Bis-triazolylchalcogenium-Functionalized Benzothiadiazole Derivatives as Light-up Sensors for DNA and BSA.

A range of bis-triazolylchalcogenium-BTD 3 was synthesized by a copper-catalyzed azide-alkyne cycloaddition of azido arylchalcogenides 1 and 4,7-diethynylbenzo[c][1,2,5]thiadiazole 2. Eight new compounds were obtained in moderate to good yields using 1 mol % of copper(II) acetate monohydrate under mild reaction conditions. In addition, the synthesized bis-triazolylchalcogenium-BTD 3a-3h were investigated regarding their photophysical, electrochemical, and biomolecule binding properties in solution. In general, compounds presented strong absorption bands at the 250-450 nm region and cyan to green emission properties. The redox process attributed to the chalcogen atom was observed by electrochemical analysis (CV techniques). In addition, spectroscopic studies by UV-vis, steady-state emission fluorescence, and molecular docking calculations evidenced the ability of each derivative to establish interactions with calf-thymus DNA (CT-DNA) and bovine serum albumin (BSA). The behavior presented for this new class of compounds makes them a promising tool as optical sensors for biomolecules.

The neurotherapeutic role of a selenium-functionalized quinoline in hypothalamic obese rats.

RATIONALE: Obesity is considered one of the major global health problems and increases the risk of several medical complications, such as diabetes and mental illnesses. OBJECTIVE: The present study investigated the effect of 7-chloro-4-(phenylselanyl) quinoline (4-PSQ) on obesity parameters, behavioral and neurochemical alterations in hypothalamic obese rats. METHODS: Male Wistar rats received subcutaneous neonatal injections of monosodium glutamate (MSG, 4g/kg) or saline. After the Lee Index evaluation, rats were divided into groups and treated with 4-PSQ (5 mg/kg, intragastric route) or canola oil once a day (post-natal days (PND) 60→76). Open-field, elevated plus-maze, forced swim task, object recognition/location memory, and stepdown inhibitory avoidance tasks were conducted from PND 66 to 74. On PND 76, rats were euthanized and epididymal fat, blood, cerebral cortex, andhippocampus were removed. Blood biochemical parameters and cortical/hippocampal acetylcholinesterase (AChE) and Na /K -ATPase activities were assessed. RESULTS: MSG increased the Lee Index characterizing the chemically induced hypothalamic obesity model. 4-PSQ reversed the increases of epididymal fat, blood glucose, and triglyceride levels caused by MSG exposure. 4-PSQ attenuated anxiety-like and depression-like behaviors induced by neonatal administrations of MSG. Memory deficits found in MSG-obese rats were reversed by treatment with 4-PSQ. Neurochemical alterations produced by MSG evidenced by stimulation ofNa+/K+-ATPase and AChE activities in the cerebral cortex and hippocampus of rats were normalized by 4-PSQ treatment. CONCLUSIONS: In brief, 4-PSQ therapy improved hypothalamic obesity-related parameters, as well as psychiatric symptoms, cognitive impairment, and neurochemical alterations found in obese rats.

Fluorescent Benzoselenadiazoles: Synthesis, Characterization, and Quantification of Intracellular Lipid Droplets and Multicellular Model Staining.

In this work, we described the synthesis of 10 new fluorescent 2,1,3-benzoselenadiazole small-molecule derivatives and their chemical- and photocharacterizations. The new derivatives could, for the first time, be successfully applied as selective live cell imaging probes (at nanomolar concentrations) and stained lipid-based structures preferentially. Density functional theory (DFT) calculations were used to help in understanding the photophysical data and the intramolecular charge-transfer (ICT) processes of the synthesized dyes. Some derivatives showed impressive cellular responses, allowing them to be tested as probes in a complex multicellular model (i.e., Caenorhabditis elegans). When compared with the commercially available dye, the new fluorescent compounds showed far better results both at the cellular level and inside the live worm. Inside the multicellular complex model, the tested probes also showed selectivity, a feature not observed when the commercial dye was used to carry out the bioimaging experiments.

The anxiolytic effect of a promising quinoline containing selenium with the contribution of the serotonergic and GABAergic pathways: Modulation of parameters associated with anxiety in mice.

Recently, we demonstrated the promising anxiolytic action of 7-chloro-4-(phenylselanyl) quinoline (4-PSQ) in mice. For this reason, the objective of this study was to expand our previous findings by investigating the contribution of serotoninergic and GABAergic systems to the anxiolytic action of this compound. Pretreatment with different serotoninergic antagonists (pindolol, WAY100635 and ketanserin) blocked the anxiolytic effect caused by 4-PSQ (50 mg/kg, per oral) in the elevated plus maze (EPM) test. The contribution of the GABAergic system was investigated by pretreatment with pentylenetetrazole (a GABAA receptor antagonist) (PTZ). 4-PSQ diminished the PTZ-induced anxiety, and did not modify the locomotor, exploratory and motor activities of mice. Later, this group of animals was euthanized and the blood was removed to determine the levels of corticosterone, and cerebral cortex and hippocampus to determine the mRNA expression levels of cAMP response element binding protein (CREB), brain derived neurotrophic factor (BDNF) and nuclear factor kappa B (NF-κB), as well as the Na+, K+ ATPase activity and reactive species (RS) levels. 4-PSQ was able to significantly reverse the increase in RS and corticosterone levels, as well as the decrease of CREB and BDNF expression in the cerebral structures and increase of NF-κB expression in the hippocampus. Finally, 4-PSQ restored the Na+, K+ ATPase activity in the cerebral structures evaluated. Here, we showed that the modulation of serotonergic and GABAergic systems, factors related to neurogenesis, oxidative status and Na+, K+ ATPase activity contributes to the anxiolytic effect of 4-PSQ and reinforces the therapeutical potential of this compound for the treatment of anxiety.

7-Chloro-4-(Phenylselanyl) Quinoline with Memory Enhancer Action in Aging Rats: Modulation of Neuroplasticity, Acetylcholinesterase Activity, and Cholesterol Levels.

This study investigated the effect of 7-chloro-4-(phenylselanyl) quinoline (4-PSQ) to restore the cognitive impairment caused by aging in male Wistar rats. Moreover, modulation of neuroplasticity markers, acetylcholinesterase (AChE) activity, and cholesterol levels was performed. Aged rats were intragastrically treated with 4-PSQ (5 mg/kg) for 7 days. Animals were tested in behavioral tasks, and then plasma (to determine cholesterol levels), hippocampus, and cerebral cortex (to determine neural cell adhesion molecule (NCAM) and polysialyltransferase (PST) levels, and AChE activity) were removed. Our findings demonstrated that treatment of aged rats with 4-PSQ restored short-term and long-term memories in the object recognition tests. 4-PSQ treatment did not restore exploratory activity (rearings) but partially restored locomotor activity (crossings) reduced by aging in the open-field test. Moreover, the compound restored the reduction in the NCAM and PST levels, and AChE activity in cerebral structures, as well as the increase in the plasma cholesterol levels, caused by aging in rats. In conclusion, 4-PSQ restored cognitive impairment caused by aging in rats by modulating synaptic plasticity, cholinergic system, and cholesterol levels.

Current advances of pharmacological properties of 7-chloro-4-(phenylselanyl) quinoline: Prevention of cognitive deficit and anxiety in Alzheimer's disease model.

This study investigated the effect of 7-chloro-4-(phenylselanyl) quinoline (4-PSQ) at a dose of 1 mg/kg in memory impairment and anxiety in an Alzheimer's disease (AD) model induced by amyloid ß-peptide (Aß) (fragment 25-35) in mice. The involvement of acetylcholinesterase (AChE) activity and lipid peroxidation in hippocampus and cerebral cortex was evaluated. Male Swiss mice were pretreated with 4-PSQ (1 mg/kg, intragastrically (i.g.), daily) for fourteen days. Thirty minutes after the first treatment with 4-PSQ, the animals received a single injection of Aß (3 nmol/3 µl/per site, intracerebroventricular (i.c.v.)). Mice were submitted to the behavioral tasks (open-field, elevated plus maze, Barnes maze, object recognition and location, and step-down inhibitory avoidance tests) from the fifth day onwards. On the fifteenth day, blood was removed for analysis of biochemical markers (glucose, triglycerides, urea, aspartate (AST) and alanine (ALT) aminotrasferases), and cerebral cortex and hippocampus for determination of AChE activity and thiobarbituric acid reactive species (TBARS) levels. Aß caused memory impairment, anxiogenic behavior, increased AChE activity in the cerebral structures and TBARS levels in the cerebral cortex. 4-PSQ was effective to protect against behavioral changes, AChE activity and TBARS levels. In conclusion, 4-PSQ protected against learning and memory impairment and anxiety in a mouse model of AD induced by Aß, and anticholinesterase and antioxidant actions are involved in the pharmacological effect of the compound.

Ação da enzima eectinase na extração do suco de jabtiicaba / Pectiase enzyme action in jabuticaba?s juice extraction

A enzima pectinase destaca-se pelo potencial de extração de sólidos solúveis presentes nas cascas de frutas. No caso da casca de jabuticaba, este fator é muito interessante, pois esta é rica em nutrientes e compostos que contribuem para o aumento da doçura e da cor. Assim, o objetivo deste trabalho foi realizar um estudo para avaliação da influência da adição da enzima pectinase na extração do suco de jabuticaba (Myrcia jabuticaba cauliflora Berg). Os efeitos foram observados por meio de análises físico-químicas (acidez, açúcares redutores e não redutores, anidrido sulfuroso livre e total, sólidos solúveis totais, concentração de polifenóis e antocianinas, pH e cinzas) e sensorial (teste de escala hedônica e escala de atributos) dos sucos elaborados com (T2) e sem a adição da enzima (T1). Os resultados mostraram diferença significativa entre as amostras, principalmente em relação à concentração de antocianinas e cinzas, ambos maiores em T2. Além disso, T2 apresentou maior rendimento (± 5%), coloração mais intensa e um suco mais límpido. Os resultados da análise sensorial mostraram diferença significativa no teste de escala hedônica e no atributo sabor, onde ambos apresentaram as médias de 5 em T1 e 6 em T2, o que corresponde respectivamente a ?não gostei, nem desgostei? e ?gostei ligeiramente?. Assim, comprovou-se que com a adição da enzima pectinase, melhorou o aspecto visual e sensorial, além da maior extração de composto de grande interesse para a saúde como as antocianinas e os minerais.

Pectinase enzyme stands out because of its soluble solid extraction potential found in fruit peels. In the case of jabuticaba peel, this factor is really interesting, because it is rich in nutrients and compounds that contribute to increase sweetness and color. Thus, the objective of this study was to evaluate the influence of pectinase enzyme in jabuticaba juice extraction (Myrcia jabuticaba cauliflora Berg). The effects were observed through physical and chemical analysis (acidity, reducing and non-reducing sugars, free and total sulfurous anhydride, total soluble solids, concentration of polyphenols and anthocyanins, pH and ashes) and sensory (hedonic scale test and range of attributes) from juices prepared with (T2) and with no enzyme addition (T1). The results have shown a meaningful difference among the samples, mainly in regarding anthocyanin concentration, and ashes, both higher in T2. Besides this, T2 had a bigger yield (± 5%), more intense coloring and clearer juice. The sensory analysis results showed meaningful difference in the hedonic scale test and in the flavor attribute where both presented the average of 5 in T1 and 6 in T2, respectively corresponding to ?I didn?t like it nor dislike it.? and ?I slightly liked it.?. Therefore, it was proven that with the addition of pectinase enzyme, the visual and sensory aspect improved, besides the bigger compound extraction which can be of interest for health as well as for anthocyanins and minerals.

Elaboração de barras de cereais com ingredientes alternativos e regionais do oeste do Paraná / Elaboration of cereal bars with alternative and regional ingredients from the western of Paraná

A tendência de consumir mais alimentos nutritivos, no lugar de doces e guloseimas tem levado ao aparecimento de novos tipos de produtos, tais como barras de cereais diversificadas. Dentro dos produtos a base de cereais, as barras podem fornecer importante suplementação de calorias e elementos nutritivos como lipídeos, fibras, proteínas, minerais e vitaminas. Uma alternativa que vem ganhando corpo desde o início da década de 1970 consiste no aproveitamento de resíduos (principalmente cascas e sementes), ou seja, o processo de fabricação de farinhas, a partir de certas frutas como matéria-prima para a produção de alguns alimentos perfeitamente passíveis de serem incluídos na alimentação humana. Desse modo, este trabalho teve por objetivo utilizar ingredientes alternativos na elaboração das barras de cereais, tornando estas mais nutritivas, com propriedades funcionais diversificadas e verificar a aceitabilidade desse produto. Foram desenvolvidas quatro diferentes tipos de barras de cereais com ingredientes alternativos e disponíveis na região, tais como: sementes de abóbora, melão e melancia, e farinha da casca de maracujá. Realizou-se análise sensorial das barras desenvolvidas por uma equipe orientada, para avaliação da aceitabilidade de cada uma das barras de cereais. Assim, determinou-se a composição centesimal de uma das barras por meio das análises físico-químicas de: lipídeos, carboidratos, fibras, minerais, umidade, proteínas e valor calórico. A barra de cereal formulada a partir de produtos alternativos, como sementes e casca de frutas, apresentou baixo valor calórico, apreciáveis quantidades de fibras e proteínas e baixo teor de lipídeos. Além disso, também apresentaram grande aceitabilidade; e devido à introdução de alimentos alternativos como sementes e casca de frutas, tornaram-se um produto mais nutritivo, e com propriedades funcionais diversificadas para serem consumidas diariamente, como lanches.

The tendency of consuming more nutritious food instead of sweets and candies led to the emergence of new sorts of products such as diverse cereal bars. Among the products made from cereals, bars can provide important supplemental calories and nutrients such as lipids, fiber, protein, minerals and vitamins. One alternative that has become popular since the beginning of the 1970s is the use of waste material (mainly peels and seeds), that is, the process of making flour from certain fruits as raw material for the production of some foods is perfectly likely to be included in food. This study aimed to use alternative ingredients in the preparation of cereal bars, making them more nutritious, with diverse functional properties and acceptability of the same. It was developed four different sorts of cereal bars with alternative ingredients and also available in the region, such as, pumpkin seeds, melon and watermelon, and passion?s peel flour. It was accomplished a sensory analysis of the developed bars by a team-oriented to evaluate the acceptability of each of the cereal bars. It was determined the chemical composition of one of the bars through the physical and chemical analysis of: lipids, carbohydrates, fiber, minerals, humidity, protein and calorific content. The cereal bar made from alternative products such as seeds and fruit?s peel, showed lower calorific value, greater amount of fiber and carbohydrates and less fat. The cereal bar presented great acceptability and because of the introduction of alternative food such as seeds and fruit?s peel, became a more nutritious product with functional diverse properties to be consumed daily as snacks.

Kinetics of solvent-free lipase-catalyzed glycerolysis of olive oil in surfactant system.

This work reports experimental data and kinetic modeling of solvent-free glycerolysis of olive oil using a commercial immobilized lipase (Novozym 435) in the presence of Triton X-100 surfactant for the production of monoacylglycerols (MAG) and diacylglycerols (DAG). The experiments were performed in batch mode evaluating the effects of temperature (30-70 degrees C), enzyme concentration (2.5-18 wt %), Triton X-100 concentration (10-20 wt %), and glycerol to oil molar ratio (3:1, 6:1, and 9:1). Experimental results showed that lipase-catalyzed solvent-free glycerolysis with the addition of Triton X-100 might be a potential alternative route to conventional organic solvent methods, as good conversions were obtained with relatively low enzyme concentrations (9 wt %) in short reaction times (240 min). The glycerolysis and hydrolysis parallel reactions were considered with rate constants estimated by minimizing a maximum likelihood function. A very satisfactory agreement between experimental data and model results was obtained, thus allowing a better understanding of the reaction kinetics.

Degradation of dimethyl disulfide using homogeneous Fenton's reaction.

In this work the degradation of a model odor compound (dimethyl disulfide, DMDS) using Fenton's reaction is reported. Dimethyl disulfide is present in wastewaters generated during production of poultry feather and viscera meal. Oxidation was carried out in batch reactor with temperature control. Experimental design technique was used to investigate the influence of concentration of hydrogen peroxide and Fe(2+), temperature and pH on degradation of DMDS. Control reactions using H(2)O(2) without Fe(2+) were carried out, but DMDS degradation could only reach 60% for a 0.025 mg L(-1) DMDS solution, at pH 3, 60 degrees C using 10,000 mg L(-1) H(2)O(2) in 30 min of reaction. The Fenton's reaction could effectively remove DMDS, reaching 95% degradation at pH 3, 60 degrees C, 5 mg L(-1) H(2)O(2) and 1 mg L(-1) Fe(2+) after only 10 min of contact. A kinetic study of the Fenton's reaction was carried out, varying the concentration of hydrogen peroxide, Fe(2+) and temperature.

Study of odor compounds in gaseous effluents generated during production of poultry feather and viscera meal using headspace solid phase microextraction.

This work reports the screening and characterization of odor compounds in gaseous effluents generated during the production of poultry feather and viscera meal, the by-products of the poultry meat industry. Chemical analysis was carried out by solid phase microextraction in the headspace (HS-SPME) mode. Exhaust air of thermal processing of poultry feather and viscera were sampled online from a bench-scale digester, condensed, and collected in sampling flasks. Both volatile and semivolatile organic compounds present in the condensed gases were extracted under agitation at constant temperature. The extracts were analyzed with a gas chromatograph coupled to a mass spectrometric detector (GC/MSD). The identification of compounds was carried out by comparing the mass spectra obtained with those from the Wiley library and quantification was accomplished through authentic analytical standards. For the determination of the best extraction conditions and analysis, extraction fibers of different coatings and polarities were tested: divinylbenzene/carboxen/polydimethyilsiloxane (DVB/CAR/PDMS), carbowax/divinylbenzene (CW/DVB), and polydimethylsiloxane (PDMS) and chromatography columns of different polarities: DB-WAX (polar) and DB-5 (nonpolar). The best extraction conditions and analysis of the compounds of interest were obtained by the use of the SPME fiber with DVB/CAR/PDMS coating and analysis by GC/MSD with polar capillary column. Several carboxylic acids were identified, as well as mercaptans, amines, and aldehydes of great environmental importance.