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981.
Lidia Moreira Lima Tiago Fernandes da Silva Carlos Eduardo da Silva Monteiro Cristiane Aparecida-Silva Walfrido Bispo Júnior Aline Cavalcanti de Queiroz Magna Suzana Alexandre-Moreira Gisele Zapata-Sudo Eliezer J. Barreiro 《Molecules (Basel, Switzerland)》2021,26(16)
Acylhydrazones are still an important framework to the design of new bioactive compounds. As treatment of chronic pain represents a clinical challenge, we decided to modify the structure of LASSBio-1514 (1), previously described as anti-inflammatory and analgesic prototype. Applying the homologation as a strategy for molecular modification, we designed a series of cyclopentyl- (2a–e), cyclobutyl- (3a–e), and cyclopropylacylhydrazones (4a–e) that were synthetized and evaluated in murine models of inflammation and pain. A comparison of their in silico physicochemical and drug-like profile was conducted, as well as their anti-inflammatory and analgesic effect. Compounds 4a (LASSBio-1755) and 4e (LASSBio-1757) displayed excellent in silico drug-like profiles and were identified as new analgesic lead-candidates in acute and chronic model of pain, through oral administration. 相似文献
982.
Arlindo Csar Matias Pereira Helison de Oliveira Carvalho Danna Emanuelle Santos Gonalves Karyny Roberta Tavares Picano Abraho Victor Tavares de Lima Teixeira dos Santos Heitor Ribeiro da Silva Francinaldo Sarges Braga Roberto Messias Bezerra Alessandro de Sousa Nunes Maira Tiyomi Sacata Tongo Nazima Júlia Gomes Cerqueira Talisson Taglialegna Janayra Maris Teixeira Jos Carlos Tavares Carvalho 《Molecules (Basel, Switzerland)》2021,26(16)
This study aimed to evaluate and compare the effects of co-treatment with purified annatto oil (PAO) or its granules (GRA, Chronic®) with that of testosterone on the orchiectomy-induced osteoporosis in Wistar rats. After surgery, rats were treated from day 7 until day 45 with testosterone only (TES, 7 mg/kg, IM) or TES + PAO or GRA (200 mg/kg, p.o.). The following parameters were evaluated: food/water intake, weight, HDL, LDL, glucose, triglycerides (TG), total cholesterol (TC), alkaline phosphatase levels, blood phosphorus and calcium contents, femur weight, structure (through scanning electron microscopy), and calcium content (through atomic absorption spectrophotometry). Our results show that orchiectomy could significantly change the blood lipid profile and decrease bone integrity parameters. Testosterone reposition alone could improve some endpoints, including LDL, TC, bone weight, and bone calcium concentration. However, other parameters were not significantly improved. Co-treatment with PAO or GRA improved the blood lipid profile and bone integrity more significantly and improved some endpoints not affected by testosterone reposition alone (such as TG levels and trabeculae sizes). The results suggest that co-treatment with annatto products improved the blood lipid profile and the anti-osteoporosis effects of testosterone. Overall, GRA had better results than PAO. 相似文献
983.
L.M. da Silva M.C. de Melo A.N. Medina F.G. Gandra 《Physica B: Condensed Matter》2009,404(19):3018-3020
We report on results of X-ray powder diffraction, magnetization and specific heat measurements of the pseudo-ternary (Ce1−xLax)PdIn2 system with x=0; 0.2; 0.4 and 0.6. The results show a linear increase of the unit cell volume and a reduction of the ferromagnetic transition as La content increases. The Debye temperature, Sommerfeld coefficient and crystal field parameters were estimated from specific heat data, and are found to be weakly dependent of the Ce concentration. Also, the variation of magnetic entropy at TC is only weakly dependent on x (ΔS≅0.92Rln2) indicating that TK/TC is approximately constant along the series. The TC and TK behaviors are explained by the variation of the exchange parameter due to the volume change when Ce is replaced by La. Our results indicate that the chemical pressure is the dominant effect rather than the chemical disorder for determining the physical proprieties of the (Ce1−xLax)PdIn2 system. 相似文献
984.
D. S. L. Pontes E. Longo F. M. Pontes M. S. Galhiane L. S. Santos Marcelo A. Pereira-da-Silva J. H. D. da Silva A. J. Chiquito P. S. Pizani 《Applied Physics A: Materials Science & Processing》2009,96(3):731-740
Ferroelectric Pb1−x−y
Ca
x
Sr
y
TiO3 thin films (denoted by PCST90, PCST70, and PCST30) were deposited on the Pt/Ti/SiO2/Si substrates by a chemical solution deposition method. Their properties were investigated from the viewpoint of crystal
structure, microstructure, dielectric, and ferroelectric properties. X-ray diffraction patterns revealed the formation of
PCST90, PCST70, and PCST30 thin films without any secondary phases. Infrared and Raman spectroscopy results show that a gradual
phase transition from tetragonal to pseudocubic or cubic perovskite structure may occur in PCST thin films with the simultaneous
increase of Ca2+ and Sr2+ contents. Both substitution of isovalent Ca2+ and Sr2+ at Pb2+-site enhanced the dielectric constant and reduced the remnant polarization. In addition, ferroelectric test analyses show
that the PCST thin films undergo a ferroelectric-to-paraelectric phase transformation with an amount of Pb2+, Ca2+, and Sr2+ at 30%, 35%, and 35% mol, respectively. Hence, the absence of ferroelectric property may be attributed to a decreasing of
the octahedron distortion in the perovskite structure accompanied by a weakening of long-range ferroelectric order. 相似文献
985.
L.C. Alves M.G.S. Cavalcanti H.R.C. Araújo G.M. Silva D.L. Veras M.H.S. Paiva F.A. Brayner 《Micron (Oxford, England : 1993)》2009,40(5-6):659-664
Single dose of diethylcarbamazine (DEC) used in control programs is effective in breaking the transmission of filariasis. In order to investigate the effect of aggressive therapy on Wuchereria bancrofti (Wb) microfilariae, DEC was given to 29 patients who were positive for the circulating filarial antigen (CFA) assay but did not have clinical manifestations of filariasis, at 6 mg/kg/day for 12 days and again six months later using the same dosing regimen. For each patient, microfilarial density and serum CFA were followed up for two years. Ultrastructural analyses on Wb microfilariae obtained after repeated treatment with DEC were also performed. Microfilaremia and antigenemia decreased significantly after 12 months but returned to the initial levels after 24 months. This could indicate, as shown by other authors, that aggressive repeated therapy with DEC alone is ineffective in eradicating adult W. bancrofti, particularly in infected but asymptomatic individuals. The objective of the present study was to analyze the microfilaremic and antigenemic behavior and ultrastructural changes caused by different DEC concentrations in vitro in Wb microfilariae obtained from individuals who were sensitive and refractory to treatment. After in vitro treatment of the microfilariae using 5 and 10 μg/ml of DEC for 1 h, ultrastructural analysis revealed low levels of cell damage compared with embryos obtained from individuals from a different area who had never received DEC treatment before. The results obtained suggest that microfilariae from patients who receive repeated aggressive therapy are less sensitive to DEC in vitro. 相似文献
986.
L. R. Calixto M. C. Bandéca F. B. Silva A. N. S. Rastelli S. T. Porto-Neto M. F. Andrade 《Laser Physics》2009,19(8):1867-1871
The purpose of this study was to evaluate the effectiveness of different light-curing units on the bond strength (push-out) of glass fiber posts in the different thirds of the root (cervical, middle and apical) with different adhesive luting resin systems (dual-cure total-etch; dual-cured and self-etch bonding system; and dual-cure self-adhesive cements), Disks of the samples (n = 144) were used, with approximately 1 mm of thickness of 48 bovine roots restored with glass fiber posts, that were luted with resin cements photo-activated by halogen LCU (QTH, Optilux 501) and blue LED (Ultraled), with power densities of 600 and 550 mW/cm2, respectively. A universal testing machine (MTS 810 Material Test System) was used with a 1 mm diameter steel rod at cross-head speed of 0.5 mm/min until post extrusion, with load cell of 50 kg, for evaluation of the push-out strength in the different thirds of each sample. The push-out strength values in kgf were converted to MPa and analyzed through Analysis of Variance and Tukey’s test, at significance level of 5%. The results showed that there were no statistical differences between the QTH and LED LCUs. The self-adhesive resin cement had lower values of retention. The total-etch and self-adhesive system resin cements seem to be a possible alternative for glass fiber posts cementation into the radicular canal and the LED LCU can be applied as an alternative to halogen light on photo-activation of dual-cured resin cements. 相似文献
987.
J. M. Silva E. Drigo Filho J. R. Ruggiero 《The European physical journal. E, Soft matter》2009,29(2):245-251
This paper studies energy localization conditions in lattices of the type proposed by Peyrard and Bishop. Homogeneous and
inhomogeneous lattices are analyzed and the role of interfaces in the latter is emphasized. Simulations allowed us to identify
critical energy values for the existence of localization. After a certain energy value, it is possible to observe the loss
of energy localization along the chain. 相似文献
988.
989.
S.?Denifl I.?M?hr F.?Ferreira da Silva F.?Zappa T. D.?M?rk P.?Scheier 《The European Physical Journal D - Atomic, Molecular, Optical and Plasma Physics》2009,51(1):73-79
Here we report electron impact ionization studies with the amino acid valine in different environments, i.e., (i) isolated
in the gas phase, (ii) embedded in superfluid helium droplets and (iii) co-embedded with water in superfluid helium droplets.
Mass spectra are presented for all three environments for which changes in the fragmentation pattern of valine upon ionization
are investigated. Comparison is made with previous electron impact ionization and photoionization studies with valine in the
gas phase which confirms the fragile nature of this amino acid. Embedding valine in cold superfluid helium droplets leads
to the formation of highly abundant protonated valine clusters. Co-embedding water with valine in helium droplets reduces
fragmentation of valine. 相似文献
990.
Érica L. Silva Thales R.F. Pontes Bárbara L. Francelino E. Sócrates T. do Egito Artur S. Carriço 《Journal of magnetism and magnetic materials》2009,321(10):1566-1570
We report a study to develop a magnetic system for local delivery of amoxicillin. Magnetite microparticles produced by coprecipitation were coated with a solution of amoxicillin and Eudragit®S100 by spray drying. Scanning electron microscopy, optical microscopy, X-ray powder diffraction and vibrating sample magnetometry revealed that the particles were superparamagnetic, with an average diameter of 17.2 μm, and an initial susceptibility controllable by the magnetite content in the suspension feeding the sprayer. Our results suggest a possible way to treat Helicobacter pylori infections, using an oral drug delivery system, and open prospects to coat magnetic microparticles by spray drying for biomedical applications. 相似文献