Organofluorine Hydrazone Derivatives as Multifunctional Anti-Alzheimer's Agents with CK2 Inhibitory and Antioxidant Features

A set of novel hydrazone derivatives were synthesized and analyzed for their biological activities. The compounds were tested for their inhibitory effect on the phosphorylating activity of the protein kinase CK2, and their antioxidant activity was also determined in three commonly used assays. The hydrazones were evaluated for their radical scavenging against the DPPH, ABTS and peroxyl radicals. Several compounds have been identified as good antioxidants as well as potent protein kinase CK2 inhibitors. Most hydrazones containing a 4-N(CH₃)₂ residue or perfluorinated phenyl rings showed high activity in the radical-scavenging assays and possess nanomolar IC₅₀ values in the kinase assays.     

Crowding as an Agronomic Factor Determining the Development of Plants and the Productivity of Linseed (Linum usitatissimum L.)

ABSTRACT

Nine sowing densities of linseed were compared in a two-year experiment. Self-regulation of the density of a linseed stand resulted in a differentiated branching of the plants. The number of capsules on a linseed shoot, as well as seeds in the capsule, and the number of seeds from the shoot were highly varied from year to year, and there is even a stronger differentiation in the weight of 1000 seeds. Linear relationships were noted between the mass of seeds from the linseed plant and the number of capsules. The yield of linseed was affected by both factors. An increasing sowing rate reduced the seed yield from the shoot and the plant. At lower seeding rates, the lateral shoots contributed in the seeds yield of the plant to a higher degree compared to the main ones.     

Linear correlation between pH value of stimulated beef and electrical current intensity

The aim of the present study was to determine mathematical relationships between pH changes in beef 24 h post-slaughter and changes in the intensity of electrical current flowing through bull and heifer carcasses during high-voltage electrical stimulation. The electrical stimulation was applied 40 min postmortem for 120 s. The pH values of m. longissimus thoracis et lumborum were analyzed in the function of electrical current intensity changes and its change during electrical stimulation. Mathematical linear correlations of the y = ax ± b type were demonstrated between pH values at 2, 6, and 24 h postmortem and the initial (I_i) and ultimate (I_u) electrical current intensity values, the difference between them and the initial pH values determined before electrical stimulation. High multiple correlation coefficients (R² = 0.416, α ≤ 0.001) between I_u and pH values 24 h post-slaughter enabled concluding that there is a possibility to predict a pH value of stimulated carcass with high accuracy, and thus also beef quality, based merely on the ultimate electrical current intensity values.     

Estramustine and estrone analogs rapidly and reversibly inhibit deoxyribonucleic acid synthesis and alter morphology in cultured human glioblastoma cells

Estramustine is an estradiol-based agent that has been shown to accumulate in human glioma cells, resulting in a concentration-dependent alteration in cell size and shape within minutes and an inhibition of proliferation over 3 to 6 days. We evaluated human glioblastoma cultures with [3H]thymidine incorporation assays to determine estramustine's early effects on deoxyribonucleic acid synthesis in these tumors. Because estramustine shares a common structural motif with other antimicrotubule drugs, we synthesized four A-ring conjugates of estrone that contained a carbamate moiety but lacked nitrogen mustard. These analogs were examined by [3H]thymidine incorporation and compared with vinblastine. Greater than 70% inhibition of [3H]thymidine incorporation occurred within 1 hour of treatment with estramustine at 10(-5) mol/L, which increased to 80% inhibition at 4 hours. Ethyl carbamate JE208 was nearly as effective as estramustine in inhibiting deoxyribonucleic acid synthesis, and both were more effective than vinblastine. The inhibitory effects of estramustine and estrone analogs were reversible; vinblastine was not reversible. Although estramustine and JE208 induced similar antiproliferative and morphological changes in glioblastoma cells that persisted for at least 4 days, there was a modest recovery of morphology and thymidine incorporation with JE208 after prolonged treatment. The common findings with estramustine and JE208 suggest that these agents may have a similar mechanism of action and form the basis for the investigation of new agents that may rapidly and reversibly inhibit glioblastoma.     

Fundamentals of modelling concurrency using discrete relational structures

We consider relational structures such that is a set and are two binary relations on . For a number of different classes of structures we show that any structure can be represented as the intersection of its maximal extensions. Such a property – called extension completeness – can be seen as a generalisation of Szpilrajn's theorem which states that each partial order is the intersection of its total order extensions. When can be interpreted as causality and as ‘weak’ causality we obtain a model of concurrent histories generalising that based on causal partial orders. Received 1 February 1994 / 6 May 1996     

The significance of appendectomy for appendicitis on subsequent fertility

A study was undertaken to determine fertility in a group of females who as children had been operated on for appendicitis. The 134 women operated on for appendicitis were reviewed. Their ages ranged from 2-18 years at the time of appendectomy. Our data show that perforated appendicitis before puberty has little if any role in the etiology of tubal infertility.     

A dislocation shielding prediction of the toughness transition during cleavage of semibrittle crystals

An interconnected set of observations assesses current equilibrium models of the ductile-brittle-transition temperature (DBTT). This involvesin situ transmission electron microscopy (TEM) studies of crack-tip dislocations in single and polycrystals and bulk fracture toughness tests at various temperatures. Beyond K_I values of 8 MPa · m^1/2 in both iron-base single and polycrystals, large numbers of redundant dislocations are created, as postulated recently by Weertman. [38] Still, the necessary shielding dislocations, as required by equilibrium, can be detected at values as high as 20 and 40 MPa · m^1/2 byex situ TEM and electron channeling, respectively. In addition, the close approach of dislocations to the crack tip in some of the studies, as opposed to others, suggests that large dislocation free zones (DFZ) are a thin-film artifact. However, a failure criterion based partly on the Rice-Thomson model’21 is both consistent with the absence of a large DFZ and observed fracture toughness variations with test temperature. It is emphasized that this toughness transition is entirely in the semibrittle regime where cleavage is the failure mode. Nevertheless,K _lc values increase from 3 to 60 MPa·m^1/2 with an increase in test temperature. This article is based on a presentation made in the symposium “Quasi-Brittle Fracture” presented during the TMS fall meeting, Cincinnati, OH, October 21–24, 1991, under the auspices of the TMS Mechanical Metallurgy Committee and the ASM/MSD Flow and Fracture Committee.     

Impossible and ambiguous shading patterns

A smooth object depicted in a monochrome image will often exhibit brightness variation, or shading. A problem much studied in computer vision has been that of how object shape may be recovered from image shading. When the imaging conditions are such that an overhead point-source illuminates a smooth Lambertian surface, the problem may be formulated as that of finding a solution to an eikonal equation. This article will focus on the existence and uniqueness of such solutions, reporting recent results obtained. With regard to existence, shading patterns are exhibited for which there is no corresponding object shape. Specifically, a necessary and sufficient condition is presented for a circularly symmetric eikonal equation to admit exclusively unbounded solutions; additionally, a sufficient condition is given for an eikonal equation to have no solution whatsoever. In connection with uniqueness, we consider eikonal equations, defined over a disc, such that the Euclidean norm of the gradient of any solution is circularly symmetric, vanishes exactly at the disc center, and diverges to infinity as the circumference of the disc is approached. Contrary to earlier influential work, a class of such eikonal equations is shown to possess simultaneously circularly symmetric and noncircularly symmetric bounded smooth solutions.