Synthesis of 3,4‐Fused 2‐Quinolones from an (ortho‐Aminophenyl)propiolate via Sequential Cycloaddition/Lactam Formation

An N‐phthalimide‐protected (ortho‐aminophenyl)propiolate was prepared by the carboxylation of the corresponding silylalkyne precursor with carbon dioxide. The obtained propiolate was further transformed to various 3,4‐fused 2‐quinolones via cycloadditions and subsequent deprotection/lactam formation.

     

Fatigue behaviour of dissimilar friction stir welds between wrought and cast aluminium alloys

Wrought aluminium alloy, A6016-T4, was welded to cast one ADC12 by a friction stir welding technique. A6016 was set on the advancing side, while ADC12 was on the retreating side based on the pre-tensile test results. The dissimilar welds exhibited lower fatigue strengths than A6016 but higher than that of ADC12. Fatigue strengths increased when the tool was offset into ADC12, which could be explained based on the risk volume concept. When ADC12 was set on the advancing side, the fatigue strengths decreased. Microstructural observation revealed that the macroscopic structure in the stir zone drastically changed by putting ADC12 on the advancing side, and insufficient mixing of dissimilar alloys resulted in the lower fatigue strengths.     

Pesticide adsorption by granular activated carbon adsorbers. 2. Effects of pesticide and natural organic matter characteristics on pesticide breakthrough curves

The principal objective of this study was to elucidate mechanisms by which NOM affects the adsorption of a nonpolar (simazine) and a polar (asulam) herbicide on activated carbon. Experiments were carried out in microcolumns that were continuously fed solutions containing NOM with different molecular weight (MW) distributions and intermittently solutions containing the same NOM plus simazine or asulam. The MW distributions of a groundwater NOM were altered by coagulation and ultrafiltration, which resulted in the preferential removal of high-MW, UV260-absorbing NOM. At a given NOM loading, the simazine removal efficiency was higher in the column that was preloaded with raw groundwater than in columns receiving coagulated or ultrafiltered water. In contrast, the asulam removal efficiency was similar for all three NOM solutions at a given NOM loading. Therefore, the results suggested that low-MW, UV260-absorbing NOM molecules competed directly with strongly adsorbing pesticides, such as simazine, for adsorption sites. For more weakly adsorbing pesticides, such as asulam, direct competition for adsorption sites originated not only from the strongly adsorbing, low-MW NOM, but also from more weakly adsorbing, higher-MW NOM. Consequently, the competing NOM fraction increases as the adsorbability of the SOC decreases, a result that was confirmed by adsorption data for additional pesticides of similar size. However, a smaller pesticide competed more effectively for adsorption sites than a larger pesticide of similar polarity, suggesting that the concentration of competing NOM decreases as the MW of the SOC decreases.     

Effects of microbial degradation of biofoulants on microfiltration membrane performance in a membrane bioreactor

In membrane bioreactors (MBRs) for wastewater treatment, membrane fouling, particularly biofouling caused by soluble microbial products (SMP), is a nuisance problem causing decreases in permeation flux. In a previous study, we identified primary biofoulants of microfiltration (MF) membranes in SMP as polysaccharides containing uronic acids that undergo inter- and intramolecular ionic cross-linking by polyvalent cations, forming a gelatinous mass that clogs membrane pores. In the present study, we therefore attempted to isolate biofoulant-degrading microorganisms from activated sludge on a polygalacturonic acid-overlaid agar medium and evaluate their efficiency for preventing biofouling of MF membranes. Among the isolates, the fungal strain HO1 identified as Phialemonium curvatum degraded 30% of polysaccharides containing uronic acids into smaller molecules in a SMP solution containing a high concentration of saccharides after 30 days of cultivation. Microfiltration tests using a laboratory-scale submerged MBR indicated that the filtration resistance of this degraded SMP solution was lower than that of the control SMP solution without fungal inoculation. Importantly, accumulation of gelatinous mass on the membrane responsible for biofouling was avoided in the SMP solution augmented with P. curvatum HO1 during the microfiltration test. This is the first report to describe a new method for avoiding biofouling of MBRs by microbial degradation of primary biofoulants.     

Cell type-specific modulation of cell growth by transforming growth factor beta 1 does not correlate with mitogen-activated protein kinase activation

Transforming growth factor beta 1 (TGF-beta 1) is a multifunctional cytokine that positively or negatively regulates the proliferation of various types of cells. In this study we have examined whether or not the activation of the mitogen-activated protein (MAP) kinases is involved in the transduction of cell growth modulation signals of TGF-beta 1, as MAP kinase activity is known to be closely associated with cell cycle progression. Although TGF-beta 1 stimulated the growth of quiescent Balb 3T3 and Swiss 3T3 cells, it failed to detectably stimulate the tyrosine phosphorylation and activation of the 41- and 43-kDa MAP kinases at any time point up to the reinitiation of DNA replication. TGF-beta 1 also failed to stimulate the expression of the c-fos gene. Furthermore, TGF-beta 1 synergistically enhanced the mitogenic action of epidermal growth factor (EGF) without affecting EGF-induced MAP kinase activation in these fibroblasts, and it inhibited the EGF-stimulated proliferation of mouse keratinocytes (PAM212) without inhibiting EGF-induced MAP kinase activation. Thus, the ability of TGF-beta 1 to modulate cell proliferation is apparently not associated with the activation of MAP kinases. In this respect, TGF-beta 1 is clearly distinct from the majority, if not all, of peptide growth factors, such as platelet-derived growth factor and EGF, whose ability to modulate cell proliferation is closely associated with the activation of MAP kinases. These results also suggest that the activation of MAP kinases is not an absolute requirement for growth factor-stimulated mitogenesis.     

Neutron spectra and angular distributions of concrete-moderated neutron calibration fields at JAERI

The Facility of Radiation Standards of Japan Atomic Energy Research Institute has been equipped with concrete-moderated neutron calibration fields as simulated workplace neutron fields. The fields use an 241Am-Be neutron source placed in the narrow space surrounded by concrete bricks, walls and floor. The neutron spectra and the neutron fluence rates of the fields were measured with the Bonner multi-sphere spectrometer system (BMS), spherical recoil-proton proportional counters, and a liquid scintillation counter (NE-213). The results were compared with each other. The reference values of H*(10) were determined from the results of BMS. The angular distributions of neutron fluence were calculated using MCNP-4B2 to obtain the reference values of Hp(10). The calculated results show that the scattered neutrons have a wide range of incident angles. The reference Hp(10) values considered the angular distribution were found to be 10-18% smaller than those without consideration.     

Bacterially Secretable Single-Chain Tandem Macrocyclic Peptides for High Affinity and Inhibitory Activity

The inhibition of protein-protein interactions (PPIs) is an effective approach for therapy. Owing to their large binding surface areas to target proteins, macrocyclic peptides are suitable molecules for PPI inhibition. In this study, we developed single-chain tandem macrocyclic peptides (STaMPtides) that inhibits the vascular endothelial growth factor (VEGF) receptor 2 (VEGFR2). They were artificially designed to comprise two different VEGFR2-binding macrocyclic peptides linked in tandem by peptide linkers and secreted by Corynebacterium glutamicum. Most potent VEGFR2-inhibitory STaMPtides with length-optimized linkers exhibited >1000 times stronger inhibitory activity than their parental monomeric peptides, possibly due to the avidity effect of heterodimerization. Our approach of using STaMPtides for PPI inhibition may be used to inhibit other extracellular factors, such as growth factors and cytokines.