1‐Arylsulfonyl‐5‐(N‐hydroxyacrylamide)indolines Histone Deacetylase Inhibitors Are Potent Cytokine Release Suppressors

A series of 1‐arylsulfonyl‐5‐(N‐hydroxyacrylamide)indolines ( 7 – 15 ) has been developed; the compounds exhibited potent histone deacetylase (HDAC) inhibitory activities. Notably, almost all of this series exhibited better HDAC‐inhibitory and antiproliferative activities than 3‐(1‐benzenesulfonyl‐1H‐indol‐5‐yl)‐N‐hydroxyacrylamide ( 6 ), as reported in a previous study. Among these compounds, 3‐[1‐(4‐methoxybenzenesulfonyl)‐2,3‐dihydro‐1H‐indol‐5‐yl]‐N‐hydroxyacrylamide ( 9 ) showed a two‐ to tenfold increase in activity compared to SAHA ( 1 ) in the suppression of lipopolysaccharide‐induced cytokine production. Compound 9 also caused a marked reduction in carrageenan‐induced acute inflammation in a rat model. Taken together, these data indicated that 1‐arylsulfonyl‐5‐(N‐hydroxyacrylamide)indolines HDAC inhibitors exhibit potent anti‐inflammatory activity.     

Neural Membrane Signaling Platforms

Throughout much of the history of biology, the cell membrane was functionally defined as a semi-permeable barrier separating aqueous compartments, and an anchoring site for proteins. Little attention was devoted to its possible regulatory role in intracellular molecular processes and neuron electrical signaling. This article reviews the history of membrane studies and the current state of the art. Emphasis is placed on natural and artificial membrane studies of electric field effects on molecular organization, especially as these may relate to impulse propagation in neurons. Implications of these studies for new designs in artificial intelligence are briefly examined.     

Factors Affecting the Study of Chemistry in Different Countries Around the World: Findings from an International Survey

Improving teaching and student learning in chemistry classrooms is an important goal that is constantly researched. Several comparative studies of science teaching have been carried out on different parameters, e. g. misconceptions which science teachers and students may have regarding the scientific concepts they learn and teach. Here we describe science teaching in general, and chemistry teaching in particular, in 12 countries including Israel. Different parameters are compared, including the hours that are devoted to science, the subjects included, the pedagogy, and teachers′ salaries. The survey covers all school levels: elementary school, secondary school and high school. At the high‐school level, the comparison focused on chemistry studies. In this study the variances variables, such as the hours that are allocated for science teaching, did not show an appreciable effect on students′ achievements. It was also found that, in countries where chemistry studies at the high‐school level are not mandatory, innovative pedagogies are more likely to replace the traditional chemistry teaching methods where chemistry is taught according to the structure of the subject based on basic concepts that underlie the curriculum. The study provided an additional support to the importance of the professional development of science and chemistry teachers and suggest that the autonomy that is given to them could influence the quality of science teaching and students′ achievements.     

Characterization of the weak link of wool fibers

The variance of fiber morphology along a fiber and the natural and artificial flaws in the fiber structure represent the primary reasons for the weak link of fibers. Accordingly, the fiber weak link can be divided into two types, that is, the geometrical thinnest part and the structural weak point. Scanning electron microscopic observation was used to characterize the morphological features of the fiber weak points whose forms are the normal thin sections, natural flaws, and artificial damage. Both the fiber profile morphology and the tensile behavior of wool fibers have been measured using a single‐fiber analyzer (SIFAN) and an optical microscope with a CCD camera plus an XQ‐1 fiber tensile tester (OM + XQ). The results from the SIFAN and OM+XQ methods indicate that the fibers breaking at their minimum diameters represent only one part of the broken fibers. The percentage of this kind of breakage is in the range of 40–60%. A new approach is presented to identify the weak‐point breakage relying on the fiber tensile behavior. The experimental results show that the probabilities of weak‐point, normal, and thinnest‐part breakage evaluated by these methods approximate 40, 60, and slightly more than 80%, respectively. © 2003 Wiley Periodicals, Inc. J Appl Polym Sci 90: 1206–1212, 2003     

Synthetic and Biological Studies of Sesquiterpene Polygodial: Activity of 9‐Epipolygodial against Drug‐Resistant Cancer Cells

Polygodial, a terpenoid dialdehyde isolated from Polygonum hydropiper L., is a known agonist of the transient receptor potential vanilloid 1 (TRPV1). In this investigation a series of polygodial analogues were prepared and investigated for TRPV1‐agonist and anticancer activities. These experiments led to the identification of 9‐epipolygodial, which has antiproliferative potency significantly exceeding that of polygodial. 9‐Epipolygodial was found to maintain potency against apoptosis‐resistant cancer cells as well as those displaying the multidrug‐resistant (MDR) phenotype. In addition, the chemical feasibility for the previously proposed mechanism of action of polygodial, involving the formation of a Paal–Knorr pyrrole with a lysine residue on the target protein, was demonstrated by the synthesis of a stable polygodial pyrrole derivative. These studies reveal rich chemical and biological properties associated with polygodial and its direct derivatives. These compounds should inspire further work in this area aimed at the development of new pharmacological agents, or the exploration of novel mechanisms of covalent modification of biological molecules with natural products.     

Biomass Recovery Method for Adenosine Triphosphate (ATP) Quantification Following UV Disinfection

A biomass recovery method was developed to monitor UV disinfection efficacy using adenosine triphosphate (ATP). Typically, disinfection monitoring at wastewater treatment facilities (WWTFs) involves quantifying fecal and total coliforms or colony forming units, the results of which take a minimum of 24 h to produce. ATP quantification immediately before and after UV treatment, which takes only minutes, shows little reduction and often an increase in the microbial population since UV irradiation results in cells that are viable (i.e., still producing ATP) but not culturable. To overcome this, our biomass recovery method incorporates an incubation step to encourage life cycling of microbes. Average log reductions in cellular ATP (cATP) were found to be ?0.28 ± 0.19, ?0.011 ± 0.153, ?0.17 ± 0.32, and 0.065 ± 0.074 using direct ATP measurements on UV-treated samples from WWTFs A, B, C, and D, respectively, while those using the recovery method were correspondingly 0.17 ± 0.34, 1.8 ± 0.8, 0.20 ± 0.35, and 0.72 ± 0.26. The response of the biomass recovery-ATP method indicated a significant direct correlation to the microbial population reduction observed in heterotrophic plate count (HPC) and Colilert® methods using both pure Escherichia coli culture and secondary municipal wastewater effluent.     

Synthesis of carbon nanosheets by inductively coupled radio-frequency plasma enhanced chemical vapor deposition

An ultrathin sheet-like carbon nanostructure, carbon nanosheet, has been effectively synthesized with CH₄ diluted in H₂ by an inductively coupled radio-frequency plasma enhanced chemical vapor deposition. Nanosheets were obtained without catalyst over a wide range of deposition conditions and on a variety of substrates, including metals, semiconductors and insulators. Scanning electron microscopy shows that the sheet-like structures stand on edge on the substrate and have corrugated surfaces. The sheets are 1 nm or less in thickness and have a defective graphite structure. Raman spectra show typical carbon features with D and G peaks at 1350 and 1580 cm⁻¹, respectively. The intensity ratio of these two peaks, I(D)/I(G), increases with methane concentration or substrate temperature, indicating that the crystallinity of the nanosheets decreases. Infrared and thermal desorption spectroscopies reveal hydrogen incorporation into the carbon nanosheets.     

Pressure Fluctuation Analysis of Laboratory Scale Air/Polyethylene Fluidized Beds

Differential pressure fluctuations were studied along the wall of a laboratory scale column filled with a polyethylene resin. Air flow rates to the column were varied in order to examine the changes in wall pressure with respect to superficial gas velocity. Statistical and spectral analysis was used to study the periodic features of column wall pressure measurements in the dense region of a fluidized bed. From the analysis, it is evident that multiple flow regimes exist in the column. These flow regimes are dependent upon the height above the distributor. Results also show a significant peak developing at 1 Hz as superficial gas velocity increases.     

Defining Media Enjoyment as the Satisfaction of Intrinsic Needs

This article presents a model of enjoyment rooted in self‐determination theory ( Deci & Ryan, 1985 ) that includes the satisfaction of three needs related to psychological well‐being: autonomy, competence, and relatedness. In an experiment designed to validate this conceptualization of enjoyment, we manipulate video game characteristics related to the satisfaction of these needs and examine their relative effects on enjoyment. The validated model explains 51% of the variance in enjoyment, even without including needs usually studied in relation to enjoyment such as pleasure seeking. Results indicate the utility of defining enjoyment as need satisfaction. These results are discussed in terms of a broader conceptualization of enjoyment represented as the satisfaction of a comprehensive set of functional needs.