New selective acetylcholinesterase inhibitors designed from natural piperidine alkaloids

Five new piperidine alkaloids were designed from natural (-)-3-O-acetyl-spectaline and (-)-spectaline that were obtained from the flowers of Senna spectabilis (sin. Cassia spectabilis, Leguminosae). Two semi-synthetic analogues (7 and 9) inhibited rat brain acetylcholinesterase, showing IC50 of 7.32 and 15.1 mu M, and were 21 and 9.5 times less potent against rat brain butyrylcholinesterase, respectively. Compound 9 (1 mg/kg, ip) was fully efficacious in reverting scopolamine-induced amnesia in mice. The two active compounds (7 and 9) did not show overt toxic effects at the doses tested in vivo. (c) 2005 Elsevier Ltd. All rights reserved.

On linear combinations of L-orthogonal polynomials associated with distributions belonging to symmetric classes

This paper deals with the classes S-3(omega, beta, b) of strong distribution functions defined on the interval [beta(2)/b, b], 0 < beta < b <= infinity, where 2 omega epsilon Z. The classification is such that the distribution function psi epsilon S-3(omega, beta, b) has a (reciprocal) symmetry, depending on omega, about the point beta. We consider properties of the L-orthogonal polynomials associated with psi epsilon S-3(omega, beta, b). Through linear combination of these polynomials we relate them to the L-orthogonal polynomials associated with some omega epsilon S-3(1/2, beta, b). (c) 2004 Elsevier B.V. All rights reserved.

On the denominator values and barycentric weights of rational interpolants

We improve upon the method of Zhu and Zhu [A method for directly finding the denominator values of rational interpolants, J. Comput. Appl. Math. 148 (2002) 341-348] for finding the denominator values of rational interpolants, reducing considerably the number of arithmetical operations required for their computation. In a second stage, we determine the points (if existent) which can be discarded from the rational interpolation problem. Furthermore, when the interpolant has a linear denominator, we obtain a formula for the barycentric weights which is simpler than the one found by Berrut and Mittelmann [Matrices for the direct determination of the barycentric weights of rational interpolation, J. Comput. Appl. Math. 78 (1997) 355-370]. Subsequently, we give a necessary and sufficient condition for the rational interpolant to have a pole. (c) 2006 Elsevier B.V. All rights reserved.

COMPARATIVE INVITRO ACTIVITY OF 3 CEPHALOSPORINS AGAINST STAPHYLOCOCCUS-AUREUS ISOLATED FROM BOVINE MASTITIS

This report compares the in vitro activity of three cephalosporins (cephalothin, cefoxitin and ceftriaxone) against 57 Staphylococcus aureus strains isolated from cows with clinical mastitis on the basis of the minimal inhibitory (MIC) and minimal bactericidal concentrations (MBC). The majority of the S aureus strains showed resistance to cefoxitin and ceftriaxone and sensitivity to cephalothin. The highest MICs and MBCs were found for cefoxitin and ceftriaxone. Antimicrobial tolerance (MBC/MIC greater-than-or-equal-to 32:1) was observed in relation to cephalothin and ceftriaxone. The data suggest that these cephalosporins may not be effective for the treatment of staphylococcal bovine mastitis. The precise definition of their antimicrobial efficacies requires more detailed in vitro and in vivo studies.

New anti-Alzheimer drugs from biodiversity: the role of the natural acetylcholinesterase inhibitors

Alzheimer's disease (AD) is a progressive neurodegenerative pathology with severe economic and social impact. There is currently no cure, although cholinesterase inhibitors provide effective temporary relief of symptoms in some patients. Nowadays, drug research and development are based on the cholinergic hypothesis that supports the cognition improvement by regulation of the synthesis and release of acetylcholine in the brain. There are only four commercial medicines approved for treatment of AD, and natural products have played an important alternative role in the research for new acetylcholinesterase inhibitors, as exemplified through the discovery of galantamine. This profile conducts us to give in this paper an overview relating the several classes of natural products with anti-cholinesterasic activity as potential templates to the design of new selective and powerful anti-Alzheimer drugs.

Ceramic materials in dentistry: historical evolution and current practice

Dental ceramics are presented within a simplifying framework allowing for facile understanding of their development, composition and indications. Engineering assessments of clinical function are dealt with and literature is reviewed on the clinical behaviour of all-ceramic systems. Practical aspects are presented regarding the choice and use of dental ceramics to maximize aesthetics and durability, emphasizing what we know and how we know it.

Mechanistic approach to predict real machining time for milling free-form geometries applying high feed rate

An accurate estimate of machining time is very important for predicting delivery time, manufacturing costs, and also to help production process planning. Most commercial CAM software systems estimate the machining time in milling operations simply by dividing the entire tool path length by the programmed feed rate. This time estimate differs drastically from the real process time because the feed rate is not always constant due to machine and computer numerical controlled (CNC) limitations. This study presents a practical mechanistic method for milling time estimation when machining free-form geometries. The method considers a variable called machine response time (MRT) which characterizes the real CNC machine's capacity to move in high feed rates in free-form geometries. MRT is a global performance feature which can be obtained for any type of CNC machine configuration by carrying out a simple test. For validating the methodology, a workpiece was used to generate NC programs for five different types of CNC machines. A practical industrial case study was also carried out to validate the method. The results indicated that MRT, and consequently, the real machining time, depends on the CNC machine's potential: furthermore, the greater MRT, the larger the difference between predicted milling time and real milling time. The proposed method achieved an error range from 0.3% to 12% of the real machining time, whereas the CAM estimation achieved from 211% to 1244% error. The MRT-based process is also suggested as an instrument for helping in machine tool benchmarking.

Carbon isotope composition as a tool to control the quality of herbs and medicinal plants

Isotope screening is a simple test for determining the photosynthetic pathway used by plants. The scope of this work was to classify the photosynthetic type of some herbs and medicinal plants through studies of the carbon isotope composition (δ13C). Also, we propose the use of carbon isotope composition as a tool to control the quality of herbs and medicinal plants. For studies of δ13C, δ 13C‰ = [R (sample)/R (standard) - 1] × 10-3, dry leaves powdered in cryogenic mill were analyzed in a mass spectrometer coupled with an elemental analyzer for determining the ratio R = 13CO2/12CO2. In investigation of δ13C of 55 species, 23 botanical families, and 44 species possessed a C3 photosynthetic type. Six species found among the botanical families Euphorbiaceae and Poaceae were C4 plants, and 5 species found among the botanical families Agavaceae, Euphorbiaceae, and Liliaceae possessed CAM-type photosynthesis. Carbon isotope composition of plants can be used as quality control of herbs and medicinal plants, allowing the identification of frauds or contaminations. Also, the information about the photosynthetic type found for these plants can help in introducing and cultivating exotic and wild herbs and medicinal plants.

Influence of vegetable oil in the viscosity of biodiesel-a review

Viscosity is a measure fluid resistance to flowing, affecting the fuel spray in the combustion chamber and, by this way, thus the formation of carbon deposits. The analysis of the influence of vegetable oil viscosity in biodiesel seems appropriate, because biodiesel viscosity is a function of vegetable oil. The increase of the fuel viscosity, promoted by biodiesel, has a major impact on the dynamics of jet fuel, increasing its speed and distance of penetration, obtaining therefore an increase in the amount of turbulent movement of the jet and thus an increase in the rate of preparation of the mixture, air-fuel, when adding biodiesel to diesel oil. The negative effect of this higher fuel viscosity is the increase of the wear of the train of gears, cam shaft, and valve push rod of all the injection pumps due to the higher pressure of injection. The viscosity of biodiesel is influenced by the size of its molecule and by the increase of molecule insaturations, is directly related with its origin vegetable oil or fat. This study is a review of the influence of vegetable oils in viscosity of biodiesel. Copyright © 2008 SAE International.

Effect of hydrofluoric acid etching duration on the roughness and flexural strength of a lithium disilicate-based glass ceramic

The aim of this study was to examine the effect of different acid etching times on the surface roughness and flexural strength of a lithium disilicate-based glass ceramic. Ceramic bar-shaped specimens (16 mm x 2 mm x 2 mm) were produced from ceramic blocks. All specimens were polished and sonically cleaned in distilled water. Specimens were randomly divided into 5 groups (n=15). Group A (control) no treatment. Groups B-E were etched with 4.9% hydrofluoric acid (HF) for 4 different etching periods: 20 s, 60 s, 90 s and 180 s, respectively. Etched surfaces were observed under scanning electron microscopy. Surface profilometry was used to examine the roughness of the etched ceramic surfaces, and the specimens were loaded to failure using a 3-point bending test to determine the flexural strength. Data were analyzed using one-way ANOVA and Tukey's test (α=0.05). All etching periods produced significantly rougher surfaces than the control group (p<0.05). Roughness values increased with the increase of the etching time. The mean flexural strength values were (MPa): A=417 ± 55; B=367 ± 68; C=363 ± 84; D=329 ± 70; and E=314 ± 62. HF etching significantly reduced the mean flexural strength as the etching time increased (p=0.003). In conclusion, the findings of this study showed that the increase of HF etching time affected the surface roughness and the flexural strength of a lithium disilicate-based glass ceramic, confirming the study hypothesis.

Retention and processing methods of nasal prosthesis

Patients with congenital malformations, traumatic or pathological mutilation and maxillofacial developmental disorders can be restored aesthetically and emotionally by the production and use of facial prostheses. The aim of this study was to review the literature about the retention and processing methods of facial prostheses, and discuss their characteristics. A literature review on Medline (PubMed) database was performed by using the keywords maxillofacial prosthesis, silicone, resin, pigment, cosmetic, prosthetic nose, based on articles published from 1956 to 2010. Several methods of retention, from adhesives to the placement of implants, and different processing methods such as laser, CAD/CAM and rapid prototyping technologies have been reported. There are advantages and disadvantages of each procedure, and none can be classified as better compared to others.

Influence of polishing procedures on the surface roughness of dental ceramics made by different techniques

The aim of this study was to evaluate the influence of 2 different surface polishing procedures - glazing (GZ) and manual polishing (MP) - on the roughness of ceramics processed by computer-aided design/computer-aided manufacturing (CAD/CAM) and conventional systems (stratification technique). Eighty ceramic discs (diameter: 8 mm, thickness: 1 mm) were prepared and divided among 8 groups (n = 10) according to the type of ceramic disc and polishing method: 4 GZ and 4 MP. Specimens were glazed according to each manufacturer's recommendations. Two silicone polishing points were used on the ceramic surface for manual polishing. Roughness was measured using a surface roughness tester. The roughness measurements were made along a distance of 2 mm on the sample surface and the speed of reading was 0.1 mm/s. Three measurements were taken for each sample. The data (μm) were statistically analyzed using analysis of variance (ANOVA) and Tukey's test (α = 0.05). Qualitative analysis was performed using scanning electron microscopy (SEM). The mean (± SD) roughness values obtained for GZ were: 1.1 ± 0.40 μm; 1.0 ± 0.31 μm; 1.6 ± 0.31 μm; and 2.2 ± 0.73 μm. For MP, the mean values were: 0.66 ± 0.13 μm; 0.43 ± 0.14 μm; 1.6 ± 0.55 μm; and 2.0 ± 0.63 μm. The mean roughness values were significantly affected by the ceramic type (P = 0.0001) and polishing technique (P = 0.0047). The SEM images confirmed the roughness data. The manually polished glass CAD/CAM ceramics promoted lower surface roughness than did the glazed feldspathic dental ceramics.

Influence of convergence angle of tooth preparation on the fracture resistance of Y-TZP-based all-ceramic restorations

Objective: To investigate the influence of the convergence angle of tooth preparation on the fracture load of Y-TZP-based ceramic (YZ-Vita YZ) substructure (SB) veneered with a feldspathic porcelain (VM9-Vita VM9). Methods: Finite element stress analysis (FEA) was performed to examine the stress distribution of the system. Eighty YZ SB were fabricated using a CAD-CAM system and divided into four groups (n = 20), according to the total occlusal convergence (TOC) angle: G6-6° TOC; G12-12° TOC; G20-20° TOC; and G20MOD-20° TOC with modified SB. All SB were veneered with VM9, cemented in a fiber reinforced epoxy resin die, and loaded to failure. Half of the specimens from each group (n = 10) were cyclic fatigued (106 cycles) before testing. Failure analysis was performed to determine the fracture origin. Data were statistically analyzed using Anova and Tukey's tests (α = 0.05). Results: The greatest mean load to fracture value was found for the G20MOD, which was predicted by the FEA. Cyclic fatigue did not significantly affect the load of fracture. Catastrophic failure originating from the internal occlusal surface of the SB was the predominant failure mode, except for G20MOD. Significance: The YZ-VM9 restorations resisted greater compression load than the usual physiological occlusal load, regardless of the TOC angle of preparations. Yet, the G20MOD design produced the best performance among the experimental conditions evaluated. © 2013 Academy of Dental Materials. Published by Elsevier Ltd. All rights reserved.