Designing Multitarget Anti-inflammatory Agents: Chemical Modulation of the Lumiracoxib Structure toward Dual Thromboxane Antagonists-COX-2 Inhibitors

A series of lumiracoxib derivatives were designed to explore the influence of isosteric substitution on balancing COX-2 inhibition and thromboxane A(2) prostanoid (TP) receptor antagonism. The compounds were synthesized through a copper-catalyzed coupling procedure and characterized for their pK(a) values. TP receptor antagonism was assessed on human platelets; COX-2 inhibition was determined on human isolated monocytes and human whole blood. TPα receptor binding of the most promising compounds was evaluated through radioligand binding assays. Some of the isosteric substitutions at the carboxylic acid group afforded compounds with improved TP receptor antagonism; of these, a tetrazole derivative retained good COX-2 inhibitory activity and selectivity. The identification of this tetrazole acting as a balanced dual-acting compound in human whole blood, along with SAR analysis of the synthesized lumiracoxib derivatives, might contribute to the rational design of a new class of cardioprotective anti-inflammatory agents.     

Aberrant distribution of junctional complex components in retinoic acid receptor alpha‐deficient mice

Retinoic acid receptor alpha (RARα)‐deficient mice are sterile, with abnormalities in the progression of spermatogenesis and spermiogenesis. In this study, we investigated whether defective retinoid signaling involved at least in part, disrupted cell–cell interactions. Hypertonic fixation approaches revealed defects in the integrity of the Sertoli‐cell barrier in the tubules of RARα‐deficient testes. Dye transfer experiments further revealed that coupling between cells from the basal to adluminal compartments was aberrant. There were also differences in the expression of several known retinoic acid (RA)‐responsive genes encoding structural components of tight junctions and gap junctions. Immunostaining demonstrated a delay in the incorporation of zonula occludens (ZO‐1), a peripheral component protein of tight junctions, into the Sertoli cell tight junctions. Markedly reduced expression of connexin‐40 in mutant pachytene spermatocytes and round spermatids was found by in situ hybridization. An ectopic distribution of vimentin and disrupted cyclic expression of vimentin, which is usually tightly regulated during spermiogenesis, was found in RARα‐deficient testes at all ages examined. Thus, the specific defects in spermiogenesis in RARα‐deficient testes may correlate with a disrupted cyclic expression of RA‐responsive structural components, including vimentin, a downregulation of connexin‐40 in spermatogenic cells, and delayed assembly of ZO‐1 into Sertoli cell tight junctions. Interestingly, bioinformatic analysis revealed that many genes that are components of tight junctions and gap junctions contained potential retinoic acid response element binding sites. Microsc. Res. Tech., 2010. © 2009 Wiley‐Liss, Inc.     

Novel mesoporous aluminosilicate supported palladium-rhodium catalysts for diesel upgrading: II. Catalytic activity and improvement of industrial diesel feedstocks

Bimetallic PdRh catalysts (molar ratio Pd/Rh = 1 and 2) were prepared by impregnation of a mesoporous aluminosilicate (molar ratio Si/Al = 10 and 20). These materials are destined to be used in industrial processes aiming to improve diesel quality by hydrogenation and ring-opening of aromatic components. The four catalysts were examined for their activity in hydrogenation of naphthalene and tetralin model feedstocks, at 6 MPa, including in the presence of sulfur containing compounds. The capacity of one of these catalysts to improve the quality of hydrogenated industrial light cycle oil containing ≤50 wt ppm of sulfur was evaluated in a pilot plant. In these industrial conditions, the catalyst has a higher catalytic activity at lower temperature than a reference state of-the-art catalyst, giving a seven-point improvement of the cetane number at 280–300 °C and with formation of less than 10% of non-selective cracking products.     

Synthesis and characterization of ratiometric ion-sensitive polyelectrolyte capsules

Micrometer-sized polyelectrolyte capsules are synthesized, which have ion-sensitive fluorophores embedded in their cavities. As the membranes of the capsules are permeable to ions, the fluorescence of the capsules changed with the ion concentration. In particular, capsules sensitive to protons, sodium, potassium, and chloride ions are fabricated and their fluorescence response analyzed. In order to allow for ratiometric measurements, additional fluorophores whose emission do not depend on the ion concentration and which emit a different wavelength are co-embedded in the capsule cavities.     

CuO/CeO2 supported on Zr doped SBA-15 as catalysts for preferential CO oxidation (CO-PROX)

The application of the catalytic system CuO/CeO₂ supported on Zr doped SBA-15 mesoporous silica to the preferential oxidation of CO on hydrogen streams (CO-PROX) suitable to be used to feed PEM fuel cells, has been studied. A loading of 20% (wt.) Ce and 6% (wt.) Cu was found optimal for the CO-PROX reaction. The influence of the presence of CO₂ and H₂O in the gas feed was also studied in order to simulate the real operation conditions of a PEMFC feed stream generated by alcohol steam reforming. The catalysts were characterized by XRD, adsorption-desorption of N₂ at −196 °C, TEM, -H₂-TPR and XPS. The system reducibility was found modified by the incorporation of zirconium in the support, with improvement of both the conversion and selectivity of the catalytic system, compared to the same material without Zr.     

New trends in the seafood market. Sutchi catfish (Pangasius hypophthalmus) fillets from Vietnam: Nutritional quality and safety aspects

Sutchi catfish (Pangasius hypophthalmus) produced in the freshwater basins of Vietnam, available on the Italian market as frozen or thawed fillets, were studied for their nutritional quality and safety aspects. Proximate composition, mineral content, fatty acid profile, unsaponifiable components of the lipid fraction and drip loss during thawing at 5 °C were determined on the fillets. Fillets were characterised by high moisture levels (80–85%) and low protein (12.6–15.6%) and lipid (1.1–3.0%) contents. Total lipids were characterised by low cholesterol levels (21–39 mg/100 g), high percentages of saturated fatty acids (41.1–47.8% of total fatty acid) and low percentages of polyunsaturated fatty acids (12.5–18.8% of total fatty acids), which were mainly represented by linoleic acid (44–59% of total polyunsaturated fatty acids). The mineral composition was characterised by a high sodium content (222–594 mg/100 g), probably partially due to the sodium tripolyphosphate (E 451) used to retain moisture. As regards safety aspects, the quality of the samples analysed was good, with low residue levels of mercury, organochlorine pesticides and polychlorinated biphenyls.     

Is agriculture connected with stunting in Indonesian children living in a rice surplus area? A case study in Demak regency,central Java

Central Java province plays the main role in the production of food for national stocks in Indonesia, in which Demak is one of the 35 Regencies. Demak Regency had the sixth highest rice productivity in 2013, but at the same time, the seventh highest percentage of child malnutrition. This paradox between high rice productivity and low nutritional status of children triggered an interest in analyzing the correlations between agricultural production of households in the Demak Regency and the prevalence of stunting of children under-five. In December 2014 to February 2015, a cross-sectional survey was carried out in three sub-districts in Demak (Karanganyar, Dempet and Gajah) having the highest rice production and at the same time poor nutritional status of under-five children. The oldest under-five children from farmer family backgrounds were selected. Data on general characteristics, anthropometry of the children, as well as household socio-economics, including agricultural characteristics were obtained. Of the 335 children, 31.9% of them were stunted. A higher proportion of households that grew rice solely or mainly for own consumption (62.4%) and had significantly smaller sized rice-fields (p = 0.041) had stunted rather than non-stunted children. In total, rice production, farm income and agriculture diversity of families with non-stunted children were not significantly different from those of stunted children. However, yearly expenditure for improving family health and environmental conditions were significantly higher among non-stunted than stunted children (p = 0.044). Family decisions about what to spend money on also seemed to influence the nutritional status of the children, rather than nutritional diversity or revenue from agriculture itself. Therefore, improvement of agricultural production and diversity should be accompanied by education on household expenditure.