Protein tyrosine phosphatase 1B inhibitors from a marine-derived fungal strain aspergillus sp. SF-5929

Abstract

In the course of our continuing investigation of bioactive secondary metabolites from marine-derived fungal strains, a racemate of a novel diphenolic derivative named (±)-tylopilusin D (1) along with ten previously known secondary metabolites (2–11) were isolated from a marine-derived fungal strain Aspergillus sp. SF-5929. Their structures were elucidated mainly by analysis of NMR and MS data. In addition, the inhibitory effects of the isolated compounds against protein tyrosine phosphatase 1B (PTP1B) activity were evaluated, and compounds 1, 2, and 5–7 inhibited PTP1B activity with IC₅₀ values ranging from 3.3 to 8.1?µM. Kinetics studies suggested that compounds 1, 2, and 5 had noncompetitive inhibitory effects against PTP1B.     

Pore formation in in situ processed MgB2 superconductors

MgB₂ bulks were prepared by an in situ process which utilizes the reaction between boron and magnesium powder. The reaction time was fixed at 0.5 h and the temperature was changed from 600 °C to 1000 °C. The density decrease due to pore formation and mass (mainly magnesium) loss during the formation reaction of MgB₂ was observed in all samples. In addition to the pore formation, a pellet expansion which can be explained by the outgrowth of MgB₂ grains was also observed. Two different mechanisms were adopted to explain the pore formation; Kirkendall pores formed at a temperature below the melting point (m.p.) of magnesium by a difference in the diffusivity between magnesium and boron, and the pores formed at a temperature above the m.p. by melting of magnesium and a capillary movement. The density, T_c and J_c results suggest that the current carrying capacity can be improved by a careful control of the process parameters regarding a pore evolution.     

Anti-biofouling properties of comblike block copolymers with amphiphilic side chains

Surfaces of novel block copolymers with amphiphilic side chains were studied for their ability to influence the adhesion of marine organisms. The surface-active polymer, obtained by grafting fluorinated molecules with hydrophobic and hydrophilic blocks to a block copolymer precursor, showed interesting bioadhesion properties. Two different algal species, one of which adhered strongly to hydrophobic surfaces, and the other, to hydrophilic surfaces, showed notably weak adhesion to the amphiphilic surfaces. Both organisms are known to secrete adhesive macromolecules, with apparently different wetting characteristics, to attach to underwater surfaces. The ability of the amphiphilic surface to undergo an environment-dependent transformation in surface chemistry when in contact with the extracellular polymeric substances is a possible reason for its antifouling nature. Near-edge X-ray absorption fine structure spectroscopy (NEXAFS) was used, in a new approach based on angle-resolved X-ray photoelectron spectroscopy (XPS), to determine the variation in chemical composition within the top few nanometers of the surface and also to study the surface segregation of the amphiphilic block. A mathematical model to extract depth-profile information from the normalized NEXAFS partial electron yield is developed.     

Constructing connected bicritical graphs with edge-connectivity 2

A graph $G$ is said to be bicritical if the removal of any pair of vertices decreases the domination number of $G$. For a bicritical graph $G$ with the domination number $t$, we say that $G$ is $t$-bicritical. Let $\lambda \left(G\right)$ denote the edge-connectivity of $G$. In [2], Brigham et al. (2005) posed the following question: If $G$ is a connected bicritical graph, is it true that $\lambda \left(G\right)\ge 3?$In this paper, we give a negative answer toward this question; namely, we give a construction of infinitely many connected $t$-bicritical graphs with edge-connectivity $2$ for every integer $t\ge 5$. Furthermore, we give some sufficient conditions for a connected $5$-bicritical graph to have $\lambda \left(G\right)\ge 3$.     

Effect of apex strake incidence-angle on the vortex development and interaction of a double-delta wing

The vortex flow characteristics of a sharp-edged delta wing with an apex strake was investigated through the visualization and particle image velocimetry (PIV) measurement of the wing-leeward flow region, and the wing-surface pressure measurement. The wing model was a flat-plate, and 65°-sweep cropped-delta wing with sharp leading edges. The apex strake was also a flat-plate wing with a cropped-delta shape of 65°/90° sweep, and it can change its incidence angle. The flow Reynolds number was 2.2 × 10⁵ for the flow visualization and 8.2 × 10⁵ for the PIV and wing-surface pressure measurements. The physics of the vortex flow in the wing-leeward flow region and the suction-pressure distribution on the wing upper-surface were interrelated and analyzed. The effect of a positive (negative) strake incidence-angle was the upward movement of the strake and wing vortices away from (downward movement of the strake and wing vortices toward) the wing-upper surface and the delayed (enhanced) coiling interaction between them. This change of vortex flow characteristics projected directly on the suction pressure distribution on the wing upper-surface.     

Copper-catalyzed aerobic oxidative dehydrogenation for conversion of 2-(alkylthio)-1,4-dihydropyrimidines to 2-(alkylthio)pyrimidines

A simple and efficient aerobic oxidative dehydrogenation reaction method for the conversion of 2-(alkylthio)-1,4-dihydropyrimidines to 2-(alkylthio)pyrimidines using copper catalyst with no additives, such as an oxidant, acid, or base, has been developed. The reaction was successful with a wide range of 2-(alkylthio)-1,4-dihydropyrimidine substrates.     

Characteristic polynomials of complement of graph bundles and their applications

We study the structure of the complement of an F-bundle over a graph G when it can be expressed as an F-bundle over another graph G. In particular, we compute the characteristie polynomial of the complement of an F-bundle when its voltages lie in and abelian subgroup Г of Aut(F) which acts freely and transitively on the vertices of the fiber F Some applications to regular embeddings of graph bundles into Euclidean spaces are also discussed