Xanthenones: Calixarenes-catalyzed Syntheses, Anticancer Activity And Qsar Studies

An efficient method is proposed for obtaining tetrahydrobenzo[a]xanthene-11-ones and tetrahydro-[1,3]-dioxolo[4,5-b]xanthen-9-ones. The method is based on the use of p-sulfonic acid calix[n]arenes as catalysts under solvent-free conditions. The antiproliferative activity of fifty-nine xanthenones against six human cancer cells was studied. The capacity of all compounds to inhibit cancer cell growth was dependent on the histological origin of the cells. QSAR studies indicate that among compounds derived from β-naphthol the most efficient compounds against glioma (U251) and renal (NCI-H460) cancer cells are those having higher hydrogen bonding donor ability.131132803287Lozano, R., Naghavi, M., Foreman, K., (2013) Lancet, 380, pp. 2095-2128Nakash, O., Levav, I., Aguilar-Gaxiola, S., (2014) Psychooncology, 23, pp. 40-51Chabner, B.A., Roberts, J.T.G., (2005) Nat. Rev. Cancer, 5, pp. 65-72Lambert, R.W., Martin, J.A., Merrett, J.H., Parkes, K.E.B., Thomas, G.J., (1997) CT Int. ApplPoupelin, J.P., Saint-Rut, G., Fussard-Blanpin, O., Narcisse, G., Uchida-Ernouf, G., Lakroix, R., (1978) Eur. J. Med. Chem., 13, pp. 67-71Kumar, A., Sharma, S., Maurya, R.A., Sarkar, J., (2010) J. Comb. Chem., 12, pp. 20-24Hideo, T., Teruomi, J., (1981) Jpn. Patent, p. 56.005.480Banerjee, A., Mukherjee, A.K., (1981) Biotech. Histochem., 56, pp. 83-85Knight, C.G., Stephens, T., (1989) Biochem. J., 258, pp. 683-689Sirkencioglu, O., Talinli, N., Akar, A.J., (1995) Chem. Res., 12, p. 502Ion, R.M., Planner, A., Wiktorowicz, K., Frackowiak, D., (1998) Acta Biochim. Pol., 45, pp. 833-845Heravi, M.M., Alinejhad, H., Bakhtiari, K., Saeedi, M., Oskooie, H.A., Bamoharram, F.F., (2011) Bull. Chem. Soc. Ethiop., 25, pp. 399-406Khurana, J.M., Magoo, D.P., (2009) Tetrahedron Lett., 50, pp. 4777-4780Zhang, Z.-H., Wang, H.-J., Ren, X.-Q., Zhang, Y.-Y., (2009) Monatsh. Chem., 140, pp. 1481-1483Simões, J.B., Da Silva, D.L., De Fátima, A., Fernandes, S.A., (2012) Curr. Org. Chem., 16, pp. 949-971De Fátima, A., Fernandes, S.A., Sabino, A.A., (2009) Curr. Drug Discovery Technol., 6, pp. 151-170Varejão, E.V.V., De Fátima, A., Fernandes, S.A., (2013) Curr. Pharm. Des., 19, pp. 6507-6521Jose, P., Menon, S., (2007) Bioinorg. Chem. Appl., 28, pp. 1-16Da Silva, D.L., Fernandes, S.A., Sabino, A.A., De Fátima, A., (2011) Tetrahedron Lett., 52, pp. 6328-6330Simões, J.B., De Fátima, A., Sabino, A.A., Aquino, F.J.T., Da Silva, D.L., Barbosa, L.C.A., Fernandes, S.A., (2013) Org. Biomol. Chem., 11, pp. 5069-5073Simões, J.B., De Fátima, A., Sabino, A.A., Barbosa, L.C.A., Fernandes, S.A., (2014) RSC Adv., 4, pp. 18612-18615Shimizu, S., Shimada, N., Sasaki, Y., (2006) Green Chem., 8, pp. 608-614Fernandes, S.A., Natalino, R., Gazolla, P.A.R., Da Silva, M.J., Jham, G.N., (2012) Tetrahedron Lett., 53, pp. 1630-1633Monks, A., Scudeiro, D., Skehan, P., Shoemaker, R., Paull, K., Vistica, D., Hose, C., Boyd, M.J., (1991) J. Natl. Cancer Inst., 83, pp. 757-766Xia, B., Ma, W., Zheng, B., Zhang, X., Fan, B., (2008) Eur. J. Med. Chem., 43, pp. 1489-1498Stanton, D.T., Jurs, P.C., (1990) Anal. Chem., 62, p. 2323Stanton, D.T., Egolf, L.M., Jurs, P.C., Hicks, M.G., (1992) J. Chem. Inf. Comput. Sci., 32, p. 306Gutsche, C.D., Dhawan, B., No, K.H., Muthukrishnan, R., (1981) J. Am. Chem. Soc., 103, pp. 3782-3792Casnati, A., Ca, N.D., Sansone, F., Ugozzoli, F., Ungaro, R., (2004) Tetrahedron, 60, pp. 7869-7876Shinkai, S., Araki, K., Tsubaki, T., Some, T., Manabe, O., (1987) J. Chem. Soc., Perkin Trans. 1, pp. 2297-2299Da Silva, D.L., Reis, F.S., Muniz, D.R., Ruiz, A.L.T.G., De Carvalho, J.E., Sabino, A.A., Modolo, L.V., De Fátima, A., (2012) Bioorg. Med.Chem., 20, pp. 2645-2650Pacheco, S.R., Braga, T.C., Da Silva, D.L., Horta, L.P., Reis, F.S., Ruiz, A.L.T.G., De Carvalho, J.E., De Fátima, A., (2013) Med. Chem., 9, pp. 889-896Spartan'06, , Wavefunction, Inc., Irvine, CAStewart, J.J.P., (2007) MOPAC 2007, version 7, , 290 W Stewart Computational Chemistry, Colorado Springs, CODewar, M.J.S., Zoebisch, E.G., Healy, E.F., (1985) J. Am. Chem. Soc., 107, pp. 3902-3909Jensen, F., (2007) Introduction to computational chemistry, , John Wiley & Son Ltd, 2nd ednKatritsky, A.R., Lobanov, V.S., Karelson, M., (1996) CODESSA: Reference ManualVersion 2, , University of Florid

RENDIMIENTO DE MAÍZ Y CAMBIOS EN PROPIEDADES EDÁFICAS LUEGO DE LA APLICACIÓN DE EFLUENTES LÍQUIDOS PORCINOS

El objetivo de este trabajo fue evaluar el efecto de la aplicación de efluentes líquidos porcinos sobre la productividad del cultivo de maíz y diversas propiedades químicas y físicas de un Argiudol del centro de Santa Fe. Para ello se realizó un experimento a campo donde se aplicaron tres dosis de efluente en un diseño en bloques completamente aleatorizado con tres repeticiones. No se registraron variaciones en el número de plantas entre el inicio y el fin del ensayo. La productividad del cultivo se incrementó marcadamente por la adición del efluente lográndose la mayor respuesta en grano con la dosis intermedia. Las propiedades químicas del suelo mostraron cambios debido a la adición de efluentes porcinos mientras que las físicas, a excepción de la resistencia mecánica, no sufrieron cambios significativos. Se considera necesario realizar nuevos ensayos para monitorear fundamentalmente las propiedades químicas para minimizar riesgos de contaminación del suelo y toxicidad sobre las plantas.The aim of this paper was to assess the effect of the swine effluent application on the corn production and some chemical and physical properties of an Argiudoll of the center of Santa Fe. A field experiment was carried out applying three rates of swine liquid effluent in a randomized complete block design with three replications. No changes were observed on crop density from the the beginning to the end of the experiment. The crop productivity increased notably due to the swine effluent application and the highest yield was obtained with the intermediate rate. Soil chemical properties showed some changes related to swine effluent application while the physical properties did not show significant changes, with the exception of soil mechanical resistance. More research and continuous monitoring of the soil chemical properties are needed in order to minimize potential risks of environmental contamination and toxicity over plants. and continuous monitoring of the soil chemical properties are needed in order to minimize potential risks of environmental contamination and toxicity over plants.Fil: Micheloud, H.. Universidad Nacional del Litoral. Facultad de Ciencias Agrarias; ArgentinaFil: Carrizo, Maria Eugenia. Universidad Nacional del Litoral. Facultad de Ciencias Agrarias; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Santa Fe. Instituto de Agrobiotecnologia del Litoral; ArgentinaFil: Alesso, Carlos Agustín. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Santa Fe. Instituto de Agrobiotecnologia del Litoral; ArgentinaFil: Girello, G.. Universidad Nacional del Litoral. Facultad de Ciencias Agrarias; ArgentinaFil: Capeletti, M.. Universidad Nacional del Litoral. Facultad de Ciencias Agrarias; ArgentinaFil: Imhoff, Silvia del Carmen. Universidad Nacional del Litoral. Facultad de Ciencias Agrarias; Argentin

Tailoring the antimicrobial response of cationic nanocellulose-based foams through cryo-templating

FAPESP – FUNDAÇÃO DE AMPARO À PESQUISA DO ESTADO DE SÃO PAULOLNNANO - BRAZILIAN NANOTECHNOLOGY NACIONAL LABORATORYTo shed light on novel sustainable materials with antimicrobial functionality, in this contribution, we describe the use of cationic nanocellulose to produce foams featuring antibacterial activity against the powerful human pathogen Escherichia coli. Dialdehyde cellulose was cationized with Girard’s reagent T (GRT), mechanically disintegrated into nanofibrillated cellulose (NFC), and shaped into foams through different protocols. All steps were carried out in aqueous media and in the absence of hazardous chemicals. While evaporative drying led to compact films (density of 1.3 g cm–3), freeze-casting (i.e., freezing and freeze-drying) produced monolithic cryogels with low densities (<50 mg cm–3) and porosities of ca. 98%. Although highly porous, the cryogels obtained through rapid freezing remarkably presented smaller pores than those that were previously frozen in a slow fashion. The quaternary ammonium groups of GRT-cationized NFC removed E. coli to different extents depending upon sample morphology. We demonstrated in an innovative manner that porosity, which is directly associated with surface area, and pore size play an essential role on the antimicrobial performance. This outcome arises from the inaccessibility of bacterial cells to cationic surfaces inside monoliths composed of small pores. We herein present an uncomplicated, environmentally friendly protocol for fine-tuning the porosity and pore size of all-cellulose materials through cryo-templating. Controlling these morphometric parameters allowed us to achieve a ca. 85% higher anti-E. coli activity when comparing samples made up of the very same material (i.e., the same NFC concentration and degree of substitution) but presented as dense films. These findings bear clear implications for the pursuit of sustainable materials presenting multifunctionality2519751986FAPESP – FUNDAÇÃO DE AMPARO À PESQUISA DO ESTADO DE SÃO PAULOLNNANO - BRAZILIAN NANOTECHNOLOGY NACIONAL LABORATORYFAPESP – FUNDAÇÃO DE AMPARO À PESQUISA DO ESTADO DE SÃO PAULOLNNANO - BRAZILIAN NANOTECHNOLOGY NACIONAL LABORATORY2017/07013-1; 2017/01167-7; 2015/25406-

Palynological and physicochemical characterization of Apis mellifera L. bee pollen in the Southern region of Brazil

Bee pollen has been used for many years in both traditional medicine and supplementary nutrition, as well as in alternative diets, mainly due to its nutritional properties and health benefits. Bee pollen production is a recent activity in Brazil, having begun in the late 1980s. However, the country has the potential of being a large world producer of high quality pollen, particularly because of the great diversity of tropical flora and the resistance of the Brazilian Apis mellifera bee races. Thirty-six samples of bee pollen from the Southern region of Brazil were analyzed regarding pollen types and physicochemical and nutritional composition. Only one sample was considered monofloral, which was exclusively composed by pollen from the Asteraceae family). The State of Parana showed a greater variety of pollen types, 18 in total, representing 82% of the total number identified in this study. The bee pollen in the States of Rio Grande do Sul and Parana showed a higher number of samples with humidity content above the standard permitted by the Brazilian legislation, i.e. over 4%. The bee pollen was characterized by its high protein content with average values of 20.47%. The analysis regarding humidity, lipids and sugar showed no statistical differences among the samples (p<0.05). The pollen samples had a high concentration of reducible sugars (48%). The predominant minerals in the samples PR, SC and RS were phosphorus (7102.29, 6873.40, 6661.73 mg/kg of pollen), followed by potassium (5383.73, 4997.77, 4773.26 mg/kg of pollen), calcium (1179.05, 961.93, 848.36 mg/kg of pollen) and magnesium (818.02, 679.01, 725.89 mg/kg of pollen). Statistical analysis (Tukey test) demonstrated no significant difference between the contents of calcium, copper, iron, phosphorus and sodium in the pollen samples of the South of Brazil. However, the samples from the State of Parana contained the highest contents of potassium and differed statistically from the samples of the State of Rio Grande do Sul.FAPES

Effect of long-term treatment with insulin and/or acarbose on glomerular basement membrane thickening in alloxan-diabetic rats

Acarbose is a competitive inhibitor of the intestinal alpha-glycosidases, that can delay absorption of intestinal carbohydrates causing their malabsorption. In the present paper we studied the effects of insulin, acarbose and their association on glomerular basement membrane thickening in alloxan-diabetic rats. Twenty-five male and female Wistar rats, approximately 3 months old at the beginning of the experiment, were assigned randomly to each of five experimental groups: normal control rats, alloxan-diabetic control rats, alloxan-diabetic rats treated with acarbose, alloxan-diabetic rats treated with insulin, and alloxan-diabetic rats treated with insulin plus acarbose. Alloxan was administered in a single iv dose of 42 mg/kg body weight. Insulin was given subcutaneously at doses of 18 to 30 IU/kg corrected daily on the basis of glycosuria and ketonuria. Acarbose was given mixed with rat chow in a dose of 50 mg/100 g chow. Body weight, water and food intake and diuresis, as well as blood and urine glucose were determined after 1, 3, 6, 9, and 12 months of treatment. Glomerular basement membrane (GBM) thickening was determined by electron microscopy at the same times. Clear clinical and laboratory signs of severe diabetes, with blood glucose levels above 200 mg/dl and urine glucose above 3000 mg/dl, were observed in all alloxan-diabetic control rats, in all periods of follow-up, whereas administration of insulin or acarbose reduced the blood glucose levels of treated groups. The most satisfactory control of blood and urine glucose was observed in animals treated with both insulin and acarbose. However, diarrhea was observed in diabetic rats treated with acarbose associated or not with insulin. GBM thickening was correlated with age in all groups. Beginning at six months after diabetes induction, the GBM of untreated diabetic rats was significantly thicker (mean +/- SEM, 4.446 +/- 0.45 mm) than that of normal rats (2.977 +/- 0.63 mm). Both insulin and acarbose prevented GBM thickening and their combination induced thickening similar to the age-dependent thickening observed for normal rats of the same age. We conclude that acarbose when combined with insulin may be a good option in the control of diabetes and its renal complications

Impacto da disfunção renal na evolução intra-hospitalar após cirurgia de revascularização miocárdica

FUNDAMENTO: A doença renal crônica (DRC) é um marcador de mortalidade na cirurgia de revascularização miocárdica (CRM). OBJETIVO: Avaliar em pacientes com DRC submetidos a CRM as características clínicas e os marcadores de morbimortalidade hospitalar; comparar a evolução intra-hospitalar entre os grupos com e sem DRC, e com e sem desenvolvimento de insuficiência renal aguda (IRA). MÉTODOS: Foram analisadas as CRM isoladas realizadas num hospital público cardiológico de 1999 a 2007. Considerado disfunção renal quando creatinina > 1,5 mg/dl. Avaliaram-se características clínicas, mortalidade e complicações pós-operatórias conforme a função renal. RESULTADOS: De 3.890 pacientes, 362 (9,3%) tinham DRC. Esse grupo apresentava idade mais avançada, maior prevalência de hipertensão, disfunção ventricular esquerda, acidente vascular encefálico (AVE) prévio, doença arterial periférica e triarteriais. No pós-operatório, apresentou maior incidência de AVE (5,5% vs 2,1%), fibrilação atrial (16 vs 8,3%), síndrome de baixo débito cardíaco (14,4% vs 8,5%), maior tempo de internação na unidade de terapia intensiva (4,04 vs 2,83 dias), e maior mortalidade intra-hospitalar (10,5% vs 3,8%). Sexo feminino, tabagismo, diabete e doença vascular periférica e/ou carotídea associaram-se com maior mortalidade no grupo DRC. Pacientes que não desenvolveram IRA pós-operatória apresentaram 3,5% de mortalidade; grupo IRA não dialítica: 35,4%; grupo IRA dialítica: 66,7%. Calculando-se a taxa de filtração glomerular, observou-se aumento da mortalidade conforme o aumento da classe da DRC. CONCLUSÃO: Pacientes com DRC submetidos a CRM constituem população de elevado risco, apresentando maior morbimortalidade. IRA pós-operatória é importante marcador de mortalidade. A taxa de filtração glomerular foi inversamente relacionada com mortalidade