Organocatalytic enamine-azide [3 + 2] cycloadditions between β-keto sulfones and aryl azides can be performed at room temperature in good to excellent yields of products in the presence of catalytic amounts of pyrrolidine (5 mol %). The proposed organocatalytic methodology was found to be applicable to β-keto arylsulfones containing a range of substituents. A wide variety of aryl azides also work. Basically, this constitutes a remarkably efficient protocol for the synthesis of novel 1,2,3-triazole compounds.

Bufadienolides are structurally related to the clinically relevant cardenolides (e.g., digoxin) and are now considered as endogenous steroid hormones. Binding of ouabain to Na(+)-K(+)-ATPase has been associated, in kidney cells, to the activation of the Src kinase pathway and Na(+)-K(+)-ATPase internalization. Nevertheless, whether the activation of this cascade also occurs with other cardiotonic steroids and leads to diuresis and natriuresis in the isolated intact kidney is still unknown. In the present work, we perfused rat kidneys for 120 min with bufalin (1, 3, or 10 μM) and measured its vascular and tubular effects. Thereafter, we probed the effect of 10 μM 3-(4-chlorophenyl)1-(1,1-dimethylethyl)-1H-pyrazolo[3,4-d]pyrimidin-4amine (PP2), a Src family kinase inhibitor, and 1,4-diamino-2,3-dicyano-1,4-bis[2-aminophenylthio] butadiene (UO126), a highly selective inhibitor of both MEK1 and MEK2, on bufalin-induced renal alterations. Bufalin at 3 and 10 μM profoundly increased several parameters of renal function in a time- and/or concentration-dependent fashion. At a concentration that produced similar inhibition of the rat kidney Na(+)-K(+)-ATPase, ouabain had a much smaller diuretic and natriuretic effect. Although bufalin fully inhibited the rat kidney Na(+)-K(+)-ATPase in vitro, its IC(50) (33 ± 1 μM) was threefold higher than the concentration used ex vivo and all its renal effects were blunted by PP2 and UO126. Furthermore, the phosphorylated (activated) ERK1/2 expression was increased after bufalin perfusion and this effect was totally prevented after PP2 pretreatment. The present study shows for the first time the direct diuretic, natriuretic, and kaliuretic effects of bufalin in isolated rat kidney and the relevance of Na(+)-K(+)-ATPase-mediated signal transduction.

PURPOSE:To address the effects of fructooligosaccharides (FOS) intake on serum cholesterol levels. METHODS:We performed a search for scientific articles in MEDLINE database from 1987 to 2014, using the following English keywords: fructooligosaccharides; fructooligosaccharides and cholesterol. A total of 493 articles were found. After careful selection and exclusion of duplicate articles 34 references were selected. Revised texts were divided into two topics: "FOS Metabolism" and "FOS effects on plasma cholesterol." RESULTS:The use of a FOS diet prevented some lipid disorders and lowered fatty acid synthase activity in the liver in insulin-resistant rats. There was also reduction in weight and total cholesterol in beagle dogs on a calorie-restricted diet enriched with short-chain FOS. Another study found that 2g FOS daily consumption increased significantly serum HDL cholesterol levels but did not ensure a significant reduction in levels of total cholesterol and triglycerides.. Patients with mild hypercholesterolemia receiving short-chain FOS 10.6g daily presented no statistically significant reduction in serum cholesterol levels. However, when FOS was offered to patients that changed their lifestyle, the reduction of LDL cholesterol and steatosis was higher. CONCLUSIONS:Fructooligosaccharides intake may have a beneficial effect on lipid metabolism and regulation of serum cholesterol levels in individuals that change their lifestyle. FOS supplementation use in diets may therefore be a strategy for lowering cholesterol.

PURPOSE:To identify the current status of scientific knowledge in fructo-oligosaccharides (FOS), non-conventional sugars that play an important role in glycemia control. METHODS:We performed a search for scientific articles in MEDLINE and LILACS databases, from January 1962 to December 2011, using English/Portuguese key words: "blood glucose/glicemia", "prebiotics/prebióticos" and "dietary fiber/fibras na dieta". From an initial number of 434 references, some repeated, 43 references published from 1962 to 2011 were included in this study. The selected texts were distributed in three topics: (1) metabolism of FOS, (2) FOS and experimental studies involving glucose and (3) human studies involving glucose and FOS. RESULTS:Five studies have shown that the use of FOS reduces the fecal content and increases intestinal transit time. Experimental studies have shown that dietary supplementation with high doses (60 g/Kg) of propionate, a short-chain fatty acid decreased glycemia.The use of lower doses (3 g/kg) did not produce the same results. Study in subjects with diabetes type II showed that the addition of 8 grams of FOS in the diet for 14 days, caused a reduction in serum glucose. In another study with healthy subjects, there were no changes in glycemic control. CONCLUSIONS:This review demonstrates that consumption of FOS has a beneficial influence on glucose metabolism. The controversies appear to be due to inadequate methodological designs and/or the small number of individuals included in some studies.Key words: Review. Blood Glucose. Oligosaccharides. Prebiotics. Dietary Fiber. RESUMO OBJETIVO:Conhecer o estado atual do conhecimento científico em fructooligossacarídeos (FOS), açúcares não-convencionais que desempenham um papel importante no controle da glicemia. MÉTODOS: Realizamos uma busca de artigos científicos nas bases de dados MEDLINE e Literatura Latino-Americana e do Caribe emCiências da Saúde (LILACS), a partir de janeiro 1962 a dezembro de 2011, usando como descritores termos Português/Inglês: "glicemia/ blood glucose, "prebióticos/prebiotics" e "fibras na dieta/dietary fiber. A partir de um número inicial de 434 referências, algumas repetidas, 43 referências foram consideradas adequadas para a finalidade deste estudo e foram, portanto, selecionadas para análise. Os textos selecionados foram distribuídos em três tópicos: (1) metabolismo de FOS (2), FOS e estudos experimentais envolvendo glicose e (3) estudos em humanos envolvendo glicose e FOS. RESULTADOS: Cinco trabalhos mostraram que o uso de FOS diminui o conteúdo fecal e aumenta o tempo do transito intestinal.Estudos experimentais demonstraram que a suplementação dietética com altas doses (60 g/Kg) de propionato, um ácido graxo de cadeia curta, diminuiu a glicemia. A utilização de doses menores (3 g/Kg) não produziu os mesmos resultados. Em indivíduos diabéticos tipo II a adição de 8 g de FOS na dieta, durante 14 dias, induziu uma redução da glicemia. Em indivíduos sadios, não ocorreram alterações da glicemia. CONCLUSÕES:Essa revisão mostra...

A simple method for the direct mono- and bis-organylselenylation of N-substituted pyrroles through a multicomponent reaction promoted by ultrasonic radiation was described. These sonochemical promoted reactions were performed between different primary amines, 2,5-hexanedione and dialkyl, diheteroaryl, or diaryl diselenides, using catalytic amounts of copper iodide. Depending on the amount of copper iodide and diorganyl diselenide used in the reactions, mono- or bis-organylselenylation products were efficiently synthesized in high yields.

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