Síntese de sulfadiazina e sulfadiazina de prata em escala semi-micro: prática experimental em síntese de fármacos

The total synthesis of sulfadiazine and silver sulfadiazine from readily available starting materials was adapted to semi-micro laboratory scale and is proposed as an experiment in drug synthesis for undergraduate courses.

alfa e b-glucosidases como alvos moleculares para desenvolvimento de fármacos

Glucosidases are involved in key steps in the processing of oligosaccharides by cleaving O-glucose residues. Since they catalyze breaking and transfer reactions of glucosidic groups for the normal growth and development of all the cells, defects or genetic deficiencies in these enzymes are associated with serious disorders of the carbohydrate metabolism. Thus, glucosidases represent important targets to develop inhibitors, owing to their potential activities against viruses, tumoral growth and metastasis, diabetes, Gaucher's disease and other syndromes associated with the lisosomal storage of glucoesphingolipids, and osteoarthritis. This paper presents a description of the biochemical pathways and mechanisms of alpha and beta-glucosidases, and the currently available drugs capable to inhibit these enzymes.

Estatinas hipolipêmicas e novas tendências terapêuticas

Statins are the most used drugs for the treatment of hyperlipidemia in primary and secondary prevention, with the aim of decreasing the levels of plasmatic cholesterol- lipoproteins. Owing to their structural similarity to the substrate HMG-CoA (3-hydroxy-3-methylglutaryl-CoA), they inhibit the HMG-CoA reductase enzyme, disrupting the cholesterol biosynthesis. Currently, six therapeutic statins are available: lovastatin (Mevacor) and pravastatin (Pravachol), which are natural, sinvastatin (Zocor), a semi-synthetic derivative, and the totally synthetic statins, fluvastatin (Lescol), atorvastatin (Lipitor) and rosuvastatin (Crestor). Recent investigations have showed other important effects of statins, such as antineoplastic action and improvement in endothelial function.

Avaliação da influência da operação da termoelétrica a carvão na concentração dos metais e as no solo de Figueira, PR - Brasil

The aim of this work is to study metal and As concentrations in soil due to ash deposition from a coal plant at Figueira (PR), evaluating the macroelement (Al, Ca, Fe, Mg, Mn, Ti, V) and microelement (As, Cd, Co, Cr, Cu, Mo, Ni, Pb, Zn) concentrations in the soil around the coal plant. The plant operation caused a slight increase in the majority of the metal concentrations in the top soil close to the plant (up to 1 km) in the wind direction (NW). The elements As, Cd, Mo, Pb and Zn are considered likely soil pollutants, and As is considered the only critical element.

Síntese de glicoaminoácidos de interesse biológico

This work describes the synthesis of the glycosylated amino acids αGlcNAc-Thr, βGlcNAc-Thr and αLacNAc-Thr by the glycosylation reaction of the amino acid threonine with the corresponding glycosyl donors αGlcNAcCl and αLacN3Cl. The glycosylated amino acids containing the sugar units α-D-GlcNAc and α-D-LacNAc O-linked to threonine amino acids are related to O-glycans found in mucins of the parasite Trypanosoma cruzi, while the corresponding β-D-GlcNAc isomer is involved in cellular signaling events.

Determinação de paládio em amostras biológicas aplicando técnicas analíticas nucleares

This study presents Pd determinations in bovine tissue samples containing palladium prepared in the laboratory, and CCQM-P63 automotive catalyst materials of the Proficiency Test, using instrumental thermal and epithermal neutron activation analysis and energy dispersive X-ray fluorescence techniques. Solvent extraction and solid phase extraction procedures were also applied to separate Pd from interfering elements before the irradiation in the nuclear reactor. The results obtained by different techniques were compared against each other to examine sensitivity, precision and accuracy.

Extração seletiva de metais pesados em sedimentos de fundo do Rio Tietê, São Paulo

Sediment samples from Tietê river were submitted to chemical and sequential extractions of heavy metals (Cd, Cr, Cu, Ni, Pb and Zn). It was followed a single extraction by using 0.1 mol L-1 hydrochloric acid and a sequential procedure to evaluate possible chemical associations described as exchangeable, carbonate, reducible oxides, sulfide, organic matter and residual fractions. High concentrations of heavy metals were determined at Pirapora reservoir, which is closer to the Metropolitan Area of São Paulo while for Barra Bonita reservoir, the results showed low concentrations for such elements. Acid volatile sulfides, grain size distribution and carbon contents were also determined.

Análise de pesticidas organoclorados em água usando a microextração em fase sólida por headspace com cromatografia gasosa e espectrometria de massas

A method based on headspace - solid phase microextraction coupled with gas chromatography - mass spectrometry was validated for the quantitative determination of 18 organochlorine pesticides in water. For the extraction conditioning some parameters as the best type of coating fiber, time and temperature of extraction, pH and ionic strength were evaluated. The method HS-SPME/GC-MS/MS showed linear coefficient above 0.9948. The repeatability of the measurements were lower than 7.6%. Relative recoveries were between 88 and 110%. Limits of detection from 0.5 x 10-3 to 1.0 mg L-1 were obtained. A total of 31 samples were analyzed and 16 presented from 1 to 5 pesticides.

Métodos para análises de HPA e BTEX em águas subterrâneas de postos de revenda de combustíveis: um estudo de caso em Campo Grande, MS, Brasil

Two methods using headspace solid-phase microextraction and gas chromatography - mass spectrometry were developed for the determination of polycyclic aromatic hydrocarbons (PAH) and BTEX. Best results were obtained using DVB/CAR/PDMS fiber, with 10 min extraction at 25 °C and 0.15 min desorption at 260 °C (BTEX), and PDMS/DVB fiber, with 60 min extraction at 90 °C, 10% NaCl and 5 min desorption at 270 °C (PAH). LOD intervals were 3x10-2 - 5x10-2 µg L-1 (BTEX) and 1.6x10-3 - 1.4 µg L-1 (PAH). The methods were applied to forty-five groundwater samples from monitoring wells of gas stations and only benzene level exceeded the limit established by Brazilian regulations.

POPULATION STRUCTURE AND PRODUCTION OF COPAIBA OLEORESIN BETWEEN VALLEYS AND HILLSIDES OF THE MINING AREA OFTROMBETAS RIVER - PARÁ1

ABSTRACT We aimed in this work to study natural populations of copaiba (Copaifera multijuga Hayne) on the Monte Branco mountain at Porto Trombetas-PA, in order to support sustainable management and the exploitation of oleoresin from copaiba. We studied the population structure of copaiba on hillsides and valleys of the south face of Monte Branco, within Saracá Taquera National Forest, where bauxite ore was extracted in the biennium 2013-2014 by Mineração Rio do Norte (MRN). We produced a 100% forest inventory of the specie and of oleoresin extraction in order to quantify the potential production of the remaining area. The density of copaiba individuals with DBH > 30 cm was 0.33 individuals per hectare in the hillside and 0.25 individuals per hectare in the valley. Both environments presented a density of 0.28 individuals per hectare. The average copaiba oleoresin yield was 0.661±0.334 liters in the hillside and 0.765±0.280 liters in the valley. The average value of both environments together (hillside and valley) was 0.714±0.218 liters. From all individuals with DBH over 30 cm, 38 (58%) produced some amount of oleoresin, averaging 1.113±0.562 liters in the hillside, 1.329±0.448 liters in the valley and 1.190±0.355 liters in both environments together. The results show the need for planning the use of the surroundings of the study area in order to reach the required volume of copaiba to make feasible the sustainable management of oleoresin extraction in the region.

Uso racional de modelos animais para pesquisa e ensino de microcirurgia

O objetivo deste estudo é divulgar um modelo experimental de baixo custo, que respeita as normas regulamentadoras das experiências com animais Utilizando animais mortos em outros experimentos contribuindo com a melhora do aprendizado de microcirurgia. São utilizados cadáveres de ratos da raça Wistar, oriundo de descarte de outros cursos. Os cadáveres dos ratos descongelados são utilizados para o treinamento básico de microcirurgia dos acadêmicos do curso de medicina da Universidade Nove de Julho, visando contribuir para o treinamento de acadêmicos, sua utilização se justifica pelo baixo custo do material empregado e muitos animais são poupados durante a fase intermediária do desenvolvimento de habilidades para realização das micro-anastomoses. Este modelo experimental é de baixo custo e permite a utilização racional de animais, corroborando com as normas éticas da pesquisa experimental e contribuindo com o ensino e treinamento da microcirurgia.

Associação entre o escore do International Consultation on Incontinence Questionaire: Urinary Incontinence/Short Form e a Avaliação Urodinâmica em mulheres com incontinência urinária

OBJETIVO: Avaliar a correlação entre o International Consultation on Incontinence Questionnaire - Urinary Incontinence/Short Form (ICIQ-UI/SF) e a Avaliação Urodinâmica (AU) em mulheres com incontinência urinária (IU). MÉTODOS: Foram analisados retrospectivamente dados clínicos, AU e escore do ICIQ-UI/SF de 358 mulheres com IU atendidas em clínica privada. O teste de correlação entre ICIQ-UI/SF e os parâmetros urodinâmicos foi o teste de Spearman. Foi utilizada a curva ROC, com os valores de sensibilidade e especificidade dos escores do ICIQ-UI/SF apresentados pelas pacientes, para identificar o valor do questionário que determinasse a presença da alteração urodinâmica estudada. Para o cálculo do valor p foi utilizado o teste do c² ou exato de Fisher. O nível de significância foi de 5% e o software utilizado para análise foi o SAS versão 9.2. RESULTADOS: As pacientes com IU aos Esforços segundo a AU - IUE urodinâmica - representaram 67,3% do total; aquelas com IUE na AU e Hiperatividade Detrusora (HD) - IUM urodinâmica - 16,2%, e as pacientes com HD isolada - HD - 7,3% do total. As pacientes com AU normal representaram 9,2% do total da amostra. Houve associação significativa entre escore ³14 no ICIQ-UI/SF e as pacientes com IUE urodinâmica e IUM urodinâmica. Pacientes com Pressão de Perda ao Esforço (PPE) £90 cmH2O apresentaram escore ao ICIQ-UI/SF³15. O teste de Spearman mostrou correlação inversa fraca entre o escore e a PPE, porém não mostrou correlação entre esse escore e a Capacidade Cistométrica Máxima (CCM) ou com o volume vesical no primeiro desejo miccional. CONCLUSÃO: Houve associação entre o escore do ICIQ-UI/SF e IUE urodinâmica (isolada ou associada à HD); porém não houve associação com a HD isolada. Quanto menor o valor da PPE, maior o escore total do ICIQ-UI/SF. O ICIQ-UI/SF não foi capaz de discriminar o tipo de IU na população estudada.

Expression and distribution of connexin 32 in rat liver with experimentally induced fibrosis

The connexin 32 (Cx32) is a protein that forms the channels that promote the gap junction intercellular communication (GJIC) in the liver, allowing the diffusion of small molecules through cytosol from cell-to-cell. Hepatic fibrosis is characterized by a disruption of normal tissue architeture by cellular lesions, and may alter the GJIC. This work aimed to study the expression and distribution of Cx32 in liver fibrosis induced by the oral administration of dimethylnitrosamine in female Wistar rats. The necropsy of the rats was carried out after five weeks of drug administration. They presented a hepatic fibrosis state. Sections from livers with fibrosis and from control livers were submitted to immunohistochemical, Real Time-PCR and Western-Blot analysis to Cx32. In fibrotic livers the Cxs were diffusely scattered in the cytoplasm, contrasting with the control livers, where the Cx32 formed junction plaques at the cell membrane. Also it was found a decrease in the gene expression of Cx32 without reduction in the protein quantity when compared with controls. These results suggest that there the mechanism of intercellular communication between hepatocytes was reduced by the fibrotic process, which may predispose to the occurrence of a neoplastic process, taken in account that connexins are considered tumor suppressing genes.

Polygala extraaxillaris: oxidative stress in Brachiaria decumbens mediated by volatile oils

The volatile oils extracted from the roots of Polygala extraaxillaris were analyzed to assess whether they increase oxidative stress in Brachiaria decumbens var. Piatã, as well as to assess their effect on cellular division and cytotoxicity in laboratory. Six concentrations were used (0%, 0.35%, 0.65%, 1.25%, 0.65%, and 5.0%) with four repetitions of 25 seeds. The substance 1-(2-hydroxyphenyl) - ethanone was identified as the major constituent of the volatile oils. The results showed that the highest concentrations of the oils resulted in an increase in the oxidative stress in B. decumbens, as well as alteration in germination and growth, with a consequent reduction in the process of cellular division, causing changes in the growth standard and antioxidant defense.

Hormone replacement therapy increases levels of antibodies against heat shock protein 65 and certain species of oxidized low density lipoprotein

Hormone replacement therapy (HRT) reduces cardiovascular risks, although the initiation of therapy may be associated with transient adverse ischemic and thrombotic events. Antibodies against heat shock protein (Hsp) and oxidized low density lipoprotein (LDL) have been found in atherosclerotic lesions and plasma of patients with coronary artery disease and may play an important role in the pathogenesis of atherosclerosis. The aim of the present study was to assess the effects of HRT on the immune response by measuring plasma levels of antibodies against Hsp 65 and LDL with a low and high degree of copper-mediated oxidative modification of 20 postmenopausal women before and 90 days after receiving orally 0.625 mg equine conjugate estrogen plus 2.5 mg medroxyprogesterone acetate per day. HRT significantly increased antibodies against Hsp 65 (0.316 ± 0.03 vs 0.558 ± 0.11) and against LDL with a low degree of oxidative modification (0.100 ± 0.01 vs 0.217 ± 0.02) (P<0.05 and P<0.001, respectively, ANOVA). The hormone-mediated immune response may trigger an inflammatory response within the vessel wall and potentially increase plaque burden. Whether or not this immune response is temporary or sustained and deleterious requires further investigation.