Desenvolupament d'una metodologia per a la millora de les recomanacions en la fertilització nitrogenada dels cereals d'hivern. (II) Cereals d'hivern a les comarques de Barcelona i Girona

Es van realitzar un seguit d’assaigs de fertilització nitrogenada a les comarques de Girona i Barcelona, generalment més humides que les àrees on es van realitzar els assaigs per Sió et al., en aquest mateix volum. Els mètodes assajats van ser els del nitrogen mineral al sòl i el del contingut de nitrats a la base de les tiges (CNSBT). Per al conjunt de sòls i situacions contenido de nitratos en la base de los assajades el mètode del nitrogen mineral s'ha mostrat com una eina molt adequada per planificar l’adobat de cobertora. El mètode del CNSBT també es revela com una eina útil, especialment per a les situacions en què el cultiu té suficient nitrogen disponible al sòl; en altres tot i la seva relació amb el N mínim hi ha casos en què dóna resultats contradictoris que requereixen més recerca .

Características hidráulicas y geomorfológicas de ríos de montaña (II)

En el primer artículo, de una serie de tres destinados a una síntesis del estado del conocimiento acerca de la hidráulica y la geomorfología fluvial que se desarrollan en ríos de montaña, se puso de manifiesto el papel absolutamente determinante de las cuencas montanas en los recursos hídricos mundiales. Asimismo, se describieron los rasgos definitorios de las tres categorías de flujo consideradas en cauces de montaña en función de la concentración del sedimento transportado (de baja concentración, hiperconcentrado y lava torrencial). En este segundo artículo se exponen las principales características hidráulicas del flujo de baja concentración de sedimento.

How hard is a commercial puzzle: the eternity II challenge

Recently, edge matching puzzles, an NP-complete problem, have received, thanks to money-prized contests, considerable attention from wide audiences. We consider these competitions not only a challenge for SAT/CSP solving techniques but also as an opportunity to showcase the advances in the SAT/CSP community to a general audience. This paper studies the NP-complete problem of edge matching puzzles focusing on providing generation models of problem instances of variable hardness and on its resolution through the application of SAT and CSP techniques. From the generation side, we also identify the phase transition phenomena for each model. As solving methods, we employ both; SAT solvers through the translation to a SAT formula, and two ad-hoc CSP solvers we have developed, with different levels of consistency, employing several generic and specialized heuristics. Finally, we conducted an extensive experimental investigation to identify the hardest generation models and the best performing solving techniques.

Ética de las organizaciones de Servicios Sociales (parte II)

Este artículo, por su extensión, se dividió en dos partes. La primera, que se editó en el número anterior, se centró en descubrir las características tanto de las organizaciones del bienestar, como de la ética cuando se aplica a la organización. En esta segunda parte, se presenta un esquema para situar y analizar la dimensión ética en las organizaciones de Servicios Sociales así como la postura que, en ellos, correspondería tomar a los profesionales. Con ello se trata de establecer la conveniencia de introducir o profundizar la reflexión ética en las organizaciones de Servicios Sociales y aportar argumentos que demuestren que también incumbe a éstas el plantearse y mantener en todo lo posible un tipo de comportamiento honesto, acorde con la dignidad de todas las personas y posibilitador de una vida buena.

Produção de mudas de caramboleiras 'B-10' e 'Golden Star': II - marcha de absorção e acúmulo de nutrientes

A participação do Brasil no mercado externo de frutas tem aumentado consideravelmente e com potencial para crescer ainda mais. A constante ascensão dos dados de exportação brasileira é resultado da combinação de avanços tecnológicos do setor produtivo e de acesso a novos mercados consumidores. A caramboleira apresenta-se como uma excelente opção de cultivo de frutas exóticas, com grande potencial para atender ao mercado interno e às exportações. Assim, objetivou-se avaliar a marcha de absorção e de acúmulo de nutrientes em mudas de caramboleiras cultivadas em solução nutritiva. O experimento foi realizado em parcelas subdivididas, sendo utilizadas como parcela as duas cultivares de caramboleira ('B-10' e 'Golden Star') e, como subparcelas, cinco épocas de coleta de plantas, realizadas aos 208; 233; 258; 283 e 308 dias após o transplantio para a solução nutritiva. O delineamento foi inteiramente casualizado, com três repetições. As mudas foram cultivadas em vasos (8L) com solução nutritiva (pH=5,5 ± 0,5), com aeração. O experimento iniciou-se em 24-08-2005. Nos diferentes órgãos das mudas (folhas, caule e raízes), determinaram-se a marcha de absorção, o acúmulo de nutrientes e os índices nutricionais. Não houve diferenças no acúmulo de nutrientes entre as mudas de caramboleira de ambas as cultivares, sendo a ordem decrescente dos nutrientes em cada muda de 'B-10', no final do período experimental: N > K > Ca > Mg > S > P > Fe > Mn > B > Cu > Zn. Para a 'Golden Star', a ordem foi: N > K > Ca > Mg > P > S > Fe > Mn > B > Cu > Zn. Para as duas cultivares, o acúmulo médio foi maior nas folhas > caule > raízes. O período de maior exigência para 'B-10' foi entre 208 - 233 e, para 'Golden Star', entre 233 - 283 dias após o transplantio. As diferentes taxas de acumulação líquida dos nutrientes, nos diferentes órgãos da caramboleira, nem sempre acompanharam a taxa de acumulação de nutrientes do respectivo órgão.

Platinum (II) and palladium (II) complexes with (N,N') and (C,N,N') ligands derived from pyrazole as anticancer and antimalarial agents: synthesis, characterization and in vitro activities

The study of the reactivity of three 1-(2-dimethylaminoethyl)-1H-pyrazole derivatives of general formula [1-(CH2)2NMe2}-3,5-R2-pzol] {where pzol represents pyrazole and Rdouble bond; length as m-dashH (1a), Me (1b) or Ph (1c)} with [MCl2(DMSO)2] (Mdouble bond; length as m-dashPt or Pd) under different experimental conditions allowed us to isolate and characterize cis-[M{κ2-N,N′-{[1-(CH2)2NMe2}-3,5-R2-pzol])}Cl2] {MMdouble bond; length as m-dashPtPt (2a-2c) or Pd (3a-3c)} and two cyclometallated complexes [M{κ3-C,N,N′-{[1-(CH2)2NMe2}-3-(C5H4)-5-Ph-pzol])}Cl] {Mdouble bond; length as m-dashPt(II) (4c) or Pd(II) (5c)}. Compounds 4c and 5c arise from the orthometallation of the 3-phenyl ring of ligand 1c. Complex 2a has been further characterized by X-ray crystallography. Ligands and complexes were evaluated for their in vitro antimalarial against Plasmodium falciparum and cytotoxic activities against lung (A549) and breast (MDA MB231 and MCF7) cancer cellular lines. Complexes 2a-2c and 5c exhibited only moderate antimalarial activities against two P. falciparum strains (3D7 and W2). Interestingly, cytotoxicity assays revealed that the platinacycle 4c exhibits a higher toxicity than cisplatin in the three human cell lines and that the complex 2a presents a remarkable cytotoxicity and selectivity in lung (IC50 = 3 μM) versus breast cancer cell lines (IC50 > 20 μM). Thus, complexes 2c and 4c appear to be promising leads, creating a novel family of anticancer agents. Electrophoretic DNA migration studies in presence of the synthesized compounds have been performed, in order to get further insights into their mechanism of action.

Photocontrolled DNA Binding of a Receptor-Targeted Organometallic Ruthenium(II) Complex

A photoactivated ruthenium(II) arene complex has been conjugated to two receptor-binding peptides, a dicarba analogue of octreotide and the Arg-Gly-Asp (RGD) tripeptide. These peptides can act as"tumor-targeting devices" since their receptors are overexpressed on the membranes of tumor cells. Both ruthenium-peptide conjugates are stable in aqueous solution in the dark, but upon irradiation with visible light, the pyridyl-derivatized peptides were selectively photodissociated from the ruthenium complex, as inferred by UV-vis and NMR spectroscopy. Importantly, the reactive aqua species generated from the conjugates, [(η6-p-cym)Ru(bpm)(H2O)]2+, reacted with the model DNA nucleobase 9-ethylguanine as well as with guanines of two DNA sequences, 5′dCATGGCT and 5′dAGCCATG. Interestingly, when irradiation was performed in the presence of the oligonucleotides, a new ruthenium adduct involving both guanines was formed as a consequence of the photodriven loss of p-cymene from the two monofunctional adducts. The release of the arene ligand and the formation of a ruthenated product with a multidentate binding mode might have important implications for the biological activity of such photoactivated ruthenium(II) arene complexes. Finally, photoreactions with the peptide-oligonucleotide hybrid, Phac-His-Gly-Met-linker-p5′dCATGGCT, also led to arene release and to guanine adducts, including a GG chelate. The lack of interaction with the peptide fragment confirms the preference of such organometallic ruthenium(II) complexes for guanine over other potential biological ligands, such as histidine or methionine amino acids.

Conjugation of a Ru(II) Arene Complex to Neomycin or to Guanidinoneomycin Leads to Compounds with Differential Cytotoxicities and Accumulation between Cancer and Normal Cells

A straightforward methodology for the synthesis of conjugates between a cytotoxic organometallic ruthenium(II) complex and amino- and guanidinoglycosides, as potential RNA-targeted anticancer compounds, is described. Under microwave irradiation, the imidazole ligand incorporated on the aminoglycoside moiety (neamine or neomycin) was found to replace one triphenylphosphine ligand from the ruthenium precursor [(η6-p-cym)RuCl(PPh3)2]+, allowing the assembly of the target conjugates. The guanidinylated analogue was easily prepared from the neomycin-ruthenium conjugate by reaction with N,N′-di-Boc-N″-triflylguanidine, a powerful guanidinylating reagent that was compatible with the integrity of the metal complex. All conjugates were purified by semipreparative high-performance liquid chromatography (HPLC) and characterized by electrospray ionization (ESI) and matrix-assisted laser desorption-ionization time-of-flight (MALDI-TOF) mass spectrometry (MS) and NMR spectroscopy. The cytotoxicity of the compounds was tested in MCF-7 (breast) and DU-145 (prostate) human cancer cells, as well as in the normal HEK293 (Human Embryonic Kidney) cell line, revealing a dependence on the nature of the glycoside moiety and the type of cell (cancer or healthy). Indeed, the neomycin-ruthenium conjugate (2) displayed moderate antiproliferative activity in both cancer cell lines (IC50 ≈ 80 μM), whereas the neamine conjugate (4) was inactive (IC50 ≈ 200 μM). However, the guanidinylated analogue of the neomycin-ruthenium conjugate (3) required much lower concentrations than the parent conjugate for equal effect (IC50 = 7.17 μM in DU-145 and IC50 = 11.33 μM in MCF-7). Although the same ranking in antiproliferative activity was found in the nontumorigenic cell line (3 2 > 4), IC50 values indicate that aminoglycoside-containing conjugates are about 2-fold more cytotoxic in normal cells (e.g., IC50 = 49.4 μM for 2) than in cancer cells, whereas an opposite tendency was found with the guanidinylated conjugate, since its cytotoxicity in the normal cell line (IC50 = 12.75 μM for 3) was similar or even lower than that found in MCF-7 and DU-145 cancer cell lines, respectively. Cell uptake studies performed by ICP-MS with conjugates 2 and 3 revealed that guanidinylation of the neomycin moiety had a positive effect on accumulation (about 3-fold higher in DU-145 and 4-fold higher in HEK293), which correlates well with the higher antiproliferative activity of 3. Interestingly, despite the slightly higher accumulation in the normal cell than in the cancer cell line (about 1.4-fold), guanidinoneomycin-ruthenium conjugate (3) was more cytotoxic to cancer cells (about 1.8-fold), whereas the opposite tendency applied for neomycin-ruthenium conjugate (2). Such differences in cytotoxic activity and cellular accumulation between cancer and normal cells open the way to the creation of more selective, less toxic anticancer metallodrugs by conjugating cytotoxic metal-based complexes such as ruthenium(II) arene derivatives to guanidinoglycosides.

Notas floristicas, II

Es muy frecuente, en una gran parte de la t i e r r a baja catalana, una forma litigiosa de Galium pumilum Murr. ( = G . silvesire P o l l . = G . asperum Schreb.) que ha dado motivo a numerosas confusiones.

Fulvestrant with or without selumetinib, a MEK 1/2 inhibitor, in breast cancer progressing after aromatase inhibitor therapy: A multicentre randomised placebo-controlled double-blind phase II trial, SAKK 21/08.

BACKGROUND: Second line endocrine therapy has limited antitumour activity. Fulvestrant inhibits and downregulates the oestrogen receptor. The mitogen-activated protein kinase (MAPK) pathway is one of the major cascades involved in resistance to endocrine therapy. We assessed the efficacy and safety of fulvestrant with selumetinib, a MEK 1/2 inhibitor, in advanced stage breast cancer progressing after aromatase inhibitor (AI). PATIENTS AND METHODS: This randomised phase II trial included postmenopausal patients with endocrine-sensitive breast cancer. They were ramdomised to fulvestrant combined with selumetinib or placebo. The primary endpoint was disease control rate (DCR) in the experimental arm. ClinicalTrials.gov Indentifier: NCT01160718. RESULTS: Following the planned interim efficacy analysis, recruitment was interrupted after the inclusion of 46 patients (23 in each arm), because the selumetinib-fulvestrant arm did not reach the pre-specified DCR. DCR was 23% (95% confidence interval (CI) 8-45%) in the selumetinib arm and 50% (95% CI 27-75%) in the placebo arm. Median progression-free survival was 3.7months (95% CI 1.9-5.8) in the selumetinib arm and 5.6months (95% CI 3.4-13.6) in the placebo arm. Median time to treatment failure was 5.1 (95% CI 2.3-6.7) and 5.6 (95% CI 3.4-10.2) months, respectively. The most frequent treatment-related adverse events observed in the selumetinib-fulvestrant arm were skin disorders, fatigue, nausea/vomiting, oedema, diarrhoea, mouth disorders and muscle disorders. CONCLUSIONS: The addition of selumetinib to fulvestrant did not show improving patients' outcome and was poorly tolerated at the recommended monotherapy dose. Selumetinib may have deteriorated the efficacy of the endocrine therapy in some patients.

Two cilengitide regimens in combination with standard treatment for patients with newly diagnosed glioblastoma and unmethylated MGMT gene promoter: results of the open-label, controlled, randomized phase II CORE study.

BACKGROUND: Survival outcomes for patients with glioblastoma remain poor, particularly for patients with unmethylated O(6)-methylguanine-DNA methyltransferase (MGMT) gene promoter. This phase II, randomized, open-label, multicenter trial investigated the efficacy and safety of 2 dose regimens of the selective integrin inhibitor cilengitide combined with standard chemoradiotherapy in patients with newly diagnosed glioblastoma and an unmethylated MGMT promoter. METHODS: Overall, 265 patients were randomized (1:1:1) to standard cilengitide (2000 mg 2×/wk; n = 88), intensive cilengitide (2000 mg 5×/wk during wk 1-6, thereafter 2×/wk; n = 88), or a control arm (chemoradiotherapy alone; n = 89). Cilengitide was administered intravenously in combination with daily temozolomide (TMZ) and concomitant radiotherapy (RT; wk 1-6), followed by TMZ maintenance therapy (TMZ/RT→TMZ). The primary endpoint was overall survival; secondary endpoints included progression-free survival, pharmacokinetics, and safety and tolerability. RESULTS: Median overall survival was 16.3 months in the standard cilengitide arm (hazard ratio [HR], 0.686; 95% CI: 0.484, 0.972; P = .032) and 14.5 months in the intensive cilengitide arm (HR, 0.858; 95% CI: 0.612, 1.204; P = .3771) versus 13.4 months in the control arm. Median progression-free survival assessed per independent review committee was 5.6 months (HR, 0.822; 95% CI: 0.595, 1.134) and 5.9 months (HR, 0.794; 95% CI: 0.575, 1.096) in the standard and intensive cilengitide arms, respectively, versus 4.1 months in the control arm. Cilengitide was well tolerated. CONCLUSIONS: Standard and intensive cilengitide dose regimens were well tolerated in combination with TMZ/RT→TMZ. Inconsistent overall survival and progression-free survival outcomes and a limited sample size did not allow firm conclusions regarding clinical efficacy in this exploratory phase II study.

Eficiência quântica do fotossistema II de mudas de abacaxizeiro 'imperial' em resposta a associação com Piriformospora indica e herbicidas

O objetivo foi avaliar o efeito dos herbicidas diuron, ametryn e sulfentrazone, e da associação micorrízica na eficiência quântica do fotossistema II de mudas de abacaxizeiro 'Imperial'. Foi utilizado o esquema de parcela subdividida, tendo na parcela o fatorial 2 x 4, sendo dois tipos de mudas: inoculadas com P. indica e sem inoculação, e quatro doses de herbicidas: 0; 1,5; 3,0 e 6,0 L ha-1 para o ametryn, 0; 1,6; 3,2 e 6,4 L ha-1 para o diuron e 0; 0,4; 0,8 e 1,6 L ha-1 para o sulfentrazone, e na subparcela as épocas de avaliação, distribuídos no delineamento inteiramente casualizado, com três repetições. Os herbicidas foram aplicados ao substrato antes do plantio das mudas. A inoculação com o fungo P. indica foi feita no momento do plantio. A avaliação da eficiência quântica foi feita por meio da razão de fluorescência da clorofila a (Fv/Fm), determinada aos 60; 90 e 120 dias após o plantio das mudas, obtendo-se a fluorescência inicial, máxima, e variável. Os dados obtidos foram submetidos à análise de variância e regressão polinomial. O herbicida ametryn não comprometeu a eficiência do fotossistema II das mudas de abacaxizeiro inoculadas com o fungo P. indica. A inoculação com fungo P. indica aumentou a eficiência do fotossistema II das mudas. A aplicação dos herbicidas diuron e sulfentrazone em doses elevadas reduziu a eficiência do fotossistema II de mudas de abacaxizeiro 'Imperial' não inoculadas com o fungo P. indica.

ADUBAÇÃO NITROGENADA E POTÁSSICA EM GOIABEIRAS ‘PALUMA’:II. EFEITO NO ESTADO NUTRICIONAL DAS PLANTAS

RESUMOA adequada adubação mineral de pomares de goiabeira, sob manejo intensivo, é fator preponderante na produtividade, e o acompanhamento do estado nutricional das plantas contribui para a eficiência desta prática agronômica.Objetivou-se pesquisar o efeito de diferentes doses de nitrogênio e potássio sobre o estado nutricional de goiabeiras‘Paluma’. O experimento foi conduzido em Vista Alegre do Alto-SP, em pomar irrigado, com sete anos deidade, manejado com podas de frutificação, durante quatro ciclos de produção consecutivos. O solo é o Argissolo Vermelho-Amarelo distrófico. O delineamento experimental foi em blocos ao acaso, com trêsrepetições, em esquema fatorial com quatro doses de nitrogênio (0; 0,5; 1,0 e 2,0 kg planta-1 de N) e quatro depotássio (0;0,55; 1,1 e 2,2 kg planta-1 de K2O). A adubação nitrogenada promoveu aumento nos teores foliares de N e Mn e decréscimo nos teores de P e B, observados do segundo ao quarto ciclo produtivo. A adubaçãonitrogenada elevou os teores de Ca e Mg, respectivamente, no segundo e terceiro ciclos. Com exceção doprimeiro ciclo produtivo, os teores foliares de K e Mn aumentaram em função da adubação potássica, enquanto os teores de Mg, no segundo e quarto ciclos, diminuíram em função dessa adubação.