Synthesis of vinca alkaloids and related compounds XXVII formation of a stable 3-acylindolenine

A stable 3-acylindolenine derivative (2) has been prepared $\text{via}$ intramolecular electrophilic acylation. The reactivity of 2 has been studied.     

Effect of thermal transformation and stability on the flammability of PAN precursors-based carbon fibres

Journal of Thermal Analysis and Calorimetry - During the development of the carbon fibres and oxidized fibres, the aim was to get a material with extraordinary mechanical properties. Nowadays, it...     

On the existence of infinitely many periodic solutions to some problems of n-body type

We prove the existence of infinitely many periodic solutions with prescribed period to a class of problems of n-body type.     

Thermal stability of rat uterus during development

Summary The age dependence of thermal denaturation was monitored in rats anaesthetized after they're born at 7^th, 14^th, 21^st, 28^th, 35^thand 42^nddays. The samples were stored in rigor or physiological saline solution. The DSC scans in the early age groups show a low temperature exotherm (connective tissues: from gel to liquid crystal transition) and one endotherm (it is very probably the myosin). During further development the endotherms became more and more complex (due to the development of contractile system). At 42 days the scans seem to be similar to the adult ones. In the two buffers the endotherms markedly differ showing that the ATPase activity is present. In adult uterus, treated with nucleotides or estrogen, this activity significantly differs from the skeletal muscle. On the basis of our results we suppose, that the age dependent changes are decisive processes in the development of rat uterus.     

An attempt to distinguish between the components of a mixture of isomeric fragment ions

The [C₇H₁₀NO₃]⁺ ion in the normal mass spectrum of 2-ethoxycarbonyl-5-oxo-2-pyrrolidinepropanoic acid was shown to correspond to a mixture of two isomeric structures. By decreasing the ionizing electron energy, the one containing a CH₂CH₂COOH group becomes dominant. The proportion of the concentrations of the two isomeric ions was calculated by comparing their daughter ion spectra (obtained by linked scan at constant B/E) with the analogous spectra of a derivative partially labelled by deuterium at the carboxyl and amide groups.     

Highly enantioselective synthesis of 2-furanyl-hydroxyacetates from furans via the Friedel-Crafts reaction

The Friedel-Crafts reaction of alkyl glyoxylates with variously substituted furans was found to be efficiently catalyzed under simple, undemanding conditions by a 6,6'-dibromo-BINOL/Ti(IV) complex with high enantioselectivity. The reaction afforded chiral substituted 2-furanyl-hydroxyacetic acid esters, compounds of high synthetic interest, in good yield and enantiomeric excess, in most examples in the range of 90-97%.     

Estrogen-induced cholestasis results in a dramatic increase of b-series gangliosides in the rat liver

Hepatic ganglioside composition was investigated in normal and cholestatic Wistar rats. Cholestasis was induced by 17alpha-ethinylestradiol (EE; 5 mg/kg body weight s.c. for 18 days). As compared with controls, the EE administration resulted in severe cholestasis, as indicated by biochemical as well as morphological signs. Gangliosides isolated from the liver tissue were separated by TLC, with resorcinol-HCl detection and densitometric evaluation. As compared with controls, the total hepatic lipid sialic acid content in cholestatic rats was increased almost 2-fold (44.3 +/- 15.2 vs 79.1 +/- 9.0 nmol/g wet weight of liver tissue, p < 0.01). This increase was primarily due to the increase of ganglioside GD1a (3.6 +/- 1.0 vs 11.8 +/- 3.0 nmol/g wet weight of liver tissue, p = 0.001), as well as to the enormous up-regulation of b-series gangliosides GD3 (0.08 +/- 0.03 vs 2.0 +/- 1.2 nmol/g wet weight of liver tissue, p = 0.002), GD1b (0.1 +/- 0.06 vs 5.4 +/- 1.6 nmol/g wet weight of liver tissue, p = 0.002) and GT1b (0.06 +/- 0.03 vs 6.4 +/- 2.6 nmol/g wet weight of liver tissue, p = 0.002). As the majority of gangliosides are concentrated in cell membranes, our findings suggest that dramatic increase of b-series gangliosides might contribute to the protection of hepatocytes against the deleterious effects of cholestasis.     

Quantitative mass spectrometry for bacterial protein toxins--a sensitive, specific, high-throughput tool for detection and diagnosis

Matrix-assisted laser-desorption time-of-flight (MALDI-TOF) mass spectrometry (MS) is a valuable high-throughput tool for peptide analysis. Liquid chromatography electrospray ionization (LC-ESI) tandem-MS provides sensitive and specific quantification of small molecules and peptides. The high analytic power of MS coupled with high-specificity substrates is ideally suited for detection and quantification of bacterial enzymatic activities. As specific examples of the MS applications in disease diagnosis and select agent detection, we describe recent advances in the analyses of two high profile protein toxin groups, the Bacillus anthracis toxins and the Clostridium botulinum neurotoxins. The two binary toxins produced by B. anthracis consist of protective antigen (PA) which combines with lethal factor (LF) and edema factor (EF), forming lethal toxin and edema toxin respectively. LF is a zinc-dependent endoprotease which hydrolyzes specific proteins involved in inflammation and immunity. EF is an adenylyl cyclase which converts ATP to cyclic-AMP. Toxin-specific enzyme activity for a strategically designed substrate, amplifies reaction products which are detected by MALDI-TOF-MS and LC-ESI-MS/MS. Pre-concentration/purification with toxin specific monoclonal antibodies provides additional specificity. These combined technologies have achieved high specificity, ultrasensitive detection and quantification of the anthrax toxins. We also describe potential applications to diseases of high public health impact, including Clostridium difficile glucosylating toxins and the Bordetella pertussis adenylyl cyclase.