Synthesis, spectroscopic characterization, DFT studies and biological assays of a novel gold(I) complex with 2-mercaptothiazoline

A new gold(I) complex with 2-mercaptothiazoline (MTZ) with the coordination formula [AuCN(C(3)H(5)NS(2))] was synthesized and characterized by chemical and spectroscopic measurements, OFT studies and biological assays. Infrared (IR) and (1)H, (13)C and (15)N nuclear magnetic resonance (NMR) spectroscopic measurements indicate coordination of the ligand to gold(I) through the nitrogen atom. Studies based on OFT confirmed nitrogen coordination to gold(I) as a minimum of the potential energy surface with calculations of the hessians showing no imaginary frequencies. Thermal decomposition starts at temperatures near 160 degrees C, leading to the formation of Au as the final residue at 1000 degrees C. The gold(I) complex with 2-mercaptothiazoline (Au-MTZ) is soluble in dimethyl sulfoxide (DMSO), and is insoluble in water, methanol, ethanol, acetonitrile and hexane. The antibacterial activities of the Au-MTZ complex were evaluated by an antibiogram assay using the disc diffusion method. The compound showed an effective antibacterial activity against Staphylococcus aureus (Gram-positive) and Escherichia coli and Pseudomonas aeruginosa (Gram-negative) bacterial cells. Biological analysis for evaluation of the cytotoxic effect of the Au-MTZ complex was performed using HeLa cells derived from human cervical adenocarcinoma. The complex presented a potent cytotoxic activity, inducing 85% of cell death at a concentration of 2.0 mu mol L(-1). (C) 2011 Elsevier Ltd. All rights reserved.

Fatty acid synthesis and generation of glycerol-3-phosphate in brown adipose tissue from rats fed a cafeteria diet

In vivo fatty acid synthesis and the pathways of glycerol-3-phosphate (G3P) production were investigated in brown adipose tissue (BAT) from rats fed a cafeteria diet for 3 weeks. In spite of BAT activation, the diet promoted an increase in the carcass fatty acid content. Plasma insulin levels were markedly increased in cafeteria diet-fed rats. Two insulin-sensitive processes, in vivo fatty acid synthesis and in vivo glucose uptake (which was used to evaluate G3P generation via glycolysis) were increased in BAT from rats fed the cafeteria diet. Direct glycerol phosphorylation, evaluated by glycerokinase (GyK) activity and incorporation of [U-(14)C]glycerol into triacylglycerol (TAG)-glycerol, was also markedly increased in BAT from these rats. In contrast, the cafeteria diet induced a marked reduction of BAT glyceroneogenesis, evaluated by phosphoenolpyruvate carboxykinase-C activity and incorporation of [1-(14)C]pyruvate into TAG-glycerol. BAT denervation resulted in an approximately 50% reduction of GyK activity, but did not significantly affect BAT in vivo fatty acid synthesis, in vivo glucose uptake, or glyceroneogenesis. The data suggest that the supply of G3P for BAT TAG synthesis can be adjusted independently from the sympathetic nervous system and solely by reciprocal changes in the generation of G3P via glycolysis and via glyceroneogenesis, with no participation of direct phosphorylation of glycerol by GyK.

Glutamine supplementation does not improve protein synthesis rate by the jejunal mucosa of the malnourished rat

It has been demonstrated that glutamine, a conditionally essential amino acid, improves nitrogen balance, acts as a stimulant of protein synthesis, and decreases proteolysis in myopathic children. In contrast, other studies have shown no beneficial effect of glutamine supplementation on burn victims or critically ill patients. Nonetheless, we hypothesized that glutamine supplementation would increase the fractional protein synthesis rate (FSR) in the jejunal mucosa of malnourished male Wistar rats. Thus, the objective of the present study was to test the effect of daily oral glutamine supplementation (0.42 g kg(-1) d(-1) for 14 days) on the FSR of the jejunal mucosa of healthy and malnourished rats. A 4-hour kinetic study with L-[1-(13)C]leucine was subsequently performed, and jejunal biopsies were obtained 1.5 cm from the Treitz angle and analyzed. Malnourished rats showed a 25% weight loss and increased urinary nitrogen excretion. Plasma amino acid concentration did not differ between groups. (13)C enrichment in plasma and jejunal cells was higher in the malnourished groups than in the healthy group. The FSR (percent per hour) was similar for the control and experimental groups (P > .05), with a mean range of 220%/h to 27%/h. Oral glutamine supplementation alone did not induce higher protein incorporation by the jejunal mucosa in malnourished rats, regardless of total food intake or the presence or absence of glutamine supplementation. (C) 2009 Elsevier Inc. All rights reserved.

Ethinylestradiol and estradiol have different effects on oxidative stress and nitric oxide synthesis in human endothelial cell cultures

Study objective: To compare the effects of ethinylestradiol (EE) and 17 beta-estradiol (E(2)) on nitric oxide (NO) production and protection against oxidative stress in human endothelial cell cultures. Design: Experimental study. Settings: Research laboratory. Material: Human ECV304 endothelial cell cultures. Intervention(s): The NO synthesis was determined by flow cytometry, and oxidative stress was determined by a cell viability assay, after exposure to hydrogen peroxide (H(2)O(2)) and stimulation of endothelial cells with EE at concentrations similar to those of a contraceptive containing 30 mu g EE. Main Outcome Measure(s): The effects of EE were compared with those of E(2) at concentrations similar to those occurring during the follicular phase. Result(s): Ethinylestradiol did not increase NO synthesis and did not protect cells against oxidative stress. The viability of the cells incubated with E(2) in combination with H(2)O(2) was greater than the viability obtained with H(2)O(2) only or with H(2)O(2) in combination with EE. The cells stimulated with E(2) presented a significant increase in NO production compared with control. Conclusion(s): In contrast to the effects of E(2), EE did not protect human ECV304 endothelial cells against oxidative stress and did not increase their production of NO. (Fertil Steril (R) 2010; 94: 1578-82. (C) 2010 by American Society for Reproductive Medicine.)

Cross-cultural adaptation and reliability of Child-Initiated Pretend Play Assessment (ChIPPA)

Background. Play is an indication of a children`s development. Purpose. Organize a culturally adapt the Child-Initiated Pretend Play Assessment to Brazilian population. Method. Translation and cultural adaptation procedures consisted of translation, synthesis, back translation, author`s approval, and pretest of the assessment. For the pretest, 14 typically developing children were assessed. Was evaluated the use of play materials, duration of the assessment, and reliability. Findings. Play materials and duration of the assessment were appropriate for Brazilian children. Analysis of intra-rater reliability showed good agreement ranging from 0.90 to 1.00. Inter-rater reliability showed good to moderate agreement for five items ranging from 0.76 to 0.59. Four items showed chance to poor agreement (rho = -0.13 to 0.50). Implications. Results of the pretest indicate the Brazilian version of the ChIPPA is potentially useful for Brazilian children. ChIPPA training in Portuguese in Brazil with play observation feedback is recommended to improve inter-rater reliability.

Nitric oxide synthesis blockade reduced the baroreflex sensitivity in trained rats

Objective: The present study has investigated the effect of blockade of nitric oxide synthesis on cardiovascular autonomic adaptations induced by aerobic physical training using different approaches: 1) double blockade with methylatropine and propranolol; 2) systolic arterial pressure (SAP) and heart rate variability (HRV) by means of spectral analysis; and 3) baroreflex sensitivity. Methods: Male Wistar rats were divided into four groups: sedentary rats (SR); sedentary rats treated with N(omega)-nitro-L-arginine methyl ester (L-NAME) for one week (SRL); rats trained for eight weeks (TR); and rats trained for eight weeks and treated with L-NAME in the last week (TRL). Results: Hypertension and tachycardia were observed in SRL group. Previous physical training attenuated the hypertension in L-NAME-treated rats. Bradycardia was seen in TR and TRL groups, although such a condition was more prominent in the latter. All trained rats had lower intrinsic heart rates. Pharmacological evaluation of cardiac autonomic tonus showed sympathetic predominance in SRL group, differently than other groups. Spectral analysis of HRV showed smaller low frequency oscillations (LF: 0.2-0.75 Hz) in SRL group compared to other groups. Rats treated with L-NAME presented greater LF oscillations in the SAP compared to non-treated rats, but oscillations were found to be smaller in TRL group. Nitric oxide synthesis inhibition with L-NAME reduced the baroreflex sensitivity in sedentary and trained animals. Conclusion: Our results showed that nitric oxide synthesis blockade impaired the cardiovascular autonomic adaptations induced by previous aerobic physical training in rats that might be, at least in part, ascribed to a decreased baroreflex sensitivity. (C) 2009 Elsevier B.V. All rights reserved.

Elevated progesterone concentrations enhance prostaglandin F(2 alpha) synthesis in dairy cows

The objective was to evaluate the influence of varying plasma progesterone (P(4)) concentrations throughout the luteal phase in dairy cows on PGF(2 alpha) production (assessed as plasma concentrations of 13,14-dihydro-15-keto-PGF(2 alpha); PGFM) following treatment with estradiol-17 beta (E(2)) or oxytocin (OT). In all experiments, time of ovulations was synchronized with the OvSynch protocol and Day 0 corresponded to day of second GnRH injection. In Experiment 1, non-lactating dairy cows on Day 6 remained non-treated (n = 9), received 20 mg LH (n = 7), or had ovarian follicles larger than 6 mm aspirated (n = 8). In Experiment 2, cows on Day 6 were untreated (n = 9) or received 5000 IU hCG (n = 10). In Experiments 1 and 2, all cows received 3 mg E(2) on Day 17, and blood samples were collected every 30 min from 2h before to 10h after E(2). Experiment 3 was conducted in two periods, each from Days 0 to 17 of the estrous cycle. At the end of Period 1, animals switched treatments in a crossover arrangement. Animals in Group 2/8 (n = 4) received 2 kg/d of concentrate in the first period and 8 kg/d in the second period. Animals in Group 8/2 (n = 7) received the alternate sequence. Blood was collected daily for measurement Of P(4) 4 h after concentrate feeding. On Day 17, blood was collected from 1 h before to 1 h after a 100 IU OT injection. In Experiment 1, both plasma P(4) and release Of PGF(2 alpha) were similar between LH-treated and control cows (P > 0.10). In Experiment 2, plasma P4 was elevated to a greater extent on Day 17 in cows treated with hCG (P < 0.05) and plasma PGFM was also greater in hCG-treated animals (treatment x time interaction; P < 0.05). In Experiment 3, there was a group x period interaction (P < 0.01) for plasma P(4), indicating that less concentrate feeding was associated with greater plasma P(4). Release of PGF(2 alpha) in response to OT was greater for cows receiving less concentrate (group x period interaction; P < 0.05). In conclusion, dairy cows with more elevated blood P(4) concentrations released more PGF(2 alpha) in response to E(2) or OT. (c) 2008 Elsevier B.V. All rights reserved.

Effects of Ethanol on Synthesis of Prostaglandin F2 alpha in Bovine Females

Ethanol stimulates the production of prostaglandins in many species. The purpose of this study was to verify the effect of ethanol on the production of prostaglandin F2 alpha (PGF2 alpha) and luteolysis in bovine females. In the first experiment, Holstein cows at day 17 of the oestrous cycle were treated with 100% ethanol (0.05 ml/kg of body weight, IV; n = 5), saline (0.05 ml/kg of body weight, IV; n = 4) or synthetic prostaglandin (150 mu g of D-cloprostenol/cow, IM; n = 4). The plasma concentrations of 13, 14-dihydro-15-keto PGF2 alpha (PGFM; the main metabolite of PGF2 alpha measured in the peripheral blood) were assessed by radioimmunoassay (RIA). There was an acute release of PGFM in response to ethanol comparing to other treatments (p <= 0.05). However, only cows treated with PGF2 alpha underwent luteolysis. In the second experiment, endometrial explants of cross-bred beef cows (n = 4) slaughtered at day 17 of the oestrous cycle were cultured for 4 h. During the last 3 h, the explants were cultured with medium supplemented with 0, 0.1, I, 10 or 100 mu l of 100% ethanol/ml. Medium samples were collected at hours 1 and 4 and concentrations of PGF2 alpha were measured by RIA. Ethanol did not induce PGF2 alpha production by the endometrium. In conclusion, ethanol does not cause luteolysis in cows because it stimulates production of PGF2 alpha in extra-endometrial tissues.

Analysis in vitro of the cytotoxicity of potential implant materials. I: Zirconia-titania sintered ceramics

Zirconia (ZrO(2)) is a bioinert, strong, and tough ceramic, while titania (TiO(2)) is bioactive but has poor mechanical properties. It is expected that ZrO(2)-TiO(2) mixed ceramics incorporate the individual properties of both ceramics, so that this material would exhibit better biological properties. Thus, the objective of this study was to compare the biocompatibility properties of ZrO(2)-TiO(2) mixed ceramics. Sintered ceramics pellets, obtained from powders of TiO(2), ZrO(2), and three different ZrO(2)-TiO(2) mixed oxides were used. Roughnesses, X-ray diffraction, microstructure through SEM, hardness, and DRIFT characterizations were performed. For biocompatibility analysis cultured FMM1 fibroblasts were plated on the top of disks and counted in SEM micrographs 1 and 2 days later. Data were compared by ANOVA complemented by Tukey`s test. All samples presented high densities and similar microstructure. The H(2)O content in the mixed ceramics was more evident than in pure ceramics. The number of fibroblasts attached to the disks increased significantly independently of the experimental group. The cell growth on the top of the ZrO(2)-TiO(2) samples was similar and significantly higher than those of TiO(2) and ZrO(2) samples. Our in vitro experiments showed that the ZrO(2)-TiO(2) sintered ceramics are biocompatible allowing faster cell growth than pure oxides ceramics. The improvement of hardness is proportional to the ZrO(2) content. Thus, the ZrO(2)-TiO(2) sintered ceramics could be considered as potential implant material. (C) 2010 Wiley Periodicals, Inc. J Biomed Mater Res Part B: Appl Biomater 94B: 305-311, 2010.

Esthetic restorative materials and opposing enamel wear

This in vitro study compared the effects of a gold alloy (Degulor M), four dental ceramics (IPS Empress, IPS Empress 2, Duceram Plus, Duceram. LFC) and a laboratory-processed composite (Targis) on the wear of human enamel. The amount of wear of the enamel (dental cusps) and restorative materials (disks) were tested in water at 37 degrees C under standard load (20 N), with a chewing rate of 1.3 Hz and was determined after 150,000 and 300,000 cycles. Before the test, the average surface roughness of the restorative materials was analyzed using the Ra parameter. The results of this study indicate that Targis caused enamel wear similar to Degulor M and resulted in significantly less wear than all the ceramics tested. IPS Empress provoked the greatest amount of enamel wear and Degulor M caused less vertical dimension loss. Targis could be an appropriate alternative material to ceramic, because it is esthetic and produces opposing enamel wear comparable to gold alloy.

Effect of prolonged erosive pH cycling on different restorative materials

This in vitro study evaluated the effect of a prolonged erosive pH cycling on the superficial microhardness change (SMHC) and the erosive wear of different restorative materials. Eighty enamel specimens with prepared cavities of 1.5 x 1.5 mm were randomly divided into eight groups according to the restorative materials used for the fillings (RMGI - resin-modified glass-ionomer, CGI - conventional glass-ionomer, CR- composite resin, A - amalgam) and immersion media used (ERO - erosive medium or SAL - artificial saliva). During 35 days, half of the specimens were immersed in a cola drink (ERO), for 5 min, three times a day, and they remained in SAL between the erosive cycles. The other half of the specimens was immersed in SAL only, for the entire experimental period (control). Data were tested for significant differences by anova and Tukey`s tests (P < 0.05). Scanning electron microscopy images were made to illustrate the enamel erosive wear and restorative materials alterations. The mean SMHC (%) and mean erosive wear (mu m) of the materials were: RMGI-ERO (30/0.5); CGI-ERO (37/0.5); CR-ERO (-0.3/0.3); A-ERO (-4/0.3); RMGI-SAL (4/0.4); CGI-SAL (-6/0.4); CR-SAL (-3/0.2) and A-SAL (2/0.4). Scanning electron microscopy images showed pronounced enamel erosive wear on groups submitted to erosive pH cycling when compared with groups maintained in saliva. In conclusion, the prolonged pH cycling promoted significantly higher alterations (SMHC and erosive wear) on the glass-ionomer cements than the CR and amalgam.

Effect of erosive pH cycling on different restorative materials and on enamel restored with these materials

This in vitro study evaluated the effect of erosive pH cycling on the percentage of surface micro-hardness change (%SMHC) and wear of different restorative materials and bovine enamel restored with these materials. Eighty enamel specimens were randomly divided into eight groups according to the restorative materials and immersion media used: GI/GV-resin-modifled glass-ionomer, GII/GVI-conventional glass-ionomer, GIII/GVII-resin composite and GIV/GVIII-amalgam. Over a period of seven days, groups GI to GIV were immersed in a cola drink (ERO) for 5 minutes, 3x/day and kept in artificial saliva between erosive cycles. Groups GV to GVIII were immersed in artificial saliva (SAL) throughout the entire experimental period (control). Data were tested for significant differences using ANOVA and Tukey`s tests (p < 0.05). For %SMHC, considering the restorative materials, no significant differences were detected among the materials and immersion media. Mean wear was higher for the resin modified glass ionomer cement when compared to conventional cement, but those materials did not significantly differ from the others. For enamel analyses, erosive pH cycling promoted higher wear and %SMHC compared to saliva. There were no significant differences in wear and %SMHC of enamel around the different restorative materials, regardless of the distance from the restorative material (50, 150 or 300 mu m). In conclusion, there were only subtle differences among the materials, and these differences were not able to protect the surrounding enamel from erosion.

Comparison of GPX with or without solvent and hand files in removing filling materials from root canals-An ex vivo study

Objective. The aim of this study was to compare GPX instruments and hand files for gutta-percha removal. Study design. Fifty maxillary central incisors with a single straight canal were instrumented and filled. The teeth were divided into 5 groups of 10 specimens each, according to the gutta-percha removal techniques: group 1: GPX (21-mm-long teeth); group 2: GPX and xylol as solvent (21-mm-long teeth); group 3: GPX (25-mm-long teeth); group 4: GPX and xylol as solvent (25-mm-long teeth); and group 5: hand files and xylol as solvent. The amount of time for gutta-percha removal and the number of fractured instruments were evaluated. Radiographs were taken, and the teeth were grooved longitudinally and split. The area of residual debris was measured using Sigma Scan software. Results. The time for filling material removal was significantly shorter when GPX was used (P < .05). Overall, hand files and solvent produced fewer remnants of filling materials (P < .05). In the GPX 25 mm-long teeth group, the filling material was not removed in the apical third. Conclusions. Under the experimental conditions, the GPX instruments proved to be faster than hand instruments in removing root filling materials; however, hand instruments left a smaller amount of residual filling materials on the canal walls. The GPX instruments did not pull the gutta-percha beyond its tip. (Oral Surg Oral Med Oral Pathol Oral Radiol Endod 2010; 110: 675-680)