Lamellarin D bioconjugates I: synthesis and cellular internalization of PEG-derivatives

Herein is reported the design and synthesis of poly(ethylene glycol) derivatives of Lamellarin D with the aim of modulating their physicochemical properties, and improving the biological activity. Mono-, di- and tri-PEG conjugates with improved solubility were obtained in 18-57% overall yields from the corresponding partially protected phenolic derivatives of Lamellarin D. Conjugates 1-9 were tested in a panel of three human tumor cell lines (MDA-MB-231 breast, A-549 lung and HT-29 colon) to evaluate their cytotoxicity. Several compounds exhibited enhanced cellular internalization, and more than 85% of the derivatives showed a lower GI50 than Lam-D. Furthermore, cell cycle arrest at G2 phase, and apoptotic cell-death pathways were determined for Lamellarin D and these derivatives.

Lamellarin D bioconjugates II: synthesis and cellular internalization of dendrimer and nuclear location signal derivatives

The design and synthesis of Lamellarin D conjugates with a nuclear localization signal peptide and a poly(ethylene glycol)-based dendrimer are described. Conjugates 1-4 were obtained in 8-84% overall yields from the corresponding protected Lamellarin D. Conjugates 1 and 4 are 1.4 to 3.3-fold more cytotoxic than the parent compound against three human tumor cell lines(MDA-MB-231 breast, A-549 lung, and HT-29 colon). Besides, conjugates 3, 4 showed a decrease in activity potency in BJ skin fibroblasts, a normal cell culture. Cellular internalization was analyzed and nuclear distribution pattern was observed for 4, which contains a nuclear localization signalling sequence.

Lamellarin D bioconjugates I: synthesis and cellular internalization of PEG-derivatives

Herein is reported the design and synthesis of poly(ethylene glycol) derivatives of Lamellarin D with the aim of modulating their physicochemical properties, and improving the biological activity. Mono-, di- and tri-PEG conjugates with improved solubility were obtained in 18-57% overall yields from the corresponding partially protected phenolic derivatives of Lamellarin D. Conjugates 1-9 were tested in a panel of three human tumor cell lines (MDA-MB-231 breast, A-549 lung and HT-29 colon) to evaluate their cytotoxicity. Several compounds exhibited enhanced cellular internalization, and more than 85% of the derivatives showed a lower GI50 than Lam-D. Furthermore, cell cycle arrest at G2 phase, and apoptotic cell-death pathways were determined for Lamellarin D and these derivatives.

Synthesis and antitumor activity of mechercharmycin A analogues

Several analogs of the cytotoxic thiopeptide IB-01211 or Mechercharmycin A (1) have been synthetized. The cytotoxicity of 1 and the synthetized analogs was evaluated against a panel of three human tumor cell lines. Thiopeptide 1 and the most active derivatives, 2 and 3c, were chosen for further studies like effects on cell cycle progression and induction of apoptosis. Interestingly, the inhibition of cell division and activation of a programmed cell death by apoptosis was detected.

Oxidações catalíticas e eletrocatalíticas de substratos orgânicos. O cério como oxidante

This paper reviews the catalytic and electrocatalytic oxidation of organic compounds using cerium (IV) salts. Direct and indirect methods and those using modified electrodes are described.

Guercino (1591-1666). Capolavori da Cento e da Roma

Un dels molts actes amb què la ciutat de Roma ha celebrat els 150 anys de la unificació d"Itàlia (1861˗2011) ha estat la presentació oficial del complex i acurat procés de restauració del Palazzo Barberini (1625˗1633). Restauració de l"edifici i, alhora, reestructuració de l"espai expositiu i del discurs museogràfic de la Galleria Nazionale di Arte Antica, dirigit tot per Rossella Vodret, reconeguda historiadora de l"art i Soprintendente per il Patrimonio Storico Artistico e del Polo Museale di Roma.

Tratamento de efluentes industriais por processos oxidativos na presença de ozônio

A large variety of organic and inorganic compounds may be found in wastewater which can contribute to environmental contamination. Oxidation processes with ozone (O3; O3/UV; O3/H2O2; O3/TiO2; O3/Mn+2) and the use of ozone in the pre- or post-treatment of wastewater combined with biological processes has been extensively studied for the treatment of effluents. The aim of this work was to evaluate the potential of the ozonation process in the treatment of several industrial wastewaters, namely effluents from paper mills, and textile, whey (dairy industry), pharmaceutic sand pesticides plants.

L’Inventari de recursos turístics a l’àmbit local: metodologia per a l’inventari dels recursos naturals i culturals per a la Carta Europea de Turisme Sostenible al Parc Natural del Montseny

El present projecte neix de la proposta facilitada per l’Oficina del Parc Natural del Montseny en relació a les accions a portar a terme dins els compromisos de la Carta Europea de Turisme Sostenible (CETS) al parc durant els anys 2011-2015. Es dissenya una metodologia a portar a terme per a l’elaboració de l’inventariat dels recursos turístics, naturals i culturals, dins dels municipis que engloben el territori de la Carta. Així mateix, aquest projecte pretén ser una eina útil, no només per a la catalogació dels recursos, sinó també per a la jerarquització d’aquests en termes de potencial turístic

Experiencia interdisciplinar de coevaluación: la percepción de los estudiantes en la Universidad de Girona : percepciones sobre la coevaluación

Peer-assessment provides multiple benefits to students during their learning process. The aim of this study is to examine students’ perception regarding peer-assessment. Surveys have been conducted before and after the peer-assessment process to students from five different subjects taught at the University of Girona. The results suggest that students have a positive predisposition respect to this methodology, both before and after being implemented. However, we found slight differences between the students of the technical field compared to those in education science

Nivel de calidad de los medicamentos elaborados por los alumnos en el laboratorio de prácticas y de su control como producto acabado por parte de los mismos alumnos

Una de las prácticas de laboratorio de Tecnología Farmacéutica requiere la elaboración de comprimidos en la asignatura de Farmacia Galénica II siguiendo el mismo flujo de fabricación al empleado en la industria farmacéutica (pesada, tamización, mezclado, amasado, granulación, secado, mezclado y compresión). Estos comprimidos se analizan en la asignatura de Farmacia Galénica III (entre 6 y 12 meses más tarde) por los mismos alumnos según las directrices de la Real Farmacopea Española.En el trabajo se exponen gráficamente los resultados hallados y se comentan los principales puntos de mejora ya que el producto elaborado no es conforme en la mayoría de los casos (sólo alrededor del 50% de los productos elaborados por los alumnos podrían ser conformes, aún siendo un proceso validado). Realmente, la experiencia de los operadores es el punto más crítico que influye en los resultados de estos lotes de comprimidos, sobre todo en el laboratorio analítico. Esta hipótesis ha sido confirmada en lotes analizados por el personal cualificado del departamento de control de calidad del Servei de Desenvolupament del Medicament de la Facultat de Farmàcia de la Universitat de Barcelona, ya que en todos los casos los resultados obtenidos fueron más exactos, repetitivos y cercanos a los teóricos.

Comportamento do herbicida hexazinone em área de recarga do aqüífero Guarani cultivada com cana-de-açúcar

São Paulo state (Brazil) has an important area of sugarcane production, mainly for obtaining alcohol and sugar, where there is an intensive use of pesticides. An important recharge zone of Guarani aquifer, with supplies water for the local population, is located at Ribeirão Preto city, so the local behavior of pesticides must be investigated. The GUS index was obtained by using the paramenters Koc and half-life for hezazinone herbicide, determinated in representative soil of this region. This study has demonstrated that there is potential risks of hexazinone leaching to ground water, indicating that this herbicide must be monitored in ground water.

Validação de método multirresíduo para determinação de pesticidas em alimentos empregando QuEChERS E UPLC-MS/MS

This paper presents a practical and rapid method which was validated for simultaneous quantification and confirmation of 29 pesticides in fruits and vegetables using ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS). The samples were extracted following the method known as QuEChERS. Using the developed chromatographic conditions, the pesticides can be separated in less than 9 min. Two multiple reaction monitoring (MRM) assays were used for each pesticide. Four representative matrices (lettuce, tomato, apple and grapes) were selected to investigate the effect in recoveries and precision. Typical recoveries ranged from 70-120%, with relative standard deviation (RSDs) lower than 20%.

Derivative spectrophotometric method for determination of acyclovir in polymeric nanoparticles

A derivative spectrophotometric method was validated for quantification of acyclovir in poly (n-butylcyanoacrylate) (PBCA) nanoparticles. Specificity, linearity, precision, accuracy, recovery, detection (LOD) and quantification (LOQ) limits were established for method validation. First-derivative at 295.2 nm eliminated interferences from nanoparticle ingredients and presented linearity for acyclovir concentrations ranging from 1.25 to 40.0 µg/mL (r = 0.9999). Precision and accuracy data demonstrated good reproducibility. Recovery ranged from 99.3 to 101.2. LOD was 0.08 µg/mL and LOQ, 0.25 µg/mL. Thus, the proposed method proved to be easy, low cost, and accurate, and therefore, an useful alternative to quantify acyclovir in nanoparticles.

Etiologia da podridão do coleto de Brachiaria brizantha em pastagens da amazônia

Desde 1995, pastos formados com Brachiaria brizantha cv. Marandu vêm sendo devastados por uma doença cujo sintoma típico é a morte de touceiras. Das amostras de plantas coletadas nos municípios de Paragominas (PA), Carutapera (MA) e Araguaína (TO), exibindo sintomas iniciais da doença, bem como, de sementes obteve-se quatro isolados de Pythium spp. e um de Rhizoctonia solani associados aos tecidos doentes. Os resultados dos testes de patogenicidade comprovaram que o principal agente da podridão do coleto do capim-braquiarão é Pythium periilum. A infestação do solo com mistura de inóculo dos três isolados de P. periilum e de R. solani resultou em elevada quantidade de doença (p<0,01). Na presença de alta população de R. solani, no solo, a associação desses patógenos deverá aumentar as áreas degradadas de pasto de capim-braquiarão, principalmente aquelas manejadas de modo inadequado, desde que R. solani é um reconhecido patógeno de B. brizantha. Trata-se do primeiro registro de P. periilum como agente primário de doença, em coleto de B. brizantha.

O autor de si mesmo: Machado de Assis leitor de Schopenhauer

Esse texto tem por objetivo mostrar que Machado de Assis construiu a crônica "O autor de si mesmo" fazendo uso da metafísica do amor de Schopenhauer.