Pharmacokinetic Profile of A New Diclofenac Prodrug without Gastroulcerogenic Effect

Gastrotoxicity is a major problem for long-term therapy with non-steroidal anti-inflammatory drugs (NSAIDs). DICCIC (1-(2,6-dichlorophenyl)indolin-2-one) is a new diclofenac prodrug, which has proven anti-inflammatory activity without gastroulcerogenic effect. The aim of this work was to compare the pharmacokinetic profiles of diclofenac from DICCIC (7.6 mg/kg equivalent to 8.1 mg/kg diclofenac) and diclofenac (8.1 mg/kg) administration in Wistar rats weighing 250-300 g (n=20). The doses were calculated by interspecific allometric scaling based on the 2 mg/kg from diary human dose of diclofenac. Blood samples were collected in heparinized tubes via the femoral artery through the implanted catheter. The plasma was separated and quantitation was made in a HPLC system with a UV-Vis detector. The confidence limits of the bioanalytical method were appropriate for its application in a preclinical pharmacokinetic study. The AUC of diclofenac from DICCIC (53.7± 5.8 ug/mL.min) was significantly less (Mann Whitney test, p<0.05) than that of diclofenac from diclofenac administration (885.9 ± 124,8 ug/mL.min). Terminal half-life of diclofenac from DICCIC (50.1 ± 17.2 min) was significantly less (Mann Whitney test, p<0.05) than that of diclofenac from diclofenac administration (247.4 ± 100.9 min). Still the parameters clearance and distribution volume were calculated for diclofenac from diclofenac, whose results were 9.2 ±1.2 mL/min.kg and 3.3 ±1.2 L/kg, respectively. The results of DICCIC from DICCIC administration were 108.9 ± 19.6 mL/min.kg and 7.8 ± 2.4 L/kg for clearance and distribution volume, respectively. The pharmacokinetic profile demonstrated that there was an increase in diclofenac elimination and a lower exposure to diclofenac with administration of DICCIC compared to diclofenac. © 2013 Bentham Science Publishers.

Study of a series of cobalt(II) sulfonamide complexes: Synthesis, spectroscopic characterization, and microbiological evaluation against M. tuberculosis. Crystal structure of [Co(sulfamethoxazole)2(H 2O)2]·H2O

Nowadays, the research for new and better antimicrobial compounds is an important field due to the increase of immunocompromised patients, the use of invasive medical procedures and extensive surgeries, among others, that can affect the incidence of infections. Another big problem associated is the occurrence of drug-resistant microbial strains that impels a ceaseless search for new antimicrobial agents. In this context, a series of heterocyclic- sulfonamide complexes with Co(II) was synthesized and characterized with the aim of obtaining new antimicrobial compounds. The structural characterization was performed using different spectroscopic methods (UV-Vis, IR, and EPR). In spite of the fact that the general stoichiometry for all the complexes was Co(sulfonamide)2·nH2O, the coordination atoms were different depending on the coordinated sulfonamide. The crystal structure of [Co(sulfamethoxazole)2(H2O)2]·H 2O was obtained by X-ray diffraction showing that Co(II) is in a slightly tetragonal distorted octahedron where sulfamethoxazole molecules act as a head-to-tail bridges between two cobalt atoms, forming polymeric chains. Besides, the activity against Mycobacterium tuberculosis, one of the responsible for tuberculosis, and the cytotoxicity on J774A.1 macrophage cells were evaluated. © 2012 Elsevier B.V. All rights reserved.

Influence of anatomical location on CT numbers in cone beam computed tomography

Objective: To assess the influence of anatomical location on computed tomography (CT) numbers in mid- and full field of view (FOV) cone beam computed tomography (CBCT) scans. Study Design: Polypropylene tubes with varying concentrations of dipotassium hydrogen phosphate (K2HPO4) solutions (50-1200 mg/mL) were imaged within the incisor, premolar, and molar dental sockets of a human skull phantom. CBCT scans were acquired using the NewTom 3G and NewTom 5G units. The CT numbers of the K2HPO 4 phantoms were measured, and the relationship between CT numbers and K2HPO4 concentration was examined. The measured CT numbers of the K2HPO4 phantoms were compared between anatomical sites. Results: At all six anatomical locations, there was a strong linear relationship between CT numbers and K2HPO4 concentration (R 2 > 0.93). However, the absolute CT numbers varied considerably with the anatomical location. Conclusion: The relationship between CT numbers and object density is not uniform through the dental arch on CBCT scans. © 2013 Elsevier Inc.

Biocompatibility and biomineralization assessment of a new root canal sealer and root-end filling material

Objective: This study investigated the short-term subcutaneous tissue reaction and biomineralization ability of two epoxy-based root canal sealers containing calcium hydroxide (MBP and MBPc) and ProRoot MTA. Materials and methods: Polyethylene tubes containing the materials were implanted into the dorsal connective tissue of Wistar rats (n = 52) for 7 or 30 days; empty implanted tubes served as controls. Specimens were stained with hematoxylin-eosin and von Kossa stain or left unstained for observation under polarized light. Qualitative and quantitative evaluations of all tissue reactions were performed. One-way anova and the Kruskal-Wallis test were used for statistical analysis (P < 0.05). Results: No significant differences were observed among the groups. All three materials induced mild-to-moderate tissue reactions at 7 days, which decreased over time. Dystrophic mineralization and birefringent structures were observed only in the ProRoot MTA ® group. Conclusion: Both MBP and MBPc appear to be biocompatible but do not stimulate biomineralization. © 2012 John Wiley & Sons A/S.

Morphological adaptations to arboreal habitats and heart position in species of the neotropical whipsnakes genus Chironius

The evolution of arboreality in snakes is accompanied by modifications that are remarkably similar across species. Gravity is one of the most important selective agents, and arboreal snakes present adaptations to circumvent the gradient of pressure, including modifications on heart position (HP) and body slenderness (BS). However, the degree to which different life-history traits influence the cardiovascular system of snakes remains unclear. Here, we used an ecological and a phylogenetic approach to explore the relationship between habitat, HP, BS, and heart size (HS) in five species of the neotropical whipsnakes genus Chironius that occupy terrestrial, semiarboreal, and arboreal habits. Our ecological comparison indicated that the arboreal species have the most posterior-positioned heart, the most slender body, and the smallest HS, whereas the terrestrial representative of the group exhibited the most anterior heart, the less flattened body, and the largest HS. After removing the phylogenetic effect, we found no difference in HP and BS between terrestrial and arboreal species. Habitat only differed when contrasting with HS. Body slenderness and HS were correlated with HP. Our results suggest that different restrictions, such as anatomical constraints, behavior, and phylogenetic inertia, may be important for the studied species. © 2013 The Royal Swedish Academy of Sciences.

Photodynamic inactivation of Streptococcus mutans and Streptococcus sanguinis biofilms in vitro

The purpose of this study was to evaluate specific effects of photodynamic inactivation (PDI) using erythrosine (ER) and Rose Bengal (RB) photosensitizers and a blue light-emitting diode (LED) on the viability of Streptococcus mutans and Streptococcus sanguinis biofilms. Biofilms were grown in acrylic disks immersed in broth to production of biofilms, inoculated with microbial suspension (106 cells/mL) and incubated for 48 h. After the formation of biofilms, the effects of the photosensitizers ER and RB at a concentration of 5 μM for 5 min and blue LED (455 ± 20 nm) for 180 s, photosensitizers alone and conjugated were evaluated. Next, the disks were placed in tubes with sterile physiological solution (0.9 % sodium chloride) and sonicated for to disperse the biofilms. Tenfold serial dilutions were carried and aliquots seeded in brain heart infusion agar which were then incubated for 48 h. Then the numbers colony-forming units per milliliter (CFU/mL; log 10) were counted and analyzed statistically (ANOVA, Tukey test, P ≤ 0.05). Significant decreases in the viability of all microorganisms were observed for biofilms exposed to PDI mediated by both photosensitizers. The reductions with RB and ER were, 0.62 and 0.52 log10 CFU mL -1 for S. mutans biofilms (p = 0.001), and 0.95 and 0.88 log 10 CFU mL-1 for S. sanguinis biofilms (p = 0.001), respectively. The results showed that biofilms formed in vitro by S. mutans and S. sanguinis, were sensitive to PDI using a blue LED associated with photosensitizers ER or RB, indicating its use in the control of caries and periodontal diseases. © 2012 Springer-Verlag London Ltd.

The use of NaOCl in combination with CHX produces cytotoxic product

Objectives: The combination of sodium hypochlorite (NaOCl) and chlorhexidine (CHX) yields a precipitate potentially toxic (PPT). The aim of this study was to evaluate the tissue response to implanted polyethylene tubes filled with PPT-soaked fibrin sponge. Methods: Forty rats received four polyethylene tubes each; each tube was filled with fibrin sponge soaked by 2.5 % NaOCl, 2.0 % CHX, PPT (2.5 % NaOCl plus 2.0 % CHX), or not soaked (control). The observation time points were 7, 15, 30, 60, and 90 days. At each time point, eight animals were killed, and the tubes and surrounding tissues were removed, fixed, and prepared for light microscopic analysis by performing glycol methacrylate embedding, serial cutting into 3-μm sections, and hematoxylin-eosin staining. Qualitative and quantitative evaluations of the reactions were performed. Results were statistically analyzed by Kruskal-Wallis test (p < 0.05). Results: All chemical solutions caused moderate reactions at 7 days. On day 30, PPT group was more cytotoxic than the control group and the CHX group (p < 0.05). On days 15 and 60, PPT group was more cytotoxic than the control group (p < 0.05). On day 90, there was no statistically significant difference between the different groups. Conclusion: PPT is more cytotoxic than NaOCl and CHX alone, particularly in the short term. Clinical significance: Protocols which suggest the use of CHX and NaOCl must be revised because this mixture produces cytotoxic product. © 2013 Springer-Verlag Berlin Heidelberg.

Lower Permian stems as fluvial paleocurrent indicators of the Parnaíba Basin, northern Brazil

A comprehensive biostratinomic study was carried out with abundant stems from the Lower Permian Motuca Formation of the intracratonic Parnaíba Basin, central-north Brazil. The fossils represent a rare tropical to subtropical paleofloristic record in north Gondwana. Tree ferns dominate the assemblages (mainly Tietea, secondarily Psaronius), followed by gymnosperms, sphenophytes, other ferns and rare lycophytes. They are silica-permineralized, commonly reach 4 m length (exceptionally more than 10 m), lie loosely on the ground or are embedded in the original sandstone or siltstone matrix, and attract particular attention because of their frequent parallel attitudes. Many tree fern stems present the original straight cylindrical to slightly conical forms, other are somewhat flattened, and the gymnosperm stems are usually more irregular. Measurements of stem orientations and dimensions were made in three sites approximately aligned in a W-E direction in a distance of 27.3 km at the conservation unit Tocantins Fossil Trees Natural Monument In the eastern site, rose diagrams for 54 stems indicate a relatively narrow azimuthal range to SE. These stems commonly present attached basal bulbous root mantles and thin cylindrical sandstone envelopes, which sometimes hold, almost adjacent to the lateral stem surface, permineralized fern pinnae and other small plant fragments. In the more central site, 82 measured stems are preferentially oriented in the SW-NE direction, the proportion of gymnosperms is higher and cross-stratification sets of sandstones indicate paleocurrents mainly to NE and secondarily to SE. In the western site, most of the 42 measured stems lie in E-W positions. The predominantly sandy succession, where the fossil stems are best represented, evidences a braided fluvial system under semiarid conditions. The low plant diversity, some xeromorphic features and the supposedly almost syndepositional silica impregnation of the plants are coherent with marked dry seasons. Thick mudstones and some coquinites below and above the sandy interval may represent lacustrine facies formed in probably more humid conditions. The taphonomic history of the preserved plants began with exceptional storms that caused fast-flowing high water in channels and far into the floodplains. In the eastern site region, many tree ferns only fell, thus sometimes covering and protecting plant litter and leaves from further fragmentation. Assemblages of the central and western sites suggest that the trees were uprooted and transported in suspension (floating) parallel to the flow. Heavier ends of stems (according to their form or because of attached basal bulbous root mantle or large apical fronds) were oriented to upstream because of inertial forces. During falling water stage, the stems were stranded on riverbanks, usually maintaining the previous transport orientation, and were slightly buried. The perpendicular or oblique positions of some stems may have been caused by interference with other stems or shallow bars. Rare observed stems were apparently waterlogged before the final depositional process and transported as bedload. The differences of interpreted channel orientations between the three sites are expected in a braided fluvial system, considering the very low gradients of the basin and the work scale in the order of tens of kilometers. The mean direction of the drainage probably was to east and the flows apparently became weaker downstream. This study seems to provide reliable data for paleocurrent interpretations, especially considering areas with scarce preserved sedimentary structures. © 2013 Elsevier Ltd.

Sporophytic apomixis in polyploid Anemopaegma species (Bignoniaceae) from central Brazil

Apomixis and polyploidy have been important in the evolution of the angiosperms, and sporophytic apomixis has been associated with polyembryony and polyploidy in tropical floras. We studied the occurrence of polyembryony in populations of tetraploid Anemopaegma acutifolium, A.arvense and A.glaucum from the Brazilian cerrados, and histological features of sexual and apomictic processes were investigated in A.acutifolium. All populations and species were polyembryonic (68.9-98.4% of seeds). Normal double fertilization occurred in most ovules, with exceptions being that 3% of ovules were penetrated but not fertilized and in 4% of ovules both synergids were penetrated. The penetration of both synergids suggests a continuous attraction of pollen tubes and polyspermy. Adventitious embryo precursor cells (AEPs) arose from nucellar and integumental cells of the ovule in pollinated and unpollinated A.acutifolium, indicating sporophytic apomixis. However, further embryo and endosperm development required pollination and fertilization. This pseudogamy also allows concurrent sexual embryo development. Similar polyembryony rates and polyploidy indicated that A.arvense and A.glaucum are also apomictic, forming an agamic complex similar to that observed for some species of confamilial, but not closely related Handroanthus. The co-occurrence of apomixis and polyploidy in different groups of Bignoniaceae indicates homoplasious origin of these agamic complexes. © 2013 The Linnean Society of London.

Propriedades físicas de um latossolo vermelho manejado com material orgânico e submetido à compactação

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Alterações bioquímicas, morfofisiológicas e produtivas em genótipos de arroz em dois regimes hídricos

Pós-graduação em Agronomia (Agricultura) - FCA

Efeitos da terapia fotodinâmica in vitro em biofilmes formados por Candida albicans, Staphylococcus aureus e Streptococcus mutans

Pós-graduação em Biopatologia Bucal - ICT

Substrato com composto de lixo e poda de árvore para produção de mudas de Pterogyne nitens

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Avaliação da eficiência de métodos rápidos usados para detecção de coliforme totais e coliforme fecais em amostras de água, em comparação com a técnica de fermentação em tubos múltiplos

Pós-graduação em Alimentos e Nutrição - FCFAR

Modelagem do escoamento e da transferência de calor ao longo de tubos capilares não adiabáticos

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)