995 resultados para pharmacological properties


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The replacement of conventional synthetic films and coatings by biodegradable alternatives reduces the use of non-renewable resources and waste disposal problems. Considering that Portugal is a major producer of leather, and consequently a large producer of related wastes, in this research, bovine hair was tested for the production of biodegradable films directly by thermo-compression, allowing waste valorisation and reduction of environmental pollution. The aim of this study was to determine the influence of the different pre-treatments performed by two processes (removal by mechanical action and removal by chemical process), applied to bovine hair, in order to obtain a biodegradable film with appropriate properties. Mechanical properties for these films were evaluated, namely strain at break, stress at break and Young modulus. Additionally colour, solubility and swelling in water were also studied. The mechanical removal hair only produced films with Na2S treatment. Chemical removed hair (immunization) depends of the pre-treatment and the degreasing with petroleum ether or sodium sulphide pre-treatment leads better mechanical properties. The results obtained indicated that the pre-treatments have an important role in the final properties of biodegradable films.

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In order to overcome the problems associated with low water solubility, and consequently low bioavailability of active pharmaceutical ingredients (APIs), herein we explore a modular ionic liquid synthetic strategy for improved APIs. Ionic liquids containing l-ampicillin as active pharmaceutical ingredient anion were prepared using the methodology developed in our previous work, using organic cations selected from substituted ammonium, phosphonium, pyridinium and methylimidazolium salts, with the intent of enhancing the solubility and bioavailability of l-ampicillin forms. In order to evaluate important properties of the synthesized API-ILs, the water solubility at 25 °C and 37 °C (body temperature) as well as octanol–water partition coefficients (Kow's) and HDPC micelles partition at 25 °C were measured. Critical micelle concentrations (CMC's) in water at 25 °C and 37 °C of the pharmaceutical ionic liquids bearing cations with surfactant properties were also determined from ionic conductivity measurements.

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IBD is a gastro-intestinal disorder marked with chronic inflammation of intestinal epithelium, damaging mucosal tissue and manifests into several intestinal and extra-intestinal symptoms. Currently used medical therapy is able to induce and maintain the patient in remission, however no modifies or reverses the underlying pathogenic mechanism. The research of other medical approaches is crucial to the treatment of IBD and, for this, it´s important to use animal models to mimic the characteristics of disease in real life. The aim of the study is to develop an animal model of TNBS-induced colitis to test new pharmacological approaches. TNBS was instilled intracolonic single dose as described by Morris et al. It was administered 2,5% TNBS in 50% ethanol through a catheter carefully inserted into the colon. Mice were kept in a Tredelenburg position to avoid reflux. On day 4 and 7, the animals were sacrificed by cervical dislocation. The induction was confirmed based on clinical symptoms/signs, ALP determination and histopathological analysis. At day 4, TNBS group presented a decreased body weight and an alteration of intestinal motility characterized by diarrhea, severe edema of the anus and moderate morbidity, while in the two control groups weren’t identified any alteration on the clinical symptoms/signs with an increase of the body weight. TNBS group presented the highest concentrations of ALP comparing with control groups. The histopathology analysis revealed severe necrosis of the mucosa with widespread necrosis of the intestinal glands. Severe hemorrhagic and purulent exsudates were observed in the submucosa, muscular and serosa. TNBS group presented clinical symptoms/signs and histopathological features compatible with a correct induction of UC. The peak of manifestations became maximal at day 4 after induction. This study allows concluding that it’s possible to develop a TNBS induced colitis 4 days after instillation.

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OBJECTIVE: To translate the Need for Recovery Scale (NFR) into Brazilian Portuguese and culturally adapt it and assess the stability, internal consistency and convergent validity of the Brazilian scale among industrial workers. METHODS: The translation process followed the guidelines for cultural adaptation of questionnaires including the steps of translation, synthesis, back translation, expert committee review, and pre-testing. The Brazilian Portuguese NFR, final version (Br-NFR) was assessed for stability (n=52) and internal consistency (n=192) and for convergent validity through simultaneous assessment with other instruments: the Borg Scale (n=59); the Chalder Fatigue Questionnaire (n=57) and 3 subscales of the SF-36 (n=56). RESULTS: Stability and internal consistency met the criterion for a reliable measure (ICC=0.80 and Cronbach's alpha =0.87, respectively). The convergent validity between Br-NFR and other instruments also showed good results: Borg Scale (r= 0.64); Chalder Questionnaire (r= 0.67); SF-36 subscales: vitality (r= -0.84), physical functioning (r= -0.54), and role-physical (r= -0.47). CONCLUSIONS: The Br-NFR proved to be a reliable instrument to evaluate work-related fatigue symptoms in industrial workers. Furthermore, it showed significant and good correlations with well-established instruments such as the Borg Scale, the Chalder Questionnaire and SF-36 vitality subscale, supporting the validity of the Br-NFR.

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Agência Financiadora - Fundação para a Ciência e Tecnologia - PTDC/CTM NAN/113021/2009

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The oceans remain a major source of natural compounds with potential in pharmacology. In particular, during the last few decades, marine cyanobacteria have been in focus as producers of interesting bioactive compounds, especially for the treatment of cancer. In this study, the anticancer potential of extracts from twenty eight marine cyanobacteria strains, belonging to the underexplored picoplanktonic genera, Cyanobium, Synechocystis and Synechococcus, and the filamentous genera, Nodosilinea, Leptolyngbya, Pseudanabaena and Romeria, were assessed in eight human tumor cell lines. First, a crude extract was obtained by dichloromethane:methanol extraction, and from it, three fractions were separated in a Si column chromatography. The crude extract and fractions were tested in eight human cancer cell lines for cell viability/toxicity, accessed with the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) and lactic dehydrogenase release (LDH) assays. Eight point nine percent of the strains revealed strong cytotoxicity; 17.8% showed moderate cytotoxicity, and 14.3% assays showed low toxicity. The results obtained revealed that the studied genera of marine cyanobacteria are a promising source of novel compounds with potential anticancer activity and highlight the interest in also exploring the smaller filamentous and picoplanktonic genera of cyanobacteria.

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In life cycle impact assessment (LCIA) models, the sorption of the ionic fraction of dissociating organic chemicals is not adequately modeled because conventional non-polar partitioning models are applied. Therefore, high uncertainties are expected when modeling the mobility, as well as the bioavailability for uptake by exposed biota and degradation, of dissociating organic chemicals. Alternative regressions that account for the ionized fraction of a molecule to estimate fate parameters were applied to the USEtox model. The most sensitive model parameters in the estimation of ecotoxicological characterization factors (CFs) of micropollutants were evaluated by Monte Carlo analysis in both the default USEtox model and the alternative approach. Negligible differences of CFs values and 95% confidence limits between the two approaches were estimated for direct emissions to the freshwater compartment; however the default USEtox model overestimates CFs and the 95% confidence limits of basic compounds up to three orders and four orders of magnitude, respectively, relatively to the alternative approach for emissions to the agricultural soil compartment. For three emission scenarios, LCIA results show that the default USEtox model overestimates freshwater ecotoxicity impacts for the emission scenarios to agricultural soil by one order of magnitude, and larger confidence limits were estimated, relatively to the alternative approach.

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A dc magnetron sputtering-based method to grow high-quality Cu2ZnSnS4 (CZTS) thin films, to be used as an absorber layer in solar cells, is being developed. This method combines dc sputtering of metallic precursors with sulfurization in S vapour and with post-growth KCN treatment for removal of possible undesired Cu2−xS phases. In this work, we report the results of a study of the effects of changing the precursors’ deposition order on the final CZTS films’ morphological and structural properties. The effect of KCN treatment on the optical properties was also analysed through diffuse reflectance measurements. Morphological, compositional and structural analyses of the various stages of the growth have been performed using stylus profilometry, SEM/EDS analysis, XRD and Raman Spectroscopy. Diffuse reflectance studies have been done in order to estimate the band gap energy of the CZTS films. We tested two different deposition orders for the copper precursor, namely Mo/Zn/Cu/Sn and Mo/Zn/Sn/Cu. The stylus profilometry analysis shows high average surface roughness in the ranges 300–550 nm and 230–250 nm before and after KCN treatment, respectively. All XRD spectra show preferential growth orientation along (1 1 2) at 28.45◦. Raman spectroscopy shows main peaks at 338 cm−1 and 287 cm−1 which are attributed to Cu2ZnSnS4. These measurements also confirm the effectiveness of KCN treatment in removing Cu2−xS phases. From the analysis of the diffuse reflectance measurements the band gap energy for both precursors’ sequences is estimated to be close to 1.43 eV. The KCN-treated films show a better defined absorption edge; however, the band gap values are not significantly affected. Hot point probe measurements confirmed that CZTS had p-type semiconductor behaviour and C–V analysis was used to estimate the majority carrier density giving a value of 3.3 × 1018 cm−3.

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OBJECTIVE: To develop an instrument to assess discrimination effects on health outcomes and behaviors, capable of distinguishing harmful differential treatment effects from their interpretation as discriminatory events. METHODS: Successive versions of an instrument were developed based on a systematic review of instruments assessing racial discrimination, focus groups and review by a panel comprising seven experts. The instrument was refined using cognitive interviews and pilot-testing. The final version of the instrument was administered to 424 undergraduate college students in the city of Rio de Janeiro, Southeastern Brazil, in 2010. Structural dimensionality, two types of reliability and construct validity were analyzed. RESULTS: Exploratory factor analysis corroborated the hypothesis of the instrument's unidimensionality, and seven experts verified its face and content validity. The internal consistency was 0.8, and test-retest reliability was higher than 0.5 for 14 out of 18 items. The overall score was higher among socially disadvantaged individuals and correlated with adverse health behaviors/conditions, particularly when differential treatments were attributed to discrimination. CONCLUSIONS: These findings indicate the validity and reliability of the instrument developed. The proposed instrument enables the investigation of novel aspects of the relationship between discrimination and health.

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In this work, we show a set of growth conditions, for the two step process, with which the growth of CZTSe is successful and reproducible. The properties of the best CTZSe thin films grown by this method were examined by SEM/EDS, XRD, Raman scattering, AFM/EFM, transmittance and reflectance measurements, photoluminescence (PL) measurements and hot point probe. A broad emission band was observed in the photoluminescence spectrum of the CZTSe thin film. The band gap energy was estimated to be around 1.05 eV at room temperature, using the transmittance and reflectance data, and CZTSe samples show p-type conductivity with the hot point probe. The different characterization techniques show that we could grow single phase CZTSe thin films with our optimized process conditions.

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Cu2ZnSnS4 is a promising semiconductor to be used as absorber in thin film solar cells. In this work, we investigated optical and structural properties of Cu2ZnSnS4 thin films grown by sulphurization of metallic precursors deposited on soda lime glass substrates. The crystalline phases were studied by X-ray diffraction measurements showing the presence of only the Cu2ZnSnS4 phase. The studied films were copper poor and zinc rich as shown by inductively coupled plasma mass spectroscopy. Scanning electron microscopy revealed a good crystallinity and compactness. An absorption coefficient varying between 3 and 4×104cm−1 was measured in the energy range between 1.75 and 3.5 eV. The band gap energy was estimated in 1.51 eV. Photoluminescence spectroscopy showed an asymmetric broad band emission. The dependence of this emission on the excitation power and temperature was investigated and compared to the predictions of the donor-acceptor-type transitions and radiative recombinations in the model of potential fluctuations. Experimental evidence was found to ascribe the observed emission to radiative transitions involving tail states created by potential fluctuations.

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The main purpose of this work is to present and to interpret the change of structure and physical properties of tantalum oxynitride (TaNxOy) thin films, produced by dc reactive magnetron sputtering, by varying the processing parameters. A set of TaNxOy films was prepared by varying the reactive gases flow rate, using a N2/O2 gas mixture with a concentration ratio of 17:3. The different films, obtained by this process, exhibited significant differences. The obtained composition and the interpretation of X-ray diffraction results, shows that, depending on the partial pressure of the reactive gases, the films are: essentially dark grey metallic, when the atomic ratio (N + O)/Ta < 0.1, evidencing a tetragonal β-Ta structure; grey-brownish, when 0.1 < (N + O)/Ta < 1, exhibiting a face-centred cubic (fcc) TaN-like structure; and transparent oxide-type, when (N + O)/Ta > 1, evidencing the existence of Ta2O5, but with an amorphous structure. These transparent films exhibit refractive indexes, in the visible region, always higher than 2.0. The wear resistance of the films is relatively good. The best behaviour was obtained for the films with (N + O)/Ta ≈ 0.5 and (N + O)/Ta ≈ 1.3.

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Hydroxycinnamic acids (HCAs) are important phytochemicals possessing significant biological properties. Several investigators have studied in vitro antioxidant activity of HCAs in detail. In this review, we have gathered the studies focused on the structure-activity relationships (SARs) of these compounds that have used medicinal chemistry to generate more potent antioxidant molecules. Most of the reports indicated that the presence of an unsaturated bond on the side chain of HCAs is vital to their activity. The structural features that were reported to be of importance to the antioxidant activity were categorized as follows: modifications of the aromatic ring, which include alterations in the number and position of hydroxy groups and insertion of electron donating or withdrawing moieties as well as modifications of the carboxylic function that include esterification and amidation process. Furthermore, reports that have addressed the influence of physicochemical properties including redox potential, lipid solubility and dissociation constant on the antioxidant activity were also summarized. Finally, the pro-oxidant effect of HCAs in some test systems was addressed. Most of the investigations concluded that the presence of ortho-dihydroxy phenyl group (catechol moiety) is of significant importance to the antioxidant activity, while, the presence of three hydroxy groups does not necessarily improve the activity. Optimization of the structure of molecular leads is an important task of modern medicinal chemistry and its accomplishment relies on the careful assessment of SARs. SAR studies on HCAs can identify the most successful antioxidants that could be useful for management of oxidative stress-related diseases.

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Modern real-time systems, with a more flexible and adaptive nature, demand approaches for timeliness evaluation based on probabilistic measures of meeting deadlines. In this context, simulation can emerge as an adequate solution to understand and analyze the timing behaviour of actual systems. However, care must be taken with the obtained outputs under the penalty of obtaining results with lack of credibility. Particularly important is to consider that we are more interested in values from the tail of a probability distribution (near worst-case probabilities), instead of deriving confidence on mean values. We approach this subject by considering the random nature of simulation output data. We will start by discussing well known approaches for estimating distributions out of simulation output, and the confidence which can be applied to its mean values. This is the basis for a discussion on the applicability of such approaches to derive confidence on the tail of distributions, where the worst-case is expected to be.

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A recent trend in distributed computer-controlled systems (DCCS) is to interconnect the distributed computing elements by means of multi-point broadcast networks. Since the network medium is shared between a number of network nodes, access contention exists and must be solved by a medium access control (MAC) protocol. Usually, DCCS impose real-time constraints. In essence, by real-time constraints we mean that traffic must be sent and received within a bounded interval, otherwise a timing fault is said to occur. This motivates the use of communication networks with a MAC protocol that guarantees bounded access and response times to message requests. PROFIBUS is a communication network in which the MAC protocol is based on a simplified version of the timed-token protocol. In this paper we address the cycle time properties of the PROFIBUS MAC protocol, since the knowledge of these properties is of paramount importance for guaranteeing the real-time behaviour of a distributed computer-controlled system which is supported by this type of network.