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

Electroferótipos de rotavirus em crianças com e sem quadros de gastroenterite.

It was defined the electropherotypes of rotavirus identified in stools of a groups (named "case") of 500 children with diarrhea, ranging in age from 0 to 12 months. A group (named "control") of 500 children of the same age group, without diarrhea or respiratory infections, were evaluated. Human rotavirus was detected in 14.8% of the children with diarrhea. Of the positive samples 5 had the "short" and 11 the "long" electropherotype. In the control group rotavirus was detected in 0.8% of children and all the three positive samples had "long" electropherotype

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

Non-Hardware-Based Non-Technical Losses Detection Methods: A Review

Non-Technical Losses (NTL) represent a serious concern for electric companies. These losses are responsible for revenue losses, as well as reduced system reliability. Part of the revenue loss is charged to legal consumers, thus, causing social imbalance. NTL methods have been developed in order to reduce the impact in physical distribution systems and legal consumers. These methods can be classified as hardware-based and non-hardware-based. Hardware-based methods need an entirely new system infrastructure to be implemented, resulting in high investment and increased cost for energy companies, thus hampering implementation in poorer nations. With this in mind, this paper performs a review of non-hardware-based NTL detection methods. These methods use distribution systems and consumers’ data to detect abnormal energy consumption. They can be classified as network-based, which use network technical parameters to search for energy losses, data-based methods, which use data science and machine learning, and hybrid methods, which combine both. This paper focuses on reviewing non-hardware-based NTL detection methods, presenting a NTL detection methods overview and a literature search and analysis

Shielding and stealth effects of zwitterion moieties in double-functionalized silica nanoparticles

Surface functionalization of silica nanoparticles (SiO2NPs) has been considered as a promising strategy to develop target-specific nanostructures. However, finding a chemical functionalization that can be used as an active targeting moiety while preserving the nanoparticles colloidal stability in biological fluids is still challenging. We present here a dual surface modification strategy for SiO2NPs where a zwitterion (ZW) and a biologically active group (BAG) (amino, mercapto or carboxylic functionalities) are simultaneously grafted on the nanoparticles’ surface. The rationale behind this strategy is to generate colloidally stable nanoparticles and avoid the nonspecific protein adsorption due to ZW groups insertion, while the effective interaction with biosystems is guaranteed by the BAGs presence. The biological efficacy was tested against VERO cells, E. coli bacteria and Zika viruses and a similar trend was observed for all tested particles. The desirable “stealth property” to prevent nonspecific protein adhesion also generated a ZW shielding effect of the BAG functionality hindering their proper interaction and activity in cells, bacteria and viruses553540548CONSELHO NACIONAL DE DESENVOLVIMENTO CIENTÍFICO E TECNOLÓGICO - CNPQFUNDAÇÃO DE AMPARO À PESQUISA DO ESTADO DE SÃO PAULO - FAPESP440379-2016-4; 130767-201615/25406-5; 16/16905-0; 16/21598-0; 17/01167-7; 17/06692-2;17/09203-2The authors would like to acknowledge the financial support of the São Paulo Research Foundation – FAPESP (processes 15/25406-5, 16/16905-0, 16/21598-0, 17/01167-7, 17/06692-2 and 17/09203-2), CNPq, Capes and Decit (processes 440379-2016-4 and 130767-2016-1). The authors also thank LME and LCS labs in LNNano – CNPEM for the use of electron microscopy and atomic force microcopy facilitie

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