Maria Teresa Jansem de Almeida Catanho

Antiinflammatory property of 3-aryl-5-(n-propyl)-1,2,4-oxadiazoles and antimicrobial property of 3-aryl-5-(n-propyl)-4,5-dihydro-1,2,4-oxadiazoles: Their syntheses and spectroscopic studies

The synthesis of six 3-aryl-5-(n-propyl)-4,5dihydro-1,2,4-oxadiazoles 3a-f has been achieved in a facile manner by the reaction of an appropriate arylamidoxime 1a-f with butyraldehyde 2. Oxidation of 3a-f individually using MnO(2) in CH(2)Cl(2) or sodium hypochlorite in THF/H(2)O furnished 1,2,4-oxadiazoles 4a-f in good to excellent yields. Compounds 4a-f were also evaluated against inflammation. Except 4e, all of them reduced inflammation, however, 4c presented better antiinflammatory activity. A preliminary antimicrobial activity tests of 3a-f showed that these compounds possess activity against some microorganisms. In fact, 3c and 3f have been found to be more effective against Staphylococcus aureus, Mycobacterium smegmatis, and Candida albicans.

The effect of glucantime™ on the labeling of blood constituents with technetium-99m

PURPOSE The labeling of red blood cells (C) with 99mTc is employed in clinical nuclear medicine for a variety of diagnostic procedures. Drugs can alter this labeling method and modify the disposition of the radiopharmaceuticals. In this paper, the influence of glucantime on the labeling of blood constituents with 9mTc was reported. METHODS Blood was withdrawn from rats and incubated with glucantime. Stannous chloride and 99mTc were added. After centrifugation, plasma (P) and (C) were isolated. Samples of P and C were precipitated with TCA 5%, centrifuged and insoluble (IF) and soluble fractions (SF) separated. The percentages of total activity injected (%ATI) in C, IF-P and IF-C were calculated (p < 0.05). RESULTS The %ATI on C decreased from control to following concentrations of glucantime (6.25%; 12.5%; 25%; 50%; 100%), respectively: 94.06 +/- 1.29 (control) to 77.15 +/- 2.79; to 76.68 +/- 1.88; to 75.15 +/- 2.79; to 72.64 +/- 4.40 and to 63.05 +/- 3.84. On IF-C the %ATI decreased from control to all the concentrations of glucantime (3.125%;6.25%; 12.5%; 25%; 50%; 100%), respectively: 93.34 +/- 1.18 (control) to 78.81 +/- 2.76; to 74.76 +/- 4.82; to 74.02 +/- 5.32; to 64.35 +/- 4.82; to 62.81 +/- 1.97 and to 54.55 +/- 3.58. CONCLUSIONS This effect was probably due to products present in this drug that may complex with ions (Sn(+2) and 99mTcO4) or have a direct or indirect effect on intracellular stannous ion concentration.

Avaliação do controle radioquímico do Ricinus communis L. e Tc-99m na marcação de hemácias

Ricinus communis L. belongs to the Euphorbiaceae family, from whose fruits the ricin oil is extracted, highly toxic. In this study it was analyzed the effect of the extract of Ricinus communis L. in the labeling of red blood cells with Tc-99m through the radiochemical control. The results showed that in the radiochemical control through chromatography, it was observed that the extract labeled with Tc-99m showed two fractions with 130.007 and 494.592 cpm, and in the labeling of red blood cells, with %ATI of 61.88 and 41.32% in the fractions 1 and 2. It has been concluded that the extract of Ricinus communis alters the captivating of Tc-99m in vitro, competing with the radioactive material in the possible binding sites of the red blood cells, as well in the capacity of oxidation of the stannous ion or by competition with the pertechnetate ion.

Effect of the extract of Ricinus communis L. on the osmotic fragility, labeling of red blood cells with Technetium-99m and morphology of the cells

The aim of this study was to evaluate the influence of the proteic extract of R. communis on the cell physiology by the osmotic fragility, labeling of the blood elements with the 99mTc and cell morphology. To evaluate the osmotic fragility, the blood samples of the Wistar rats were incubated with the concentrations of R. communis and with the solutions of NaCl (0.4; 0.7; 0.9%). In the labeling of the blood elements procedure, the rat blood was treated with a solution of Tc-99m and TCA at 5%, determining the rate of radioactivity (%ATI) in the plasma (P) and in the red blood cells (RBC). The soluble and insoluble fractions of the plasma were also evaluated. The cells morphology submitted to the extract was evaluated by the optical microscopy (x40). The results indicated that the rate of the hemolysis increased in the presence of 0.125 mg/mL of the extract. There was a decay of 49.69% in the rate of ATI in the insoluble fraction of the cells, with the morphological alterations in the red blood cells. These results suggested that the extract changed the capability of binding of the red blood cells due to the stannous ion oxidation, modifying the cells structure.

Effects of the Electromagnetic field, 60 Hz, 3 µT, on the hormonal and metabolic regulation of undernourished pregnant rats

Epidemiological studies have implicated maternal protein-calorie deficiency as an important public health problem in developing countries. Over the last decades, a remarkable diffusion of electricity and an increased level of the electromagnetic field (EMF) in the environment have characterized modern societies. Therefore, researchers are concerned with the biological effects of 50-60 Hz, EMF. The aim of this paper is to show the effects of EMF of 60 Hz, 3 muT, exposure for two hours per day in the regulation of the hormonal and metabolic concentrations in pregnant rats, which were fed by Regional Basic Diet (RBD) during their pregnancy as compared with pregnant rats fed a standard diet. Pregnant rats exposed to EMF of 60 Hz, 3 muT, over the pregnancy and fed with RBD presented an increase in glucose release when compared with the Group subjected only to the RBD ration. Rats fed RBD presented a decrease in their insulin and cortisol serum levels when compared with the Group fed with casein. The T3 and T4 concentrations presented the greatest variation among the Groups. The relation T4:T3 was much exaggerated in the Group subjected to RDB and exposed to EMF when compared to the others. In conclusion, the group subjected to the association of EMF and undernutrition suffered a decrease in its serum concentration of T4 and T3 when compared to the well-nourished group and the relationship T4:T3 in the former group was almost eighteen-fold the later one.

Influence of a 60 Hz, 3 μT, electromagnetic field on the reflex maturation of wistar rats offspring from mothers fed a regional basic diet during pregnancy

Abstract The aim of the present study was to observe how the exposition of the pregnant rats to the electromagnetic field (EMF), with frequency of 60 Hz, magnetic field of 3 μT for 2 h per day and/or using the so-called regional basic diet (RED) influenced the reflex maturation in their offspring. Four groups were formed: Group A (casein), B (casein and EMF), C (RED) and D (RED and EMF). The diet manipulation occurred during the pregnancy. The reflexes—assessed daily between 12:00 and 14:00—were: palm grasp (PG), righting reflex (RR), cliff avoidance (CA), vibrissae placing (VP), negative geotaxis (NG), auditory startle (AS) and free-fall righting (FFR). The association between EMF and deficient diet caused a delay in all reflexes when compared with Group A. When the diets were compared with both groups exposed to EMF, the delay occurred in the RR, VP, NG and CA in Group D. In the Groups C and A, the delay was observed in RR, CA, VP, NG, AS and PG. In relation to the EMF, Group B differed from Group A in CA, AS, FFR and PG and Group D differed from C in the PG. In conclusion, all the reflexes studied in this research were delayed by the association of the EMF with undernutrition during pregnancy.

Possíveis efeitos adversos dos campos eletromagnéticos (50/60 Hz) em humanos e em animais

Os avancos tecnologicos tem aumentado o numero de equipamentos eletricos e eletronicos, seja nas residencias ou mesmo no ambiente de trabalho, fazendo com que a populacao conviva com grande numero de fontes de irradiacao eletromagnetica, com os mais diversos niveis de potencia e frequencia. Por muitos anos, alguns cientistas e engenheiros acreditaram que o campo eletromagnetico (CEM) com frequencia extremamente baixa nao pudesse causar efeitos e alteracoes significantes no material biologico. O objetivo deste trabalho e verificar os possiveis efeitos adversos dos CEMs em humanos e animais, que foram publicados nos ultimos anos, atraves de uma revisao da literatura disponivel em Medline, revistas nacionais e internacionais e catalogos de obras de referencia na area dos CEM (50/60 Hz). Como resultado foi observado que o CEM (50/60 Hz) e capaz de produzir diversos efeitos adversos em humanos e animais, como por exemplo: disturbios na reproducao, doencas degenerativas, efeitos psiquiatricos e psicologicos, alteracoes citogeneticas, alteracoes no sistema cardiovascular, nervoso e neuroendocrino, bem como nos parâmetros biologicos e bioquimicos. Apesar de todas estas constatacoes e devido a muitas controversias entre varios autores, faz-se necessario um estudo mais especifico e aprofundado sobre o assunto.

An aqueous extract of Vitex agnus castus alters the labeling of blood constituents with technetium-99m

The development of experimental assays to study properties of herbal medicine is worthwhile. Vitex agnus castus (VAC) is utilized in popular medicine and some actions have been attributed to its extract. Blood cells (BC) and plasma proteins are labeled with technetium-99m (Tc-99m) and have been used in nuclear medicine, as in basic research. This procedure uses a reducing agent and stannous ion is utilized. There are reports that drugs can alter this labeling process. The aim of this work was to evaluate the influence of an aqueous extract of VAC on the labeling of blood constituents with Tc-99m. Blood was incubated with VAC, stannous chloride and Tc-99m, as sodium pertechnetate, and centrifuged. Samples of BC and plasma were separated, aliquots of BC and plasma were also precipitated with trichloroacetic acid to obtain soluble and insoluble fractions and the percentage of radioactivity (%ATI) was determined. The results show a statistical (p<0.05) alteration in the %ATI on blood compartments and on the insoluble fractions of plasma and BC. Probably, this extract would have chemical compounds with oxidant properties.

Aspectos reprodutivos e perfil hormonal dos esteróides sexuais do pirarucu, Arapaima gigas (SCHINZ,1822), em condições de cativeiro

The purpose of this study was to characterize the growth, reproduction and hormonal profile of pirarucu, Arapaima gigas, and validate one sexual dimorphism characteristic. The experiment was carried in the fish farm Santo Antonio II, Presidente Figueredo city in the state of Amazonas – Brazil, from February 2004 to February 2005. In the experiment, 24 fishes were selected and divided in three groups, with eight fish in each one. The pirarucus from “A” group were older than four years. In “B” group the fishes were three years old and in “C” group these were two years old. The pirarucus were stocked in 400 m 2 excavated ponds, one pond for each group. Reproductive behavior like feeding interest, fights, pair formation and presence of nest were observed. Blood samples were taken monthly from all fishes during the experiment period, the sexual dimorphism characteristic was observed. Testosterone (T), 17b-estradiol (E 2 ) and 17ahidroxi-progesterona (17aOHP) levels were measured by radioimunoassay (RIA) in solid phase. All males of group “A” and “B” could be identified by an orange mark under the head, and the levels of T validated this data, proving the empirical knowledge of river men. T and E 2 levels of group “A” and “B” picked in the beginning of raining period and the 17αOHP levels were higher in the end of raining period. The levels of these hormones in “C” group fishes followed the tendency of “A” and “B” group hormonal levels, but in lower concentration.

Quantitative structure-activity relationships (QSAR) of 4-amino-2,6-diarylpyrimidine-5-carbonitriles with anti-inflammatory activity

The experimental anti-inflammatory activities of eight 4-amino-2,6-diarylpyrimidine-5-carbonitriles were subjected to a QSAR analysis based on results from B3LYP/6-31G(d,p) and AM1 electronic structure calculations. Principal component analyses and regressions based on these data indicate that potentially more active compounds should have low dipole moment and partition coefficient values and also be affected by the values of the charges of the carbon atoms through which the two aromatic rings are bonded to the pyrimidinic ring. Two new molecules were predicted to be at least as active as those with the highest activities used in the model building stage. One of them, having a methoxy group attached to one of the aromatic rings, was predicted to have an anti-inflammatory activity value of 52.3%. This molecule was synthesized and its experimental activity was found to be 52.8%, in agreement with the AM1 theoretical prediction. This value is 5% higher than the largest value used for modeling.