CNS-selective noncompetitive cholinesterase inhibitors derived from the natural piperidine alkaloid (-)-spectaline

LASSBio-767 [(-)-3-O-acetyl-spectaline] and LASSBio-822 [(-)-3-O-tert-Boc-spectaline] were recently described as cholinesterase inhibitors derived from the natural piperidine alkaloid (-)-spectaline, obtained from the flowers of Senna spectabilis (Fabaccae). We investigated their mechanism of inhibition of acetylcholinesterase and their efficacy in reversing scopolamine-induced amnesia. Competition assays with the substrate acetylthiocholine showed a concentration-dependent reduction in rat brain cholinesterase V-max without changes in apparent K-m. The kinetic data for LASSBio-767 and LASSBio-822 were best fit by a model of simple linear noncompetitive inhibition with K-i of 6.1 mu M and 7.5 mu M, respectively. A dilution assay showed a fast and complete reversal of inhibition, independent of incubation time. Simulated docking of the compounds into the catalytic gorge of Torpedo acetylcholinesterase showed interactions with the peripheral anionic site, but not with the catalytic triad. Anti-amnestic effects in mice were assessed in a step-down passive avoidance test and in the Morris water maze 30 min after injection of scopolamine (1 mg/kg i.p.). Saline, LASSBio-767, or LASSBio-822 was administered 15 min before scopolamine. Both compounds reversed the scopolamine-induced reduction in step-down latency at 0.1 mg/kg i.p. LASSBio-767 reversed scopolamine-induced changes in water maze escape latency at 1 mg/kg i.p. or p.o., while its cholinergic side effects were absent or mild up to 30 mg/kg i.p. (LD50 above 100 mg/kg i.p.). Thus, the (-)-spectaline derivatives are potent cholinergic agents in vivo, with a unique profile combining noncompetitive cholinesterase inhibition and CNS selectivity, with few peripheral side effects. (C) 2007 Elsevier B.V. All rights reserved.

Penicillium expansum versus antagonist yeasts and patulin degradation in vitro

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Morphology of eggs of Dioctophyme renale Goeze, 1782 (Nematoda: Dioctophymatidae) and influences of temperature on development of first-stage larvae in the eggs

Este estudo teve a finalidade de fornecer dados morfológicos de ovos de D. renale e do desenvolvimento de larvas de primeiro estádio em ovos mantidos em diferentes temperaturas. Os ovos foram obtidos por centrífugação da urina de cães parasitados e colocados em placas de Petri em estufa BOD, durante 90 dias. O experimento consistiu de três tratamentos (GI - 15 ºC, GII - 20 ºC e GIII - 26 ºC) com cinco repetições cada. Os ovos apresentaram tamanho médio de 67,23 x 42,78 µm, e o tempo médio de incubação foi inversamente proporcional à temperatura de incubação e as larvas apresentaram motilidade por aproximadamente uma semana após sua formação.

Hidrólise da uréia em latossolos: efeito da concentração de uréia, temperatura, pH, armazenamento e tempo de incubação

Este trabalho objetivou estudar a velocidade de hidrólise da uréia em dois diferentes solos brasileiros (Latossolo Vermelho Aluminoférrico típico e Latossolo Vermelho distrófico típico) onde foram realizados ensaios sobre o efeito do tempo e condições de armazenamento, concentração do substrato (uréia), temperatura, pH e tempo de incubação sobre a atividade da urease. As melhores condições de armazenamento foram em temperatura ambiente ou 5 ºC, após secagem ao ar, por um período de até 7 dias; para as condições estudadas, o melhor tempo de incubação foi de uma hora a 25-30 ºC, sem a utilização de tampão para acertar o pH, e a concentração de uréia suficiente foi de 3,30 g L-1, para o Latossolo Vermelho Aluminoférrico típico, e de 2,5 g L-1, para o Latossolo Vermelho distrófico típico para obter a velocidade máxima da enzima.

Quantificação de bactérias totais e esporuladas no solo

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Degradação ruminal de silagem de capim-elefante com adição de vagem de algaroba triturada

This research was carried out to evaluate the ruminal degradation of dry matter (DM), crude protein (CP) and neutral detergent fiber (NDF) of silages of elephant grass (Pennisetum purpureum) cutting in 70; 90 and 110 days after regrowth with inclusion of 0; 5; 10 and 15% of mesquite (Prosopis juliflora) meal, based on natural matter in a completely randomized design, in split plot arrangement. Samples of silages were incubated in the rumen of two Jersey cows for 3; 6; 12; 24; 48; 72 and 96 h, and the bags at time "zero" were only washed with water to determine the soluble fraction. There was not interaction (P> 0.05) incubation time x inclusion of mesquite pods x cutting age of the grass for DM degradability, there was only interaction (P <0.05) between these factors for CP and NDF degradability. The most effective DM degradability (42.54%) was observed for 15% inclusion of mesquite pods. The effective CP degradability was higher (69.04%) for elephant grass silage with 70 days after regrowth with 15% of mesquite pods. The inclusion of mesquite pods in elephant grass silages improve DM, CP and NDF degradability, while increment of the age after regrowth result in reduction of this parameters.

Breeding biology and nest site characteristics of the scarlet ibis in southeastern Brazil

The breeding biology of the only Scarlet Ibis Eudocimus ruber colony in southeastern Brazil was studied during the 1996-97 breeding season. The ibises began to visit their colony site by mid-September. Nest building and egg laying took place in early November and was synchronous, making the first nesting pulse. Mean clutch size in this pulse was 2.45 eggs/nest, and 0.67 young/nest reached age three weeks, when they were able to walk about the nest tree and environs. Predation was the main cause of nest failures (74% of all losses), followed by nest collapses (19%). A second nesting pulse, also synchronous, started in late December, when the young from the first nests were already able to wander about the colony and make short flights. Mean clutch size of this pulse was 2.05 eggs/nest and productivity was 0.34 young/nest. Nest collapses during storms accounted for 58% of the losses, and predation for a further 27%. A third pulse, with only a few nests, started when the second pulse young were in their third week, but no nest was successful. The incubation time was 21-24 days, and the young were able to fly well when 40 days old, deserting the colony by age 75 days. Nesting early in the breeding season yielded greater success. Nests were built close to each other (a sphere with a 1.8 m radius and centered on an average nest would include the four nearest neighbors) and there was always more than one nest per tree. Most nests were built on the upper third of the nest-tree and had some cover from overhanging branches. There was a trend for the ibises building their nests in even closer proximity during the second pulse, perhaps as a strategy to lessen individual predation risks. Received 30 August 2000, accepted 4 October 2000.

Anti-genotoxic effect of aqueous extracts of sun mushroom (Agaricus blazei Murill lineage 99/26) in mammalian cells in vitro

The sun mushroom is the popular name for the Agaricus blazei Murill fungus, a mushroom native to south-eastern Brazil, which has been frequently used in popular medicine mainly in the form of tea to treat various ailments (stress, diabetes, etc.). In the present study, the genotoxic and/or anti-genotoxic effects ofA. blazei on mammalian cells in culture was assessed by checking the increase or reduction of micronucleus (MN) frequency and comets. The sun mushroom (lineage 99/26) was used as aqueous extracts prepared (2.5%) at three different temperatures (60, 25 and 4°C). The in vitro micronucleus (MN) test in binucleated cells and comet assay were used in V79 cells cultivated in HAM-F10+DMEM medium (1:1), supplemented with 10% of fetal bovine serum. The experiments were divided into four treatment types: 1. Negative control; 2. Positive control with MMS; 3. Treatments with the three forms of extracts (60, 25 and 4°C); and 4. Treatments with the extracts in different associations (simultaneous, pre-treatment, post-treatment and simultaneous after pre-incubation for 1 h) with MMS. None of the A. blazei extracts show genotoxic activity. In the comet assay no protecting effect was found. The results obtained in the MN test showed that the three forms of extracts used had protective activity, suggesting that the compound or active ingredients of A. blazei are always present in these extracts. The greater protective efficiency of the simultaneous treatment and simultaneous treatment with pre-incubation mixture with MMS suggests that the extracts have an antimutagenic action of the desmutagenic type. © 2002 Elsevier Science Ltd. All rights reserved.

Isolamento de fungos produtores de ácido γ-linolênico de solo da Estação Ecologica de Juréia-Itatins, SP

Fungi producing γ-linolenic acid (GLA) were isolated from soil of the Ecological Station of Juréia-Itatins, SP. This essential fatty acid has aroused great interest due to its increasing by applications in pharmaceutical industry. The GLA production by zygomycetous fungi is an alternative way of comparing seed extraction. Thirty-two zygomycetous strains of Mucorales were isolated, most of them belonging to Mucor genus. The GLA production was evaluated after 4 days of incubation at 25°C on a rotary shaker at 150 rpm in medium containing 2% glucose, and 1% yeast extract, following new medium addition (20%) and incubation for an additional period of 3 days at 12°C, without agitation. The GLA production varied according to the microorganism and the strain.

Adesão de protozoários ̀a superfície de dispositivos intra-uterinos

Intrauterine devices (IUD) have been used by approximately hundred million of women in the world. IUD are unprescribed to women who have pelvic inflammation disease predisposition which is caused in general by non-treated sexually transmitted diseases (STD). Trichomoniasis, one of the most important vaginal infections, is caused by a flagellated protozoan, Trichomonas vaginalis, transmitted by sexual contact and also asyntomatic women are able to transmit it. The objective of this work was verify by scanning microscopy the adhesion of this protozoan on plastic and metalic IUD surfaces. IUD fragments were added in Diamond medium containing T. vaginalis and after 3 days at 37°C incubation, they were taken out and treated as necessary for scanning microscopy. The analysis showed showed the adhesion of the protozoans on plastic and metalic IUD surfaces. Even though the IUD were not yet directly associated with high incidence of the inflammation pelvic disease, it would become an infection reservoir of potencial pathogenic organisms.

Effectiveness of Microwave Sterilization on Three Hard Chairside Reline Resins

Purpose: The aim of this study was to evaluate the effectiveness of microwave irradiation sterilization on hard chairside reline resins. Materials and Methods: Specimens of three reline resins (Kooliner, Tokuso Rebase, and Ufi Gel Hard) were fabricated and subjected to ethylene oxide sterilization. The specimens were then individually inoculated (107 cfu/mL) with Tryptic Soy Broth media containing one of the tested microorganisms (C albicans, S aureus, B subtilis, and P aeruginosa). After 48 hours at 37°C, the samples were vortexed for 1 minute and allowed to stand for 9 minutes, followed by a short vortex to resuspend any organisms present. After inoculation, 40 specimens of each material were immersed in 200 mL of water and subjected to microwave irradiation at 650 W for 6 minutes. Forty non-irradiated specimens were used as positive controls. Replicate specimens (25 μL) of suspension were plated at dilutions of 10-3 to 10-6 on plates of selective media appropriate for each organism. All plates were incubated at 37°C for 48 hours. After incubation, colonies were counted, and the data were statistically analyzed by the Kruskal-Wallis test. Twelve specimens of each material were prepared for SEM. Results: All immersed specimens showed consistent sterilization of all the individual organisms after microwave irradiation. SEM examination indicated an alteration in cell morphology after microwave irradiation. Conclusion: Microwave sterilization for 6 minutes at 650 W proved to be effective for the sterilization of hard chairside reline resins.

Assessment of anaerobic sewage sludge quality for agricultural application after metal bioleaching

The effects of metal bioleaching on nutrient solubilization, especially nitrogen and phosphorous, from anaerobically-digested sewage sludge were investigated in this work. The assessment of the sanitary quality of the anaerobic sludge after bioleaching was also carried out by enumerating indicator (total coliforms, fecal coliforms, and fecal streptococci) and total heterotrophic bacteria. The experiments of bioleaching were performed using indigenous sulphur-oxidizing bacteria (Thiobacillus spp.) as inoculum and samples of anaerobically-digested sludge. Nitrogen and phosphorous solubilization from sewage sludge was assessed by measuring, respectively, the concentration of Total Kjeldahl Nitrogen, ammonia, nitrate/nitrite, and soluble and total phosphorous before and after the bioleaching assays. At the end of the experiment, after 4 days of incubation (final pH of 1.4), the following metal solubilization yields were obtained: zinc, 91%; nickel, 87%; copper, 79%; lead, 52%; and chromium, 42%. As a result of sludge acidification, the viable counts of selected indicator bacteria were decreased to below the detection limit (4 × 103 cfu 100 ml-1), followed by an increase in the mineral fraction of nitrogen (from 6 to 10%) and in the soluble fraction of phosphorous (from 15 to 30%). Although some loss of sludge nutrients can occur during solid-liquid separation following bioleaching, its beneficial effects as metal removal and reduction of pathogenic bacteria are sufficient to consider the potential of this treatment before sludge disposal onto agricultural fields.

Estudo biológico e morfométrico dos estádios ninfais de Rhodnius neglectus Lent, 1954 (Hemiptera, Reduviidae)

The following parameters of the biological cycle of the Rhodnius neglectus were determined under a temperature of 28°C and relative humidity of the air varying between 52-94%: a) average period of incubation: 13.67 days; b) rate of the eggs eclosion: 86.18%; c) average period of growth of the 1st, 2nd, 3rd, 4th, 5th instar nymphs: 18.91, 15.19, 21.38, 21.34, 30.43 days, respectively; d) percentage of death in the instar nymphs: 13.82, 18.26, 9.95, 8.78, 15.06% respectively; e) percentage of changes per instar nymphs: 86.18, 81.74, 90.05, 91.22, 84.94% respectively. The morphometric study with the stereoscopic microscope and Leica image analyses system, using the Qwin software, of the five instar nymphs showed that in the five instar nymphs a gradual growth of the head, thorax and abdomen occurs. In all the instars the abdomen is the largest segment. In the four first instars the head is larger than the thorax. In the fifth instar the head and the thorax present equivalent sizes.

Microbiota fúngica de um prédio com laboratórios da região de Araraquara-SP

From September 2000 to January 2001, airborne fungi were isolated from the building of the Clinical Analyses laboratories, including its didactic and research rooms, in Araraquara São Paulo State, Brazil, by using Andersen, MAS-100® (MERCK) machine, with Sabouraud chloramphenicol medium. After 5 days of incubation at 25°C, the colonies of the fungi were counted, resulting in the identification of 21 taxa. Cladophialophora spp. was the most isolated in internal and external environments as well, followed by Penicillium spp. and Mycelia spp. In accordance with the resolution n° 9, January 2003 (ANVISA), fungi considered unacceptable were found in nine internal environments and one of these presented the amount of fungi above of the acceptable limit. Among the obtained fungi, at least 16 taxa were reported as opportunistic, nine were related to plant diseases and seven were associated to allergy problems.