemical recovery and counted either by Cerenkov counting on TRI CARB 2900 TR liquid scintillation counter or low level alpha?Cbeta proportional counter.     

New vegetable and fruit–vegetable juices treated by high pressure

The aim of this work was to find sensory suitable combinations of not commonly used vegetables, that is, cabbage, celeriac and parsnip, into mixed fruit–vegetable juices, two-species vegetable juices and vegetable juices with whey. These juices might have the potential to offer consumers new, interesting, tasty and nutritional products. Another interesting variation could be preparation of vegetable juices in combination with sweet whey. Nutritional and sensory evaluations were carried out using juices prepared in the laboratory. The total phenolic content, in addition to ascorbic acid and antioxidant activity, was determined. The developed juices with high nutritional value should increase very low fruit and vegetable consumption in the Czech population. The prepared juices were high pressure pasteurized (410 MPa). This technique retains the desired levels of important nutritional substances, while being destructive to live microbial cell structure. The germination of spores is suppressed by low pH value.     

Power factor of very thin thermoelectric layers of different thickness prepared by laser ablation

Room temperature conductivity and the Seebeck coefficient of thin layers prepared by laser ablation from Bi₂Te₃ target were explored. The power factor was calculated for samples prepared at substrate temperature of 360°C with the density of the laser beam 5 J cm⁻² and at substrate temperature of 410°C with the density of the laser beam 2 J cm⁻² during the deposition. Oscillations of the conductivity and the power factor with the layer thickness were observed at room temperature. The oscillations of conductivity were also verified at the temperature of 77 K. The period of oscillations depends on the preparation conditions. This behavior has been theoretically explained by the quantum size effect in the layers containing different phases and in addition, it was demonstrated by the X-ray Diffraction measurement. The behavior of the power factor of the layers is compared to the behavior of the figure of merit of the layers published earlier.     

Die Exoelektronen- und Thermoelektronenemission bei einigen Halogeniden

Zusammenfassung Es wird Vergleich angestellt zwischen den experimentellen und theoretischen Thermoemissionskurven für den mono- und bimolekularen Proze bei Kristallen von NaCl und CaF₂, die die Farbzentren F enthalten. Rechnerisch wird der Einflu der Austrittsarbeit auf die Lage der Thermoemissionsmaxima und auf die Intensität der Thermoemission verfolgt. Die bei den Halogeniden erzielten Ergebnisse gaben die Möglichkeit, gewisse Schlüsse zu ziehen über den Mechanismus der Thermoelektronenemission bei Oxydkathoden.

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- NaCl u CaF₂, F. . , .

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Wir danken unseren Kollegen, insbesondere dem Kandidaten der phys. math. Wissenschaften J. Kanturek für die wertvollen Diskussionen und K. Listoová für die sorgfältige Durchführung der Versuche.     

Advances in the Development of Chemical Oxygen-iodine Laser

Results of three problems investigated on a Chemical Oxygen-Iodine Laser (COIL) in our laboratory are presented in connection with the advanced COIL development in the world. These problems concern: i) A gain modulation on the laser transition in iodine atom, I(²P_1/2) - (²P_3/2), by external magnetic field, and its utilization for a COIL output power stabilization, ii) An evaluation of the Einstein A-coefficient of singlet oxygen, O₂(¹ _g), and its utilization in advanced diagnostics for O₂(¹ _g) determination in COIL operation, iii) A chemically driven iodine atom delivery system for advanced COIL.