Differential behavioral outcomes of 3,4-methylenedioxymethamphetamine (MDMA-ecstasy) in anxiety-like responses in mice

Anxiolytic and anxiogenic-like behavioral outcomes have been reported for methylenedioxymethamphetamine (MDMA or ecstasy) in rodents. In the present experiment, we attempted to identify behavioral, hormonal and neurochemical outcomes of MDMA treatment to clarify its effects on anxiety-related responses in 2-month-old Balb/c male mice (25-35 g; N = 7-10 mice/group). The behavioral tests used were open field, elevated plus maze, hole board, and defensive behavior against predator odor. Moreover, we also determined striatal dopamine and dopamine turnover, and serum corticosterone levels. MDMA was injected ip at 0.2, 1.0, 5.0, 8.0, 10, or 20 mg/kg. MDMA at 10 mg/kg induced the following significant (P < 0.05) effects: a) a dose-dependent increase in the distance traveled and in the time spent moving in the open field; b) decreased exploratory activity in the hole board as measured by number of head dips and time spent in head dipping; c) increased number of open arm entries and increased time spent in open arm exploration in the elevated plus maze; d) increased time spent away from an aversive stimulus and decreased number of risk assessments in an aversive odor chamber; e) increased serum corticosterone levels, and f) increased striatal dopamine level and turnover. Taken together, these data suggest an anxiogenic-like effect of acute MDMA treatment, despite the fact that behavioral anxiety expression was impaired in some of the behavioral tests used as a consequence of the motor stimulating effects of MDMA.

Determinação de 3,4-metilenodioximetanfetamina (MDMA) em comprimidos de Ecstasy por cromatografia líquida de alta eficiência com detecção por fluorescência (CLAE-DF)

This paper describes the development and validation of simple and selective analytical method for determination of 3.4-methylenedioxymethamphetamine (MDMA) in Ecstasy tablets, using high performance liquid chromatography with fluorescence detection. Analysis was performed in a reversed phase column (LiChrospher 100 C18, 150 x 4.6 mm, 5 µm), isocratic elution with phosphate buffer 25 mmol/L pH 3.0 and acetonitrile (95:5, v/v). The method presents adequate linearity, selectivity, precision and accuracy. MDMA concentration in analyzed tablets showed a remarkable variability (from 8.5 to 59.5 mg/tablet) although the tablet weights were uniform, indicating poor manufacturing control thus imposing additional health risks to the users.

Ultrastructural alterations of intracellular stages and effects on blood forms of Trypanosoma cruzi induced in vivo by 2-amino-5-(1-methyil-5-nitro-2-imidazolyl)-1,3,4 - Thiadiazole

An electron microscopy study shows that the administration of a single dose (500 mg/kg, p.o.) of 2-amino-5-(1-methyl-5-nitro-2-imidazolyl)-1, 3, 4-thiadiazole induces in mice infected with Trypanosoma cruzi results in degenerative lesions of the intracellular stages. Ultrastructural alterations are detected as early as 6 hours after the drug administration and destruction of the parasites occurs within 18 - 36 hours. Trypomastigotes are cleared from the bloodstream 4 to 6 hours after treatment. The combined effect on both developmental stages is apparently responsible for the in vivo ejfects of this drug which is the most active drug ever tested in our laboratory in experimental Chagas' disease.

Modification of oxidative status in Plasmodium berghei-infected erythrocytes by E-2-chloro-8-methyl-3-[(4'-methoxy-1'-indanoyl)-2'-methyliden]-quinoline compared to chloroquine

E-2-chloro-8-methyl-3-[(4'-methoxy-1'-indanoyl)-2'-methyliden]-quinoline (IQ) is a new quinoline derivative which has been reported as a haemoglobin degradation and ß-haematin formation inhibitor. The haemoglobin proteolysis induced by Plasmodium parasites represents a source of amino acids and haeme, leading to oxidative stress in infected cells. In this paper, we evaluated oxidative status in Plasmodium berghei-infected erythrocytes in the presence of IQ using chloroquine (CQ) as a control. After haemolysis, superoxide dismutase (SOD), catalase, glutathione cycle and NADPH + H+-dependent dehydrogenase enzyme activities were investigated. Lipid peroxidation was also assayed to evaluate lipid damage. The results showed that the overall activities of glucose-6-phosphate dehydrogenase and 6-phosphogluconate dehydrogenase were significantly diminished by IQ (by 53.5% and 100%, respectively). Glutathione peroxidase activity was also lowered (31%) in conjunction with a higher GSSG/GSH ratio. As a compensatory response, overall SOD activity increased and lipid peroxidation decreased, protecting the cells from the haemolysis caused by the infection. CQ shared most of the effects showed by IQ; however it was able to inhibit the activity of isocitrate dehydrogenase and glutathione-S-transferase. In conclusion, IQ could be a candidate for further studies in malaria research interfering with the oxidative status in Plasmodium berghei infection.

Efectividad del 3,4- dimetilpirazolfosfato (DMPP) en naranjo dulce en el noreste Argentino

El objetivo del trabajo fue evaluar el efecto del 3,4-dimetilpirazol fosfato (DMPP) en la eficiencia de la fertilización amoniacal, en naranjo dulce [Citrus sinensis (L.) Osbeck] 'Valencia late' sobre suelo arenoso, en la provincia de Corrientes, Argentina. Durante tres campañas se trabajó en un huerto de naranjo 'Valencia late' injertado sobre lima de Rangpur (Citrus limonia, Osbeck), sobre un suelo tipo Udipsamment alfico. Se utilizó un Diseño de Bloques Completos al Azar con cuatro repeticiones, parcela útil una planta más borduras, con los tratamientos: 1. (Testigo) 150 kg de N ha-1 (fertilizante 15-6-15-6); T2. 75 kg de N ha-1 (sulfonitrato de amonio (SNA) 26 % N) tratado con DMPP (0,8% respecto al N amoniacal); T3. 150 kg de N ha-1 (SNA 26 % N), tratado con DMPP (0,8% respecto al N amoniacal). En el otoño se tomaron muestras foliares de ramas fructíferas, determinándose contenido de N, P y K. En la cosecha se determinó producción por planta (kg) y se evaluó calidad de frutos. Los resultados obtenidos permiten establecer que en suelos arenosos, el agregado de DMPP mejora la eficiencia de la fertilización nitrogenada. Con igual aporte nitrogenado, se incrementan los rendimientos y las concentraciones foliares de N y con la mitad de la dosis se logran rendimientos equivalentes al testigo.

Valores preditivos das categorias 3, 4 e 5 do sistema BI-RADS em lesões mamárias nodulares não-palpáveis avaliadas por mamografia, ultra-sonografia e ressonância magnética

OBJETIVO: Avaliar os valores preditivos positivo e negativo das categorias 3, 4 e 5 do sistema BI-RADS™ em lesões mamárias nodulares não-palpáveis avaliadas por mamografia, ultra-sonografia e ressonância magnética. MATERIAIS E MÉTODOS: Vinte e nove pacientes com achados mamográficos de lesões mamárias nodulares não-palpáveis, das classes 3, 4 e 5 do BI-RADS, que realizaram exames complementares de ultra-sonografia e ressonância magnética, além de biópsia excisional. Realizaram-se 30 biópsias e correlacionaram-se as lesões e suas respectivas classificações de 3 a 5 do BI-RADS com os resultados histopatológicos. O cálculo dos valores preditivos foi feito utilizando-se equações matemáticas específicas. RESULTADOS: O valor preditivo negativo da categoria 3 pela análise mamográfica foi de 69,23%, pela análise ultra-sonográfica foi de 70,58% e pela análise por ressonância magnética foi de 100%. O valor preditivo positivo da categoria 4 pela análise mamográfica foi de 63,63%, pela análise ultra-sonográfica foi de 50% e pela análise por ressonância magnética foi de 30,76%. O valor preditivo positivo da categoria 5 foi de 100% pelas análises mamográfica e ultra-sonográfica e de 92,85% pela análise por ressonância magnética. CONCLUSÃO: O valor preditivo negativo da categoria 3 foi elevado na análise pela ressonância magnética e os valores preditivos positivos foram moderados na categoria 4 e elevados na categoria 5 pelos três métodos.

Breast Imaging Reporting and Data System - BI-RADS®: valor preditivo positivo das categorias 3, 4 e 5. revisão sistemática da literatura

OBJETIVO: Avaliar artigos, na literatura, que verificam o valor preditivo positivo das categorias 3, 4 e 5 do Breast Imaging Reporting and Data System (BI-RADS®). MATERIAIS E MÉTODOS: Foi realizada pesquisa na base de dados Medline utilizando os termos "predictive value" e "BI-RADS". Foram incluídos 11 artigos nesta revisão. RESULTADOS: O valor preditivo positivo das categorias 3, 4 e 5 variou entre 0% e 8%, 4% e 62%, 54% e 100%, respectivamente. Três artigos avaliaram, concomitantemente, os critérios morfológicos das lesões que apresentaram maior valor preditivo positivo na mamografia, sendo nódulo espiculado o critério com maior valor preditivo positivo. CONCLUSÃO: Houve grande variabilidade do valor preditivo positivo das categorias 3, 4 e 5 do BI-RADS® em todos os estudos, porém foram identificadas diferenças metodológicas que limitaram a comparação desses estudos.

Valor preditivo positivo das categorias 3, 4 e 5 do Breast Imaging Reporting and Data System (BI-RADS®)

OBJETIVO: O objetivo deste trabalho foi avaliar o BI-RADS® como fator preditivo de suspeição de malignidade em lesões mamárias não palpáveis nas categorias 3, 4 e 5, correlacionando as mamografias com os resultados histopatológicos através do cálculo do valor preditivo positivo do exame mamográfico. MATERIAIS E MÉTODOS: Trezentas e setenta e uma pacientes encaminhadas a um serviço de referência em tratamento de câncer em Teresina, PI, para realização de exames histopatológicos em mama no período de julho de 2005 a março de 2008, por terem mamografia de categorias 3, 4 ou 5, tiveram seus exames revisados. Das 371 pacientes, 265 foram submetidas a biópsia por agulha grossa e 106, a marcação pré-cirúrgica. RESULTADOS: Em relação às mamografias, 11,32% foram classificadas como categoria 3, 76,28% como categoria 4 e 12,4% como categoria 5. Os resultados histológicos demonstraram 24% de exames positivos para malignidade. Os valores preditivos positivos das categorias 3, 4 e 5 foram, respectivamente, de 7,14%, 16,96% e 82,61%. Foram calculados os valores preditivos positivos, separadamente, para as biópsias percutâneas (7,14%, 15,76%, 76,47%) e para as marcações pré-cirúrgicas (7,14%, 20%, 100%). CONCLUSÃO: Achados malignos foram subestimados pelo laudo radiológico e houve superestimação de achados benignos, o que resultou na realização desnecessária de alguns procedimentos invasivos.

Positive predictive values of Breast Imaging Reporting and Data System (BI-RADS®) categories 3, 4 and 5 in breast lesions submitted to percutaneous biopsy

Objective To evaluate the BI-RADS as a predictive factor of suspicion for malignancy in breast lesions by correlating radiological with histological results and calculating the positive predictive value for categories 3, 4 and 5 in a breast cancer reference center in the city of São Paulo. Materials and Methods Retrospective, analytical and cross-sectional study including 725 patients with mammographic and/or sonographic findings classified as BI-RADS categories 3, 4 and 5 who were referred to the authors' institution to undergo percutaneous biopsy. The tests results were reviewed and the positive predictive value was calculated by means of a specific mathematical equation. Results Positive predictive values found for categories 3, 4 and 5 were respectively the following: 0.74%, 33.08% and 92.95%, for cases submitted to ultrasound-guided biopsy, and 0.00%, 14.90% and 100% for cases submitted to stereotactic biopsy. Conclusion The present study demonstrated high suspicion for malignancy in lesions classified as category 5 and low risk for category 3. As regards category 4, the need for systematic biopsies was observed.

Cicloadições [3+4] via cátions oxialílicos: aplicações em sínteses orgânicas

Several methodologies for the generation of oxyallyl cations from polybromoketones and other substrates are discussed. The mechanistic aspect of the [3+4] cycloaddition reaction between these cations and dienes leading to the formation of seven membered ring carbocyclic compounds is presented. Finally, some synthetic applications of the [3+4] cycloaddition are shown.

Análise das isotermas de adsorção de Cu(II), Cd(II), Ni(II) e Zn(II) pela N-(3,4-dihidroxibenzil) quitosana empregando o método da regressão não linear

Adsorption of Cu(II), Ni(II), Pb(II) and Zn(II) ions from aqueous solutions by N-(3,4-dihydroxybenzyl) chitosan have been carried out. The Langmuir (L), Freundlich (F), Langmuir - Freundlich (LF), Redlich-Peterson (RP) and Tóth (T) adsorption isotherms models have been applied to fit the experimental data. Nonlinear regression computational program "Enzefitte", which is a library of the more commonly used adsorption isotherm equations for obtaining tabular outuput suitable for plotting theoretical of fitted isotherms, has been used to estimate the adsorption parameters. These parameters were used to calculate the amount adsorbed q calc., a function of concentration (C).

Síntese e atividade antibacteriana de imidas cíclicas: 3,4-dicloromaleimidas e 3-cloro-4-substituída-maleimidas

In the present study, new N-aryl and N-alkylarylcyclic imides were synthesized and their antibacterial properties against Escherichia coli and Staphylococcus aureus were evaluated by using the diffusion method. All compounds were obtained in good yield (54 - 95%) and characterized by spectral data (¹H-NMR, MS, IR) and elemental analysis (CHN). The biological results indicated that some compounds exert significative antibacterial effects, confirming previous studies on biological activities of cyclic imides.

Novos derivados do sistema heterocíclico 1H-pirazolo[3,4-b]piridina: síntese e assinalamentos de hidrogênios e carbonos por RMN 1D e 2D

The synthesis and NMR analysis of seven new 4-(aryl)amino-5-carboethoxy-1,3-dimethyl-1H-pyrazolo[3,4- b]pyridines (7-13) are described. The synthetic approach used involved the preparation of intermediates 5-aminopyrazol (4), the enamine derivative (5) and the 4-chloro-1H-pyrazolo[3,4-b]pyridine (6). Compounds (7-13) were obtained by treatment of 6 with the desired aniline. The structures of new heterocyclic compounds and their precursors intermediates were assigned on the basis of spectral analysis including 1D and 2D NMR experiments [¹H; 13C{¹H} and DEPT; ¹H x ¹H - COSY; ¹H x13C - COSY, nJ CH, n = 1, 2 or 3 (HETECOR and COLOC)].

Mechanism of 3,4-dihydroxybenzaldehyde electropolymerization at carbon paste electrodes: catalytic detection of NADH

Cyclic voltammetry was used to study 3,4-dihydroxybenzaldehyde (3,4-DHB) electropolymerization processes on carbon paste electrodes. The characteristics of the electropolymerized films were highly dependent on pH, anodic switching potential, scan rate, 3,4-DHB concentrations and number of cycles. Film stability was determined in citrate/phosphate buffer solutions at the same pH used during the electropolymerization process. The best conditions to prepare carbon paste modified electrodes were pH 7.8; 0.0 <= Eapl <= 0.25 V; 10 mV s-1; 0.25 mmol L-1 3,4-DHB and 10 scans. These carbon paste modified electrodes were used for NADH catalytic detection at 0.23 V in the range 0.015 <= [NADH] <= 0.21 mmol L-1. Experimental data were used to propose a mechanism for the 3,4--DHB electropolymerization processes, which involves initial phenoxyl radical formation.

Ácido canárico (3,4-seco derivado do lupano) em própolis do Ceará

Phytochemical investigation of a propolis sample from Alto Santo - Ceará, Brazil, allowed identification of triterpenes (lupeol, lupenone, germanicone, canaric acid) and flavonoids (quercetin, kaempferol and acacetin), which were identified by spectroscopic data (IR, MS, and NMR, including 2D techniques). This is the first report of canaric acid in propolis. Propolis extract and flavonoids showed antioxidant activity using a DPPH radical scavenging assay.