乙胺硫脲抑制蘑菇酪氨酸酶活性动力学

研究了乙胺硫脲对蘑菇酪氨酸酶单酚酶和二酚酶活性的抑制效应.结果表明,乙胺硫脲对酪氨酸酶单酚酶和二酚酶活性均有抑制作用,导致单酚酶活力和二酚酶活力下降50%的乙胺硫脲浓度(IC50)分别为14.8和45.2μmol/L.在降低酪氨酸酶酶活的同时,乙胺硫脲能明显延长单酚酶和二酚酶的延滞时间.探讨了二酚酶延滞时间产生的原因:...     

十一碳烯酰基苯丙氨酸的合成及其抑制酪氨酸酶二酚酶活性的研究

以十一烯酸和苯丙氨酸为原料,使用氯化亚砜将十一烯酸酰氯化,采用肖顿-鲍曼法(Schotten-Baumann)缩合反应合成了十一碳烯酰基苯丙氨酸钠,再经酸化分离后得到了十一碳烯酰基苯丙氨酸。利用IR,MS和~1H NMR对合成产物的结构进行了表征,同时考察了十一碳烯酰基苯丙氨酸对酪氨酸酶二酚酶活性抑制的机制。结果表明,十一碳烯酰基苯丙氨酸对酪氨酸酶二酚酶活性的抑制作用为竞争性可逆抑制,其半抑制浓度为3.711 g/L,抑制常数(K_i)为3.651 g/L。     

二氟尼柳嵌入镁铝水滑石的合成表征与研究

采用共沉淀法、离子交换法和焙烧复原法三种不同方法将二氟尼柳嵌入Mg-Al水滑石层间,得到一种有机-无机复合层状材料.通过XRD、IR、TG-DTA和元素分析等手段对材料表征,结果表明,共沉淀法和离子交换法成功地将二氟尼柳嵌入水滑石,得到的材料层状结构完整、晶相单一,且层间距扩大为1.81～2.14 nm;IR分析表明二氟尼柳嵌入水滑石后,原二氟尼柳分子中的νC=O振动峰消失,在1567 cm(1和1412 cm(1处出现羧酸盐的-COO(对称与不对称吸收谱带;二氟尼柳嵌入水滑石后其分解温度提高了140～180℃.此外,根据表征结果建立了材料超分子结构模型, 即客体二氟尼柳与水滑石层板之间以静电力和氢键相互作用,以双层交替式倾斜地排列于层板之间.     

Bioactive compounds, antioxidant, xanthine oxidase inhibitory, tyrosinase inhibitory and anti-inflammatory activities of selected agro-industrial by-products

Evaluation of abundantly available agro-industrial by-products for their bioactive compounds and biological activities is beneficial in particular for the food and pharmaceutical industries. In this study, rapeseed meal, cottonseed meal and soybean meal were investigated for the presence of bioactive compounds and antioxidant, anti-inflammatory, xanthine oxidase and tyrosinase inhibitory activities. Methanolic extracts of rapeseed meal showed significantly (P < 0.01) higher phenolics and flavonoids contents; and significantly (P < 0.01) higher DPPH and nitric oxide free radical scavenging activities when compared to that of cottonseed meal and soybean meal extracts. Ferric thiocyanate and thiobarbituric acid tests results showed rapeseed meal with the highest antioxidant activity (P < 0.01) followed by BHT, cotton seed meal and soybean meal. Rapeseed meal extract in xanthine oxidase and tyrosinase inhibitory assays showed the lowest IC(50) values followed by cottonseed and soybean meals. Anti-inflammatory assay using IFN-γ/LPS stimulated RAW 264.7 cells indicated rapeseed meal is a potent source of anti-inflammatory agent. Correlation analysis showed that phenolics and flavonoids were highly correlated to both antioxidant and anti-inflammatory activities. Rapeseed meal was found to be promising as a natural source of bioactive compounds with high antioxidant, anti-inflammatory, xanthine oxidase and tyrosinase inhibitory activities in contrast to cotton and soybean meals.     

Measurement and correlation for the solid solubility of non-steroidal anti-inflammatory drugs (NSAIDs) in supercritical carbon dioxide

The solubilities for three non-steroidal anti-inflammatory drugs (NSAIDs) of nabumetone, phenylbutazone and salicylamide in supercritical carbon dioxide were measured in this study using a semi-flow type apparatus. The experimental data were taken at 308.2, 318.2 and 328.2 K, over the pressure range from 10 to 22 MPa. The measured results were then correlated using semi-empirical equation presented by Chrastil, and that presented by Mendez-Santiago and Teja. With optimally fitted parameters, these two equations yielded satisfactory results where the average absolute relative deviation (AARD) was below 7%. Furthermore, the solid solubilities of these three compounds and seven other NSAIDs in supercritical carbon dioxide were correlated by applying the regular solution model coupled with a Flory–Huggins term. The solution model, which has fewer parameters than the semi-empirical equations, yielded comparable correlation results. The parameters in the solution model could be generalized for the specific group of NSAIDs. Finally, the predicted solubilities of 10 NSAIDs in supercritical carbon dioxide were demonstrated to be reliable.     

Mechanisms of Action of Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) and Mesalazine in the Chemoprevention of Colorectal Cancer

Colorectal cancer (CRC) is the third most common malignant neoplasm worldwide. Although conclusive evidence is still lacking, epidemiologic studies suggest that long-term use of non-steroidal anti-inflammatory drugs (NSAIDs) has chemopreventive properties against CRC. Similarly, regular consumption of mesalazine, a drug structurally related to NSAIDs, seems to reduce the risk of CRC in patients with ulcerative colitis. These observations are supported by a large body of experimental data showing the ability of such drugs to inhibit multiple pathways that sustain colon carcinogenesis. This review summarizes the current information on the molecular mechanisms by which NSAIDs and mesalazine could interfere with CRC cell growth and survival.     

The effect of lanthanum oxide (La2O3) on the structure and crystallization of poly(vinylidene fluoride)

Rare earth polymers, due to their excellent luminescence, fluorescence, laser protective, optical and magnetic properties, have attracted much research attention in recent years. However, little attention has been paid to the effect of rare earths on the structure and crystallization of polymers, which is of important significance in the development of functional polymers. X‐ray diffraction and differential scanning calorimetry were used to investigate the structure and crystallization behavior of a poly(vinylidene fluoride) (PVDF)/lanthanum oxide (La₂O₃) composite. The results showed that the degree of perfection, crystal size, crystallization rate and isothermal crystallization activation energy of PVDF in the composite decreased, compared with pure PVDF. The spherulite nucleation and growth for PVDF and PVDF composite were analyzed in detail using the Lauritzen‐Hoffman equation. The modified Avrami equation and the Mo equation were used to study the non‐isothermal crystallization kinetics. The addition of La₂O₃ did not change the crystal structure and nucleation process for PVDF, but it decreased markedly the crystal growth rate and led to the formation of unstable crystals. This was attributed to the fact that too much La₂O₃ prevented PVDF molecular chains from moving and arranging in an orderly manner into crystals. Copyright © 2010 Society of Chemical Industry     

The effect of powders homogenisation conditions on the synthesis of yttrium aluminium garnet (YAG) by a solid-state reaction

The work presents results of research on the influence of the state of homogenisation of reagent powders i.e. aluminium oxide and yttrium oxide on the synthesis of yttrium aluminium garnet. Fine powders of commercial aluminium oxide and yttrium oxide were mixed in the same manner in a laboratory ball mill but under four different conditions. Three batches of powders were prepared in water of various pH values, selected on the basis of the zeta potential measurements, and one batch was prepared in propanol. They were consolidated by filter pressing and then sintered in air at a temperature from 900 °C to 1700 °C for 1 h, with heating rate of 5 °C/min. Samples were subjected to dilatometric studies, phase composition determination, measurement of apparent density and pore size distribution, as well as a microscopic examination. Mixing environment affected, to a given extent, almost all the features of green, and partially sintered materials as well as course changes of linear dimensions. As a result, the relative densities of samples sintered at a maximum temperature ranged from 58.31% to 98.25%. The highest density was achieved for the material originating from the suspension having a pH of 9.5, in which heterocoagulation occurred.     

The cooperative effect of tri(β-chloromethyl) phosphate and cyclohexyl benzene on lithium ion batteries

Tri(β-chloromethyl) phosphate (TCEP) and cyclohexyl benzene (CHB) had been studied synchronously as the additives of the lithium ion batteries to improve the high temperature and overcharge safety. The study group used the cyclic voltammetry and environment scanning electron microscopy (ESEM) to investigate the oxidize potentials of the TCEP and CHB at normal environment and 150 °C and the surface characteristics of the positive electrode of the graphite/LiCoO₂(063465) batteries before and after overcharge. The self-extinguishing time (SET) tests were carried out to measure the effect of additives on the electrolyte combustibility. The oven and overcharge tests and other electrochemical testing methods were performed to test the reliability of the protection provided by the TCEP and CHB of the high temperature and overcharge safety and the effect of the additives on the electrochemical performance. The results show that the oxidize potential of the TCEP is about 4.75 V and the CHB about 4.6 V at normal environment and the oxidize potential of the TCEP drops to 4 V and CHB about 4.1 V at 150 °C; the TCEP has favorable effect on the self-extinguish time of the electrolyte; the surface of the LiCoO₂ positive electrode after overcharge formed a layer of CHB polymer; when the content of both additives are over 5 wt%, the batteries show improved safety through the oven tests of 150 °C and can stand 1.3 A (1 C) and constant 10 V overcharge tests; the adverse effect of TCEP and CHB on cycle performance of battery is relatively small. In sum, the cooperative use of these two additives can improve the safety of lithium ion battery greatly.     

Effects of chromium (VI) on the activities of ureolytic mixed culture

BACKGROUND: Ureolytic microbial carbonate precipitation (MCP) is a novel process for removing excess calcium from industrial effluents. This process is based on the hydrolization of urea to provide a suitable medium for the precipitation of Ca as CaCO₃. RESULT: A toxicity identification evaluation was conducted on synthetic wastewater simulating wastewater from paper recycling to determine the inhibition or toxicity of chromium(VI) ions on the activities of a ureolytic mixed culture (UMC) with respect to the removal rate of COD and removal of Ca²⁺ in batch reactors. The 50% inhibiting concentration (IC₅₀) and the 25% inhibiting concentration (IC₂₅) values of Cr(VI) on UMC were determined as 40 and 18 mg L^?1, respectively, for an exposure time of 1 day. The inhibitory effects of Cr(VI) were lower on UMC after longer exposure times of 3, 4 and 5 days. COD removal rate, ammonium production and Ca removal of samples with 512 mg Cr(VI) L^?1 were significantly inhibited. CONCLUSION The present study has shown that the effects of different metallic species, organic toxicants and other environmental factors should be taken into account when removing problematic Ca and other possible elements from the environment using UMC. Copyright © 2008 Society of Chemical Industry     

The effect of additives on the thermal stability of poly(vinyl chloride)

The effect of a range of organic additives on the thermal stability of poly(vinyl chloride), both with and without a chloroparaffin extender, was studied using a number of experimental techniques. Of the additives used the best overall balance was provided by pentaerythritol, which increased stability when the extender was present and had no effect when it was absent. The congo red test emerged as the most suitable technique, being consistent and inexpensive and able to screen several additives simultaneously. Isothermal differential thermal analysis correlated with the congo red test but required more expensive equipment, was time-consuming and demanded good mixing of the poly(vinyl chloride) compound to give reproducible results. Thermogravimetry was not sufficiently sensitive and the heat stability test was the least useful of all.     

Toughening effect of EPDM-graft-methyl methacrylate and styrene (EPDM-g-MMA-St) on methyl methacrylate-styrene copolymer (MS resin)

EPDM-graft-methyl methacrylate and styrene (EPDM-g-MMA-St) was synthesized by solution graft copolymerization of methyl methacrylate (MMA) and styrene(St) onto ethylene-proplene-diene terpolymer (EPDM) in toluene/n-heptane cosolvent using benzoyl peroxide as an initiator. Fourier transform infrared spectroscopy provides a substantial evidence of grafting of MMA and St onto EPDM. EPDM-g-MMA-St/MS resin blends (MES) were prepared by melt blending EPDM-g-MMA-St and MS resin, and the toughening effects of EPDM-g-MMA-St on MS resin were studied. The results showed that the synthesized conditions of EPDM-g-MMA-St influenced the toughening effect of EPDM-g-MMA-St on MS resin. Notched Izod impact strength of MES increased with increasing grafting ratio, grafting chain polarity of EPDM-g-MMA-St, and EPDM content in MES. Differential scanning calorimetry showed that EPDM-g-MMA-St and MS resin are compatible partially and the compatibility improves with increasing grafting chain polarity of EPDM-g-MMA-St. Transmission electron microscopy and scanning electron microscopy analysis showed that the phase structure was “sea-island” structure, and the particle diameter of EPDM-g-MMA-St increased, meanwhile, surface to surface interparticle distance decreased with an increase in EPDM content, which resulted in the toughening mechanism of MES changed into slight shear yielding of matrix from the damage mode of cavitation. © 2008 Wiley Periodicals, Inc. J Appl Polym Sci, 2008     

Solvent effect on the nucleation and growth mechanisms of poly(thiophene)

Applying the step potential method, the effect of parameters such as solvent, potential, electrolyte and monomer concentration on the nucleation and growth processes of poly(thiophene) on Pt electrode in tetrabuthylammonium hexafluorophosphate-acetonitrile or dichloromethane has been studied. The j/t transients were generally fitted by means of a mathematical equation that considers different contributions. In acetonitrile the j/t transient (0<t<30 s) present three contributions corresponding to the following mechanisms: two-dimensional instantaneous nucleation (IN2D), three-dimensional progressive nucleation (PN3D_CT) under charge transfer control and three-dimensional progressive nucleation (PN3D_dif) under diffusion control. Similar results were obtained in dichloromethane, but in this case the 3D_CT nucleus presented an instantaneous nucleation mechanism (IN3D_ct). A second wave has been observed in the j/t transients obtained in CH₃CN at t>30 s, which was fitted by a mathematical equation that included two contributions corresponding to a PN3D_CT and PN3D_dif mechanisms. In general, the charge associated to each contribution depended on the solvent, the monomer and electrolyte concentration and the applied potential. However, the PN3D_CT (CH₃CN) or IN3D_CT (CH₂Cl₂) mechanisms were always the more important contributions. The scanning electron microscopy (SEM) analysis of the deposits morphology are in agreement with the nucleation and growth models that are proposed by this method.     

Study of the solvent effect on miscibility between poly(vinyl chloride) and poly(methyl methacrylate) in the solution state – viscometric measurements

In this work, the solvent effect on the miscibility between poly(vinyl chloride) (PVC) and poly(methyl methacrylate) (PMMA) in ternary polymer solutions was examined by the viscometric method. In these systems, we could understand that the used solvents, tetrahydrofuran (THF) or N,N‐dimethylformamide (DMF), mainly affect the interaction between PVC and PMMA, while prompting various miscible properties. In PVC/PMMA/THF solution, THF is a near θ‐solvent and a poor solvent for PVC and PMMA, respectively. The mixing of the tighter PMMA coils and more extended PVC coils in THF may cause the sea–island heterogeneous structure below the weight fraction of PMMA in the polymer mixture w_PMMA = 0.7, resulting in immiscible PVC/PMMA mixtures. At w_PMMA ≥ 0.7, the PVC/PMMA mixtures are relatively miscible, giving homogeneous polymer solutions. It means that the miscibility between PVC and PMMA depends on the composition of polymer mixture. However, due to the similar affinity of DMF to PVC and PMMA, PVC/PMMA/DMF solutions exhibit high miscibility between PVC and PMMA at about w_PMMA = 0.5. © 2000 Society of Chemical Industry     

The effect of poly(ethylene glycol) mixed with poly(l‐lactic acid) on the crystallization characteristics and properties of their blends

The non‐isothermal and isothermal crystallizations of extruded poly(l ‐lactic acid) (PLLA) blends with 10, 20 and 30 wt% poly(ethylene glycol) (PEG) were investigated with differential scanning calorimetry. The formation of α‐form crystals in the blend films was verified using X‐ray diffraction and an increase in crystallinity indexes using Fourier transformation infrared spectroscopy. Crystallization and melting temperatures and crystallinity of PLLA increased with decreasing cooling rate (CR) and showed higher values for the blends. Although PLLA crystallized during both cooling and heating, after incorporation of PEG and with CR = 2 °C min^?1 its crystallization was completed during cooling. Increasingly distinct with CR, a small peak appeared on the lower temperature flank of the PLLA melting curve in the blends. A three‐dimensional nucleation process with increasing contribution from nuclei growth at higher CR was verified from Avrami analysis, whereas Kissinger's method showed that the diluent effect of 10 and 20 wt% PEG in PLLA decreased the effective energy barrier. During isothermal crystallization, crystallization half‐time increased with temperature (T_ic) for the blends, decreased with PEG content and was lower than that of pure PLLA. In addition, the Avrami rate constants were significantly higher than those of pure PLLA, at the lower T_ic. Different crystal morphologies in the PLLA phase were formed, melting in a broader and slightly higher T_m range than pure PLLA. The crystallization activation energy of PLLA decreased by 56% after the addition of 10 wt% PEG, increasing though with PEG content. Finally, PEG/PLLA blends presented improved flexibility and hydrophilicity. © 2019 Society of Chemical Industry     

The effect of thiol content on the gelation and mucoadhesion of thiolated poly(aspartic acid)

A synthetic poly(amino acid), poly(aspartic acid) modified with thioethyl side groups, was studied as an in situ gelling and mucoadhesive dosage form. The chemical structure and the controllable, large thiol content of the polymer were confirmed using ¹H NMR spectroscopy and Ellman's assay. In situ gelation of aqueous polymer solutions was induced by oxidation and monitored using oscillation rheometry. The strength of mucoadhesion towards excised mucosa was characterised by tensile tests in ex vivo experiments. Release kinetics of ophthalmic antibiotic ofloxacin was studied from an in situ crosslinked hydrogel and a liquid formulation to prove the sustained release of the former. © 2017 Society of Chemical Industry     

The effect of nanoscale vanadium pentoxide on the electrical and mechanical properties of poly(vinyl alcohol)

Poly(vinyl alcohol) (PVA) loaded with vanadium pentoxide (V₂O₅) nanoparticles was successfully prepared at room temperature and ambient pressure. Transmission electron microscopy was used to characterize the final product. It was found that V₂O₅ nanoparticles were well dispersed and uniform in shape and that the diameter of the particles was confined to within 8 nm. Addition of small amounts (0.2–1 wt%) of nanoparticulate V₂O₅ to PVA increased the electrical conductivity as well as the modulus of elasticity. The deformation behaviour after preparing the nanocomposites, irrespective of V₂O₅ concentration, is similar to that of the unfilled elastomer, implying that the mechanism of large deformation is mainly governed by the matrix. Copyright © 2007 Society of Chemical Industry     

The effect of NaCl on the eutectic phase behavior of aqueous poly(ethylene glycol) solutions

The phase behaviors of aqueous polymer solutions are known to be affected by the presence of ions even if the polymer itself does not have any charges. We studied the effect of salt (sodium chloride) on the eutectic phase behavior of non-ionic polymer, poly(ethylene glycol) (PEG) in aqueous solutions using differential scanning calorimetry. We observed that the addition of NaCl increased the liquidus temperature of PEG and decreased that of water. As a result, a steep rise (or fall) is induced in the liquidus around the eutectic point. A simple Flory-Huggins lattice model for the mixture (PEG-water-NaCl) was applied to the experimental results. The model quantitatively reproduced the change in the liquidus both with and without NaCl. The obtained interaction parameters suggest that the increase of the PEG melting temperature by NaCl can be understood as the depletion of NaCl around PEG, possibly due to the image charge repulsion.