Concentration of chosen oxycholesterols in plasma of pregnant women with pregnancy-induced hypertension

Solid-phase extraction (SPE) was applied for isolation of oxycholesterols from plasma lipid extract from pregnant women with hypertension and from a control group. Separation of oxycholesterols fraction was performed in an SD II horizontal chamber (Chromdes, Poland) using silica gel and octadecyl RPC18 silica gel TLC plates (Merck and Machery Nagel). Visualization was carried out under UV light after Liebermann-Burchard reaction specific for cholesterol and its derivatives. The oxycholesterols (5-cholestene-3beta-ol-7-one, sum of 5-cholestene-3beta, 7beta-diol and 5-cholestene-3beta, 7alpha-diol and sum of 5alpha,6alpha-epoxycholestan-3beta-ol and 5beta, 6beta-epoxycholestan-3beta-ol) were quantified by chromatograms scanning in reflectance and fluorescence mode using a CS 9301 densitometer (Shimadzu). The total concentration of the investigated oxycholesterols in the plasma of pregnant women was up to 5000 ng/mL and was statistically significantly higher in women with pregnancy induced hypertension (PIH).     

A new class of arylpiperazine derivatives: the library synthesis on SynPhase lanterns and biological evaluation on serotonin 5-HT(1A) and 5-HT(2A) receptors

An efficient solid-supported method for the synthesis of a new class of arylpiperazine derivatives containing amino acid residues has been developed. A 72-membered library was synthesized on SynPhase Lanterns functionalized by a BAL linker. A one-pot cleavage/cyclization step of aspartic and glutamic acid derivatives yielded succinimide- and pyroglutamyl-containing ligands (chemsets 9 and 10). The library representatives under study showed different levels of affinity for 5-HT(1A) and 5-HT(2A) receptors (estimated K(i) = 24-4000 and 1-2130 nM, respectively). Several dual 5-HT(1A)/5-HT(2A) ligands were found, of which two (9(3,3) and 9(3,5)) displayed high 5-HT(2A) affinity comparable to that of the reference drug ritanserin. A set of individual fragment contributions for the prediction of 5-HT(1A) and 5-HT(2A) affinity of all the library members were defined on the basis of the Free-Wilson analysis of 26 compounds. An alkylarylpiperazine fragment had essentially the same impact on the affinity for both receptors, whereas different terminal amide fragments were preferred by 5-HT(1A) (chemset 17, R(2) = adamantyl) and 5-HT(2A) (chemset 9, R(2) = norborn-2-ylmethyl) binding sites.     

Developing of Fluorescence Probes Based on Stilbazolium Salts for Monitoring Free Radical Polymerization Processes. II

The series of 1-methyl-4-(4-aminostyryl)pyridinium perchlorates was investigated as fluorescent probes for the monitoring of the free radical polymerization progress. The study on the changes in fluorescence intensity and spectroscopic shifts of studied compounds were carried out during thermally initiated polymerization of methyl methacrylate. The purpose of these studies was to find a relationship between the structure of fluorophore and the changes in their fluorescence shape and intensity observed during the monomer conversion into polymer. The probes under the study during the course of polymerization increase their fluorescence intensity at least one order of magnitude. Such increase qualified the tested probes as good fluorescence probes.     

Element Fractionation in Suspended Matter in Landfill Leachate Using Single Extractions

This study presents the determination of the pseudo-total and available element contents in suspended matter in leachate using stripping voltammetry (DPASV) on a hanging mercury drop electrode and an inductively coupled plasma mass spectrometer (ICP-MS). The following elements were studied: Zn, Pb, As, Sb, Co, Cu, Ni, Cr, Sn, Mo and Cd. To determine the pseudo-total metal contents, we applied microwave digestion using a mixture of HNO₃ and HClO₄ with a small quantity of HF. To assess the metal availability from suspended matter in leachate, the single extraction procedure with 0.1mol·L^–1 acetic acid and 0.01mol·L^–1 ammonium acetate was applied. Metal bioavailability based on single extraction with 15% H₂O₂ was determined. We also estimated the association with particular phases of suspended matter in leachate.     

Structure of Escherichia coli dUTPase in Solution: A Small Angle Neutron Scattering Study

The present study investigates shape properties of the enzyme dUTPase from Escherichia coli in the solution phase. In this work small angle neutron scattering (SANS) findings on dUTPase/D₂O solutions for temperature values of T = 8 °C and T = 37 °C are presented. The analysis of SANS data, carried out by using a prolate ellipsoid core/shell model fitting and the well‐known Guinier and Zimm analysis procedures allows the characterization of the shape of the protein in solution. By means of the comparison with experimental and theoretical data existing in literature on dUTPase in the crystalline state, we find that the protein in solution maintains its dimensions before the denaturation process. Furthermore, by analyzing the SANS spectra of dUTPase/D₂O/trehalose solutions, we emphasize the bioprotective effects of trehalose on the protein.

Structure of dUTPase.     

On the structure of level sets of uniform and Lipschitz quotient mappings from $$ \mathbb{R}^n $$ to $$ \mathbb{R} $$

We study two questions posed by Johnson, Lindenstrauss, Preiss, and Schechtman, concerning the structure of level sets of uniform and Lipschitz quotient mappings from . We show that if , is a uniform quotient mapping then for every has a bounded number of components, each component of separates and the upper bound of the number of components depends only on and the moduli of co-uniform and uniform continuity of .Next we prove that all level sets of any co-Lipschitz uniformly continuous mapping from to are locally connected, and we show that for every pair of a constant and a function with , there exists a natural number , so that for every co-Lipschitz uniformly continuous map with a co-Lipschitz constant and a modulus of uniform continuity , there exists a natural number and a finite set with card so that for all has exactly components, has exactly components and each component of is homeomorphic with the real line and separates the plane into exactly 2 components. The number and form of components of for are also described - they have a finite tree structure.     

One-Complemented Subspaces of Real Sequence Spaces

Characterizations are given for 1-complemented hyperplanes of strictly monotone real Lorentz spaces and 1-complemented finite codimensional subspaces (which contain at least one basis element) of real Orlicz spaces equipped with either Luxemburg or Orlicz norm.     

Knoevenagel Reaction of malononitrile and its “dimer” with β-ketoanilides

The reaction of benzoylacetanilides with malononitrile has been investigated. The structure of the compounds obtained (2, 3, 4) have been assigned on the basis of chemical properties and spectral data.

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Die Knoevenagel-Reaktion von Malodinitril und seinem Dimer mit -Ketoaniliden

Zusammenfassung Die Reaktion von Malodinitril mit Benzoylacetaniliden wurde untersucht. Die Struktur der dabei erhaltenen Verbindungen (2–4) wurde auf Basis der chemischen und spektroskopischen Eigenschaften zugeordnet.

     

Synthesis and biological properties of 1,8‐naphthalimidebutylamines. Serotonin 5‐HT1A and 5‐HT7 binding data and pass‐assisted search

Syntheses of the N‐substituted butyl derivatives of 1,8‐naphthalimide ( 1‐8 ), containing various arylpiperazines, tetrahydroisoquinoline and methylhomopiperazine moieties attached at 4‐position of the butyl chain have been described. Biological activities were evaluated in vitro for their ability to bind to serotonin 5‐HT_1A and 5‐HT₇ receptors. Due to the structural similarity of derivatives 1‐8 to psychotropic agents, the pharmacological properties of target compounds were predicted using PASS program.     

Methyl 4-O-acetyl-3-azido- and 3-azido-4-O-methylsulfonyl-2,3,6,-trideoxyhex-5- enopyranosides in DFT-level conformational studies

Geometry optimizations at the B3LYP level of density functional theory (DFT) are reported for methyl 4-O-acetyl-3-azido- and 3-azido-4-O-methylsulfonyl-2,3,6-trideoxy-alpha,beta-d-threo- and -beta-d-erythro-hex-5-enopyranosides. The most stable conformers for each compound are presented, along with the corresponding enthalpies and Gibbs free energies. The influence of the exocyclic double bond on the chair conformation is discussed. Conformations of the 1-OMe, 3-N3, and 4-OAc groups were examined, and delocalization in the OAc and N3 groups was demonstrated. The contributions of particular conformers to the total number of structures found for each hex-5-enopyranoside were calculated. The theoretical results are compared with assignments based on 1H NMR studies.