Synthesis and anticonvulsant activity of 7-benzylamino-4,5-dihydro-［1,2,4］triazolo［4,3-a］quinolines

A series of 7-substituted-benzylamino-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinoline derivatives was synthesized and evaluated for their anticonvulsant activity.The subcutaneous pentylenetetrazole test(sc-PTZ)demonstrated that the most effective compound in controlling the sc-PTZ induced seizure was 7-(3-bromine-benzylamino)-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinoline(4j)with an ED50 of 5.0 mg/kg and the PI of 20.7,which was also safer than the reference drugs.And the maximal electroshock test(MES)demonstrated that among these derivatives,7-(3-fluorobenzylamino)-4,5-dihydro-[1,2,4]trizolo[4,3-a]quinoline(4i),with an ED50 of 15.3 mg/kg and the PI of 7.2,was the safest in MES test.Furthermore,their neurotoxicities were measured by the rotarod neurotoxicity test,and the results showed that all derivatives possessed lower neurotoxicity.     

7取代苄氨基4,5二氢［1,2,4］三唑并［4,3a］ 喹啉类衍生物的合成及抗惊厥作用研究

合成7-取代苄氨基-4,5-二氢-［1,2,4］三唑并［4,3-a］喹啉类衍生物，并进行了抗惊厥作用研究.抗戊四唑(PTZ)实验结果显示，7-（3-溴苄氨基）-4,5-二氢-［1,2,4］三唑并［4,3-a］喹啉(4j)的作用最强，其ED₅₀为5.0mg/kg，保护指数PI为 20.7，作用明显强于对照药物，安全性也明显优于对照药物;而抗电惊厥实验结果表明，7-（3-氟苄氨基）-4,5-二氢-［1,2,4］三唑并［4,3-a］喹啉(4i) 的作用最强，其ED₅₀为15.3mg/kg，保护指数PI为 7.2. 同时用旋转棒法测定了化合物的神经毒性，其结果显示目标化合物的神经毒性均较低.     

Cu3Au薄膜中的［001］方向反相畴界

The order-disorder transition of the Cu₃Au film system is simulated by the Monte Carlo method. The computational results show that the antiphase boundaries in the film have different properties with antiphase boundaries in the bulk. The kind of ［001］ antiphase boundaries in the film is determined by the parity of the layer number of the film. For even-layer number film, only the non- conservative antiphase boundaries appear in the film; for the odd-layer number film, only conservative antiphase boundaries may appear. Like the situation in the bulk materials, the simulation indicates that only the non-conservative antiphase boundary wet.     

Effect of TiO_2 nanoparticles on hydrogen evolution reaction activity of Ni coatings

The electrocatalytic activity of electrodeposited Ni and Ni–TiO_2 coatings with regard to the alkaline hydrogen evolution reaction(HER) was investigated. The Ni coatings were electrodeposited from an acid chloride bath at different current densities, and their HER activities were examined in a 1.0-mol·L~(-1) KOH medium. The variations in the HER activity of the Ni coatings with changes in surface morphology and composition were examined via the electrochemical dissolution and incorporation of nanoparticles. Electrochemical analysis methods were used to monitor the HER activity of the test electrodes; this activity was confirmed via the quantification of gases that evolved during the analysis. The obtained results demonstrated that the Ni–TiO_2 nanocomposite test electrode exhibited maximum activity toward the alkaline HER. The surface appearance, composition, and the phase structure of all developed coatings were analyzed using scanning electron microscopy(SEM), energy dispersive spectroscopy(EDS), and X-ray diffraction(XRD), respectively. The improvement in the electrocatalytic activity of Ni–TiO_2 nanocomposite coating toward HER was attributed to the variation in surface morphology and increased number of active sites.     

In vitro degradation and biocompatibility of Mg-Nd-Zn-Zr alloy

In this study,in vitro degradation and biocompatibility of Mg-Nd-Zn-Zr(NZK) alloy were investigated to determine its suitability as a degradable medical biomaterial.Its corrosion properties were evaluated by static immersion test,electrochemical corrosion test,scanning electron microscopy(SEM),and energy dispersive spectroscopic(EDS) analysis,and in vitro biocompatibilities were assessed by hemolysis and cytotoxicity tests.Pure magnesium was used as control.The results of static immersion test and electrochemical corrosion test in simulated body fluid(SBF) demonstrated that the addition of alloying elements could improve the corrosion resistance.The hemolysis test found that the hemolysis rate of calcium phosphate coated NZK alloy was 4.8%,which was lower than the safe value of 5%.The cytotoxicity test indicated that NZK alloy extracts did not significantly reduce MC3T3-E1 cell viability.Hemolysis test and cytotoxicity test display excellent hemocompatibility and cytocompatibility of NZK alloy in vitro.Our data indicate that NZK alloy has excellent biocompatibility and thus can be considered as a potential degradable medical biomaterial for orthopedic applications.     

Abnormal infrared effects of nanometer scale thin film material of PtPd alloy in CO adsorption

Nanometer scale thin film material of PtPd alloy supported on glassy carbon (nm-PtPd/GC) was prepared by the electrochemical codeposition method under cyclic voltammetric conditions. STM patterns demonstrated that the prepared thin films are composed of layered crystallites in elliptic form. Electrochemical in situ FTIRS studies explored the abnormal infrared effects (AIREs) of nm- PtPd/GC for CO adsorption, which are (ⅰ) the remarkable enhancement of IR absorption, (ⅱ) the inversion of CO_ad band direction, and (ⅲ) notable increase in the full width at half maximum (FWHM) of CO_ad bands. The results demonstrated also that the enhancement factor of IR absorption varies with the thickness of PtPd alloy film and has reached a maximum value of 38.3 under the experimental conditions.     

Peat molecular fossils recording paleoclimatic change and organism replacement

The occurrence of the dominant C₂₃ n-alkane derived from bryophyte was demonstrated to be related to the cold climate, based on the GC and GC/MS analyses on a 40-cm long peat core, in which this compound exponentially varies in abundance with the depth corresponding to the well-known second Little Ice Age. Both the variation of the chemical components of modern bryophyte resulted from climatic change and the ecological data about the biological growth influenced by climate shed light on the point that the variation of this compound in the peat was related to the cold climate. This was also evidenced by the previously-reported lacustrine data. In addition, the variations of the ratios of ketones/esters and C₂₄ n-alkene/n-alkane (C_24︰1/C_24︰0) display the trend identical with that of organisms, implicating the replacement between bryophyte and monocotyledon occurring in the peat core.     

Restorable variation of cytoplasmic type of male sterile line in rice byin vitro culture

Rice male sterile (MS) lines, IR66707A and IR69700A, which possess the cytoplasm of Oryza perennis and O. glumaepatula respectively, belong to the cytoplasmic type. Their sterility could be maintained but not be restored. By somatic cell culture of these two MS lines, 47 somaclones with 465 R₁ plants were obtained. All of the 465 R₁ plants were sterile in the spring season in Guangzhou. According to the expression of the R₁ plants and the level of similarity to their donor parents, they could be divided into three types. The plants of type Ⅰ were male sterile. The sterility of some somaclones of this type could be restored by the test crossing varieties or alternated to fertile by changes of some environmental conditions. The hybrid F₁ of test cross from the MS somaclones in type Ⅰ was fertile while the hybrid F₁ from the donor MS lines was still sterile. The R₁ plants of type Ⅱ were similar to the donor parents and also male sterile. The hybrid F₁ from all of the plants of type Ⅱ crossed to test variety were still sterile, so they did not possess restorability. For the somaclone of type Ⅲ, all of R₁ plants were sterile in both male and female organs. No seed was set in both conditions of self and cross pollination. The fact that the restorable variants obtained in the cytoplasmic type of MS lines of rice by in vitro culture reported here should be the first sample in somaclonal variation in plant kingdom.     

Searching for more effective HCV NS3 protease inhibitors via modification of corilagin

Corilagin was seperated from extract of Phyllanthus urinaria L. and used as the precursor of inhibitors of hepatitis C virus (HCV) NS3 serine protease. Six derivatives were obtained through the chemical modification of corilagin and their structures were elucidated by the spectra analysis. Bioassay of these compounds showed that two of them had improved inhibitory efficiency than the precursor, with IC₅₀ values of 2.28 μmol/L and 1.52 μmol/L, respectively. The binding mode of two active compounds with substrate binding site of HCV NS3 protease was also investigated by molecular docking method.     

Neural correlates of moral judgment of lying： An event-related-potential study

The present study investigated neural mechanisms of moral judgment of lying in adults using high-density event-related potentials (ERPs). Participants were recruited to do moral judgment of 200 stories including two types of lying and their corresponding truth-telling. The results showed that both types of lying were judged more negative than their corresponding truth-telling, and moral judgment of black lying was more negative than that of modest lying. There were two main components of the ERPs evoked by the test stimuli. One was an early component, peaking at about 200 ms, and the other was a late component, peaking at about 400 ms. Over the frontal scalp sites, the early component was positive and the late component was negative, while they both reversed over the posterior sites. The ERPs of both types of lying was more positive than that of their corresponding truth-telling in the time window of 600—900 ms at the posterior sites.     

Synthesis of Water-dispersed Polyurethane Adhesive and Its Application in Pigment Printing

Water-dispersed polyurethane (PU) adhesive is a novel and highly efficient adhesive with broad application potential. In this study, the key parameters affecting the synthesis and application of this adhesive were examined, and optimal conditions were identified. The water-dispersed PU adhesive was successfully synthesized, and applied in the fastness test of pigment printing on cotton fabric. The data demonstrated that all the fastnesses of PU adhesive were better than that of the cenventional PA one.     

Sticking-up Behaviors and Surface Friction of IF Electrogalvanized Sheet Steel in Forming

X-ray diffraction (XRD), ball-disc friction and wearing machine and draw-bead test were introduced to investigat the strcusture and workability of IF sheet steel electrogalvanized deposits prepared from sulphate solution system. It was shown that the picking-up of the zinc coating on die strengthened with the increasing of friction factor which was originally affected by the coating’s structure. Duing forming, (00X) planes (X=2, 4) preferential orientation of zinc deposits increased, which resulted in enhancing the coating’s friction behaviors. Therefore, the forming mechanism of electrogalvedzed deposit was demonstrated that both friction and the stricking-up behaviors of the coating are intensified simultaneously and affect each other.     

Separation of Purine and Its Derivatives by Capillary Zone Electrophoresis

The separation of a group of 17 purine and its derivatives by capillary zone electrophoresis is presented. A systematic approach was used to study the effect of pH, buffer type, organic modifiers, applied potential, sodium dodecyl sulfate (SDS) and cyclodextrins on the separation of these purine derivatives. An ideal condition was found for their separation, which was 30 mmol/L sodium borate buffer (pH 9-9. 5), 10% (V/V) methanol buffer modifier and 20 kV. Under this condition, the 17 purine derivatives were baseline separated and the linear correlation coefficient for adenine, uric acid and 2-thioxanthine was 0. 99 over two orders of magnitude. The variation of peak areas was less than 4. 6% (n=5) and that of migration times was in the range of 0%-3%, while the samples were injected hydrodynamically at a height of 15 cm and an injection time of 8-10 s. In addition, alcohol, 1-propanol, 1-butanol and acetonitrile were also effective additives in the separation. However, SDS and various ###-cyclodextrin     

Quantitative structure activity relationship and toxicity mechanisms of chlorophenols on cells <Emphasis Type="Italic">in vitro</Emphasis>

3-(4,5-dimethylthiazd-2-yl)-2,5-diphenylentrazolium bromide (MTT) reduction assay was used to investigate the acute toxicity of 8 different chlorophenols (CPs) on rat connective tissue fibroblast L929 cells and human liver cancer HepG2 cells. Combined with the data from Quantitative Structure Activity Relationship (QSAR) approach of CPs by using the octanol-water partition coefficients (Kow),an effective model was deduced to evaluate the cytotoxicity of these chemicals. Furthermore, the relationship between the structures of CPs and their cytotoxicity was proposed.The results show that 2-chlorophenol (2-CP), 4-chlorophenol (4-CP), 2,6-dichlorophenol (2,6-DCP),2,4-dichlorophenol (2,4-DCP),2,4,6-trichlorophenol (2,4,6-TCP) and 2,3,4-trichlorophenol (2,3,4-TCP) induced apoptosis, whereas, 2,3,5,6-tetrachlorophenol (2,3,5,6-TeCP) and pentachlorophenl (PCP) demonstrated more characteristic of necrosis than apoptosis.These results establish a good experimental base both for developing the comparative evaluation of toxicity of CPs in vitro and for elucidating the toxicity mechanisms of them.     

Effect of TiO<Subscript>2</Subscript> nanoparticles on hydrogen evolution reaction activity of Ni coatings

The electrocatalytic activity of electrodeposited Ni and Ni-TiO₂ coatings with regard to the alkaline hydrogen evolution reaction (HER) was investigated. The Ni coatings were electrodeposited from an acid chloride bath at different current densities, and their HER activities were examined in a 1.0-mol·L-1 KOH medium. The variations in the HER activity of the Ni coatings with changes in surface morphology and composition were examined via the electrochemical dissolution and incorporation of nanoparticles. Electrochemical analysis methods were used to monitor the HER activity of the test electrodes; this activity was confirmed via the quantification of gases that evolved during the analysis. The obtained results demonstrated that the Ni-TiO₂ nanocomposite test electrode exhibited maximum activity toward the alkaline HER. The surface appearance, composition, and the phase structure of all developed coatings were analyzed using scanning electron microscopy (SEM), energy dispersive spectroscopy (EDS), and X-ray diffraction (XRD), respectively. The improvement in the electrocatalytic activity of Ni-TiO₂ nanocomposite coating toward HER was attributed to the variation in surface morphology and increased number of active sites.     

High-pressure and high-temperature synthesis of MgB2 and its superconductivity

The single-phase sample of MgB₂ was prepared successfully at the temperature of 900℃ and under the pressure of 3 GPa. The structure of the sample was investigated using powder X-ray diffraction and Rietveld analysis. The results show that the structure of the sample belongs to the hexagonal structure with space group of P6/mmm, a=3.0861(5) Å, c=3.5222(8) Å. The magnetic and resistance measurements indicate that the superconducting transition temperature T_c is 39 K.     

Microstructure and wear resistance of PTA clad Cr7C3/γ-Fe ceramal composite coating

A wear resistant Cr₇C₃/γ-Fe ceramal composite coating was fabricated on substrate of the hardening and tempering C degree steel by PTA (plasma transferred arc) cladding with (wt%) Fe-25Cr-7C elemental powder blends. Microstructure of the coating was characterized by OM, SEM, XRD and EDS. Wear resistance of the coating was tested under dry sliding wear condition at room temperature. The results indicate that the PTA clad ceramal composite coating has a rapidly solidified fine microstructure consisting of Cr₇C₃ primary particles uniformly distributed in the γ-Fe matrix and is metallurgically bonded to the C degree steel substrate. The PTA clad Cr₇C₃/γ-Fe ceramal composite coating has high hardness and excellent wear resistance under dry sliding wear test conditions. The excellent wear resistance of the Cr₇C₃/γ-Fe ceramal composite coating is attributed to the coating’s high hardness, strong covalent atomic bonding and refined microstructure.     

Microstructure and wear resistance of PTA clad Cr7C3/γ-Fe ceramal composite coating

A wear resistant Cr₇C₃/γ-Fe ceramal composite coating was fabricated on substrate of the hardening and tempering C degree steel by PTA (plasma transferred arc) cladding with (wt%) Fe-25Cr-7C elemental powder blends. Microstructure of the coating was characterized by OM, SEM, XRD and EDS. Wear resistance of the coating was tested under dry sliding wear condition at room temperature. The results indicate that the PTA clad ceramal composite coating has a rapidly solidified fine microstructure consisting of Cr₇C₃ primary particles uniformly distributed in the γ-Fe matrix and is metallurgically bonded to the C degree steel substrate. The PTA clad Cr₇C₃/γ-Fe ceramal composite coating has high hardness and excellent wear resistance under dry sliding wear test conditions. The excellent wear resistance of the Cr₇C₃/γ-Fe ceramal composite coating is attributed to the coating’s high hardness, strong covalent atomic bonding and refined microstructure.     

Integration and inheritance stability of foreignBt toxin gene in the bivalent insect-resistant transgenic cotton plants

Genetic and expressional stability of Bt toxin gene is crucial for the breeding of insect-resistant transgenic cotton varieties and their commercialization. Genomic Southern blot analysis of R₃, R₄ and R₅ generations of bivalent transgenic insect-resistant cotton plants was done in order to determine the integration, the copy number and the inheritance stability of Bt toxin gene in the transgenic cotton plants. The results indicated that there was a 4.7 kb positive band in the Southern blot when the genomic DNA of the bivalent transgenic insect-resistant cotton plants and the positive control (the plasmid) were digested with HindⅢ respectively. This result proved that the Bt toxin gene had been integrated into the genome of the cotton in full length. There is only one XhoⅠ restriction site in the Bt toxin gene. Southern blot analysis indicated that many copies of Bt toxin gene had been integrated into the genome of the cotton when the genomic DNA of transgenic plants was digested with XhoⅠ. Among them, there were four copies (about 17.7, 8, 5.5 and 4.7 kb in size) existing in all the tested plants of ₃, R₄ and R₅ generations. The preliminary conclusion was that there were more than four copies of Bt toxin gene integrated into the genome of the cotton, among them, more than one copy can express and inherit steadily. This result provides a scientific basis for the breeding of the bivalent insect-resis- tant transgenic cotton plants and its commercialization.     

Influence of nanometric CeO2 coating on high temperature oxidation of Cr

Isothermal and cyclic oxidation behavior of chromium and its superficially applied nanometric CeO₂ samples were studied at 900℃ in air. Scanning electronic microscopy (SEM), transmission electronic microscopy (TEM) and high resolution electronic microscopy (HREM) were used to examine the morphology and micro-structure of oxide films. It was found that ceria addition greatly improved the anti-oxidation ability of Cr both in isothermal and cyclic oxidizing experiments. Acoustic emission (AE) technique was used in situ to monitor the cracking and spalling of oxide films, and AE signals were analyzed in time-domain and number-domain according to the related oxide fracture model. Laser Raman spectrometer was also used to study the stress status of oxide films formed on Cr with and without ceria. The main reason for the improvement in anti-oxidation of chromium was that ceria greatly reduced the growing speed and grain size of Cr₂O₃. This fine-grained Cr₂O₃ oxide film might have better high temperature plasticity and could relieve parts of compressive stress by means of creeping, and maintained the ridge character and relatively low internal stress level. Meanwhile, ceria application reduced the size and the number of interfacial defects, while remarkably enhanced the adhesive property of Cr₂O₃ oxide scale formed on Cr substrate.