N-4-Phenyl-substituted 2-acetylpyridine thiosemicarbazones: Cytotoxicity against human tumor cells, structure-activity relationship studies and investigation on the mechanism of action

N-4-Phenyl 2-acetylpyridine thiosemicarbazone (H2Ac4Ph; N-(phenyl)-2-(1-(pyridin-2-yl)ethylidene) hydrazinecarbothioamide) and its N-4-ortho-, -meta- and -para-fluorophenyl (H2Ac4oFPh, H2Ac4mFPh, H2Ac4pFPh), N-4-ortho-, -meta- and -para-chlorophenyl (H2Ac4oClPh, H2Ac4mClPh, H2Ac4pClPh), N-4-ortho-, -meta- and -para-iodophenyl (H2Ac4oIPh, H2Ac4mIPh, H2Ac4pIPh) and N-4-ortho-, -meta- and -para-nitrophenyl (H2Ac4oNO(2)Ph, H2Ac4mNO(2)Ph, H2Ac4pNO(2)Ph) derivatives were assayed for their cytotoxicity against human malignant breast (MCF-7) and glioma (T98G and U87) cells. The compounds were highly cytotoxic against the three cell lineages (IC50: MCF-7, 52-0.16 nM; T98G, 140-1.0 nM; U87, 160-1.4 nM). All tested thiosemicarbazones were more cytotoxic than etoposide and did not present any haemolytic activity at up to 10(-5) M. The compounds were able to induce programmed cell death. H2Ac4pClPh partially inhibited tubulin assembly at high concentrations and induced cellular microtubule disorganization. (C) 2012 Elsevier Ltd. All rights reserved.

Determinação de elementos traços em diques mesozoicos da Serra do Mar por meio de ativação com nêutrons

A análise de elementos traço, tais como terras raras, TH, U, Ta, Hf, Ba, Rb e Ba, é uma ferramenta muito importante para estudos petrogenéticos. No intuito de estudar tais processos em diques do Enxame Serra do Mar (litoral de São Paulo e Rio de Janeiro), pertencente à Provincia Magmática do Paraná (PMP), uma das províncias de basaltos continentais mais expressivas do mundo, foram realizadas análises por ativação com nêutrons nestes diques. A técnica, empregada no Centro de Reator de pesquisa do Instituto de Pesquisas Energéticas e Nucleares, forneceu concentrações de elementos traço com os níveis de precisão de 10% e exatidão 9% os quais são adequadas para estudos petrogenéticos. Devido as baixas concentrações dos elementos analisados, a rotina experimental de preparação das amostras abrangeu processos bastantes cuidadosos para evitar contaminação. As amostras investigadas podem ser divididas em quatro grupos: rochas básicas (SiO2<55%) com Ti/Y<500; rochas intermediárias (55%63%). Diques de composição intermediária e ácida só ocorrem na Ilha de São Sebastião e na região costeira adjacente. As concentrações de elementos maiores e menores, bem como os padrões de abundância de terras raras e de outros elementos incompatíveis dessas rochas mais diferenciadas, apresentaram semelhanças significativas com os das vulcânicas Chapecó do tipo Ourinhos, sugerindo gênese similar, ou seja, incluindo também processos de contaminação crustal .

137Cs Inventory in sedimentary columns from continental shelf of São Paulo State

137Cs is an artificial radioactive isotope produced by 235U fission. This radionuclide has a high fission yield and a half-life of 30 years. It has been detected in the environment since 1945 and its principal contamination source has been nuclear tests in the atmosphere. There are other sources of 137Cs contamination in the environment, such as: release from nuclear and reprocessing plants, radioactive dumping and nuclear accidents (Chernobyl, for example). This paper presents an inventory of 137Cs on the Continental Shelf of São Paulo State, a region located between Cabo de Santa Marta Grande (Santa Catarina state) and Cabo Frio (Rio de Janeiro state). In this area, 9 cores were collected by the Instituto Oceanográfico da Universidade de São Paulo (São Paulo University Institute of Oceanography). The cores were sliced at every 2 cm; sub-samples were lyophilized, grinded and stored in plastic containers. 137Cs was determined by 661 keV photopeak using a gamma spectrometry detector (Ge hyperpure). The analysis was performed by efficiency and background in different counting times. 137Cs concentration activities varied from 0.3 to 3.6 Bq kg-1 with a mean value of 1.2±0.6 Bq kg-1. The inventory of 137Cs in this area was 13±7 Bq m-2. Values obtained are in agreement with the Southern Hemisphere, a region contaminated by atmospheric fallout due to past nuclear explosions.

Natural radionuclides distribution in the shelf and upper slope off southeast Brazil

In recent decades, Oceanography has been using a variety of radionuclides as tracers to understand the ocean dynamic processes, handling and disposal of sediments of seabed. In this context, the determination of natural radionuclides distributions (238U, 232Th and 40K) has been carried out with sediments samples from the shelf and upper slope off Southeast Brazil using a gamma spectrometry technique. The samples were sliced into strata of 2 cm, dried, ground and properly packed to be analysed. The concentration of activities was performed in a hyperpure Ge detector with a resolution of 1,9 keV for the peak of 1332,3 keV of 60Co, model GEM50P by EGG&ORTEC. The study area is located between latitudes 28°40'S and 23°00'S and extends from Cabo Frio (RJ) to Cabo de Santa Marta Grande (SC). The activity concentrations varied from 0,6 to 52,8 BqKg-1 for 238U, from 1,6 to 50,9BqKg-1 for 232Th and from 65,4 to 873,3 BqKg-1 for 40K. From these results it is possible to establish a correlation between the depositional area dynamics and the samples size parameters

Application of 137Cs and 210Pb radionuclides to determine sedimentation rates of recent sediments from admiraty Bay, Antarctica Peninsula

Studies about natural and artificial radionuclides in areas such as the Antarctic are key to understand natural and dynamic processes in marine environments. These studies are important to determine levels of radioactive elements and local sedimentation rates. Five marine sediment cores were collected in different points of Admiralty Bay, in the Antarctic Peninsula. The purpose of this study was to determine 137Cs, 226Ra and 210Pb and sedimentation rates at each site. 137Cs, 210Pb and 226Ra were assayed by gamma-counting through direct measurement of the peak at 661 keV, 47 keV and 609 keV, respectively. Sedimentation rates were obtained by 137Cs and 210Pb (CIC and CRS). The activities for 137Cs ranged from 0.84 to 7.09 Bq kg-1; to 226Ra from 6.77 to 31.07 Bq kg-1 and for 210Pb ranged from 1.10 to 36.90 Bq kg-1. The sedimentation rates obtained by the three models ranged from 0.11±0.01 cm y-1 to 0.46±0.05 cm y-1. The levels of 137Cs registered in this study, as well as in other studies in the Antarctic region indicate that global fallout is the main cause of artificial radionuclides present in this environment, since the Antarctic has not suffered a direct action of human activities that released radioactive elements. The possible grain size variations that occur in the studied points of Admiralty Bay may explain the differences found in the vertical distribution of radionuclides, because of the different values of sedimentation rates and respective dating determined in their profiles