Pharmacokinetics of hydroxymethylnitrofurazone and its parent drug nitrofurazone in rabbits

The prodrug hydroximethylnitrofurazone (NFOH) presents antichagasic activity with greatly reduced toxicity compared to its drug matrix nitrofurazone (NF). Besides these new characteristics, the prodrug was more active against the parasite T. cruzi amastigotes. These advantages make the prodrug a possible therapeutic alternative for the treatment of both acute and the chronic phase of Chagas disease. However, the knowledge of pharmacokinetic profile is crucial to evaluate the feasibility of a new drug. In this study, our objective was to evaluate the in vivo formation of NF from the NFOH single administration and to evaluate its pharmacokinetic profile and compared it to NF administration. A bioanalytical method to determine the NF and NFOH by LCMS/MS was developed and validated to perform these investigations. Male albino rabbits (n=15) received NF intravenously and orally in doses of 6.35 and 63.5 mg / kg respectively, and NFOH, 80.5 mg / kg orally. The serial blood samples were processed and analyzed by mass spectrometry. The system operated in positive and negative modes for the analites determination, under elution of the mobile phase 50:50 water: methanol. The administration of NFOH allowed the calculation of pharmacokinetic parameters for the prodrug, and the NF obtained from NFOH administration. Using the pharmacokinetic profile obtained from the NF i.v. administration, the oral bioavailability of NF from the administered prodrug was obtained (60.1%) and, as a key parameter in a prodrug administration, should be considered in future studies. The i.v. and oral administrations of NF differ in the constant of elimination (0.04 vs 0.002) and elimination half-life (17.32 min vs 276.09 min) due to the low solubility of the drug that hinders the formation of molecular dispersions in the digestory tract. Still, there was observed no statistical differences were observed between the pharmacokinetic parameters of orally administered NF and NF obtained from NFOH. The calculated area under the curve (AUC 0-∞) showed that the exposure to the parental drug was fairly the same (844.79 vs 566.44) for NF and NF obtained from the prodrug administration. The tendency to higher NF's mean residence time (MRT) as observed in the prodrug administration (956.1 min vs 496.3 min) guarantees longer time for the action of the drug and it allows the expansion of the administration intervals. These findings, added with the beneficial characteristics of the prodrug encourage new efficacy tests towards the clinical use of NFOH.

Involvement of AMPK, IKβα-NFκB and eNOS in the sildenafil anti-inflammatory mechanism in a demyelination model

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Influence of dental chair backrest inclination on the registration of the mandibular position

Varying the inclination of the dental chair backrest might alter the distribution of occlusal contact points. The purpose of this study was to identify the influence of backrest inclination on the registration of the mandibular position. Ten participants aged between 18 and 30 years with a complete permanent dentition, uncompromised motor function, no tooth mobility, and no temporomandibular disorders were selected. To register interocclusal contacts, an autopolymerizing methylmethacrylate device was adapted to the maxillary anterior teeth and a composite resin increment was added to the mandibular central incisors. Contacts were registered with the following variations in the inclination of the dental chair backrest: 90 degrees, 120 degrees, and 180 degrees. A standardized digital photograph was made of each mark in each backrest position, and the images were superimposed to measure the distances in registration from 90 to 120 and from 90 to 180 degrees. Data were analyzed with the Student paired t test (α=.05). When the chair was inclined from the 90-degree to the 120-degree position, the mandible was repositioned posteriorly by a mean of 0.67 mm, but the difference was not statistically significant. When the chair was inclined from the 90-degree to the 180-degree position, however, the mandible was repositioned posteriorly by a statistically significant mean of 1.41 mm. Mandibular position is influenced by increasing inclination, and this influence was statistically significant at a 180-degree incline.

Membrane lipid profile monitored by mass spectrometry detected differences between fresh and vitrified in vitro-produced bovine embryos

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Tradução para o português brasileiro, adaptação transcultural e validação do 3D Assessment of Hand Function

Pós-graduação em Bases Gerais da Cirurgia - FMB

A construção da carreira docente e a identidade do professor

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Manutenção da diversidade agrícola em assentamentos rurais: um estudo de caso em Moji-Mirim - SP, Brasil

Maintenance of agricultural diversity in rural settlements – a case study in Moji-Mirim, São Paulo, Brazil. This paper investigated whether farmers, when established in rural settlements, keep some traditional features with regard to crops diversity and circulation of planting material. Its aims were to make an ethnobotanical survey of species and varieties and analyze the dinamics of seeds and propagules circulation. A total of 139 varieties of food crops (55 species/28 families) were found, being 87% of them intended for self-consumption; 54% of varieties come from Minas Gerais, home state of most respondents. The number of varieties grown per household ranged from 17 to 54. The informal and free circulation of planting material is the most important way of acquisition. The circulation network is very active, showing a potential for the management of crops diversity, with emphasis on the contribution of settlers to the maintenance and valorization of traditional varieties.

Superação de dormência em sementes de messlina (Melissa officinalis L.)

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Effect of feed restriction on body composition and metabolism of goats of different genders

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Calculators in the Classroom: Help or Hindrance?

In a world where technology is ever present and ever changing, is too much technology at too young of an age detrimental to a child’s educational success? The purpose of this paper is to share the results of a four-month study that focused on the use of calculators in grade eight. This study was conducted in an eighth grade class, in a small kindergarten through twelfth grade school. This paper will share the findings of a study of a classroom in which calculator use was limited and mental computation was emphasized. The main focus of this study was whether or not there would be any improvement in the computation skills of my students and how, or if, their problem solving would be affected. As a result of this research project, I plan to permanently limit calculator use in grades seven and eight, as well as to implement a computational review that will be conducted yearly with all of my classes.

Effect of feed restriction on body composition and metabolism of goats of different genders

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

ICHTHYOFAUNA IN AN ESTUARY OF THE MATARIPE AREA, TODOS OS SANTOS BAY, BAHIA, BRAZIL

The community structure and dynamics as well as some biological parameters of selected species of the ichthyofauna of the Mataripe estuarine region affected by the Landulfo Alves Oil Refinery (RLAM) were analyzed. Twenty stations were sampled with a gillnet in five different periods: August and December 2003, March and July/August 2004 and January 2005. Thirty-five actinopterygian species and one elasmobranch species were recorded, Oligoplites saurus, Diapterus rhombeus, Lutjanus synagris and Scomberomorus brasiliensis among them, on all the campaigns. A total of 1368 specimens, weighing 36.10 kg, were caught. The ichthyofauna total biomass was greater, in weight, on the eastern side of the study region, especially at the stations close to the shoals/reefs and the rocky bottom. A similar pattern was also observed for the diversity values. In general, low evenness and diversity were observed in the area studied, possibly as a result of the fishing gear used. D. rhombeus juveniles dominated in all but one of the samplings (July 2004), in which latter Cyclichthys spinosus was dominant. Carangids and species associated with consolidated bottoms were observed, although in small numbers, throughout the study period. In spite of the limitations imposed by the gear used for sampling, the estuarine area influenced by the RLAM was seen to play a role as a growth area for the great majority of species, especially the mojarra (D. rhombeus), but it offers no fishing potential due to the prevalence of young and small individuals. Evidence of imminent spawning was recorded for Pomadasys corvinaeformis in August 2003, and recent spawning in March 2004 for Oligoplites saurus. Further, mature individuals occurred in insufficient numbers to permit population level evaluation.

No evidence of UV cone input to mono- and biphasic horizontal cells in the goldfish retina

Many animal species make use of ultraviolet (UV) light in a number of behaviors, such as feeding and mating. The goldfish (Carassius auratus) is among those with a UV photoreceptor and pronounced UV sensitivity. Little is known, however, about the retinal processing of this input. We addressed this issue by recording intracellularly from second-order neurons in the adult goldfish retina. In order to test whether cone-driven horizontal cells (HCs) receive UV cone inputs, we performed chromatic adaptation experiments with mono- and biphasic HCs. We found no functional evidence of a projection from the UV-sensitive cones to these neurons in adult animals. This suggests that goldfish UV receptors may contact preferentially triphasic HCs, which is at odds with the hypothesis that all cones contact all cone-driven HC types. However, we did find evidence of direct M-cone input to monophasic HCs, favoring the idea that cone-HC contacts are more promiscuous than originally proposed. Together, our results suggest that either UV cones have a more restricted set of post-synaptic partners than the other three cone types, or that the UV input to mono- and biphasic HCs is not very pronounced in adult animals.

Influence of HLA-DRB-1 alleles on the production of antibody against CSP, MSP-1, AMA-1, and DBP in Brazilian individuals naturally infected with Plasmodium vivax

We evaluated the influence of allelic frequency of the human leukocyte antigen (HLA) -DRB1 on the acquisition of antibody response against malaria sporozoite and merozoite peptides in patients with Plasmodium vivax malaria acquired in endemic areas of Brazil. IgG antibodies were detected by enzyme-linked immunosorbent assay against four peptides of circumsporozoite protein (CSP) (amino, carboxyl, and VK210 and VK247 repeats) and peptides of merozoite surface protein 1 (MSP-1), apical membrane antigen 1 (AMA-1), and Duffy-binding protein (DBP). We found an association between HLA-DR3 and HLA-DR5 alleles and lack of antibody response to CSP amino terminal, as well as an association between HILA-DR3 and the highest antibody response to MSP1 (Pv200L). In conclusion, we suggest a potential regulatory role of the H1A-DRB1 alleles in the production of antibodies to a conserved region of P. vivax CSP and MSP1 in Brazilian population exposed to malaria. (C) 2011 Elsevier B.V. All rights reserved.