Viscosity reduction of isotonic solutions of the photosensitizer TPCS2a by cyclodextrin complexation

Meso-tetraphenyl chlorin disulphonate (TPCS_2a) is a photosensitizer (PS) particularly developed and patented for use in the technology of photochemical internalization (PCI) against cancer. TPCS_2a is known to aggregate in aqueous media even at low concentrations (≥0.1?µM) and to form a high-viscosity network at clinically relevant concentrations (mM). The aim of this work was to evaluate the effect of two hydroxypropylated cyclodextrin derivatives of beta and gamma type, respectively i.e. HPβCD and HPγCD, on the aggregation and solubilization of TPCS_2a in isotonic solutions. Samples containing micromolar concentrations of TPCS_2a were studied spectrophotometrically, while samples containing a clinical relevant concentration (10?mM?=?9?mg/ml) of TPCS_2a were evaluated by dynamic viscosity measurements. HPβCD was determined to be a more suitable solubilizer of TPCS_2a than HPγCD in aqueous media both in the absence and presence of salt. The complexation stoichiometry between TPCS_2a/HPβCD at micromolar to millimolar concentrations of TPCS_2a was determined to be 1:3 and 1:2 in the absence and presence of isotonic NaCl, respectively. The network of TPCS_2a (10?mM) was broken down in the presence of 3% w/v (=?20?mM) HPβCD, i.e. a 1:2 molar ratio between TPCS_2a and the cyclodextrin. Formation of the inclusion complex resulted in low viscosity samples both in water and in the presence of isotonic NaCl or phosphate buffered saline (PBS) at 25?°C and 37?°C.     

Comparisons of β-Hairpin Propensity Among Peptides with Homochiral or Heterochiral Strands

Assemblies of racemic β-sheet-forming peptides have attracted attention for biomedical applications because racemic forms of peptides can self-associate more avidly than do single enantiomers. In 1953, Pauling and Corey proposed “rippled β-sheet” modes of H-bond-mediated interstrand assembly for alternating L- and D-peptide strands; this structural hypothesis was complementary to their proposal of “pleated β-sheet” assembly for L-peptides. Although no high-resolution structure has been reported for a rippled β-sheet, there is strong evidence for the occurrence of rippled β-sheets in some racemic peptide assemblies. Here we compare propensities of peptide diastereomers in aqueous solution to form a minimum increment of β-sheet in which two antiparallel strands associate. β-Hairpin folding is observed for homochiral peptides with aligned nonpolar side chains, but no β-hairpin population can be detected for diastereomers in which one strand contains L residues and the other contains D residues. These observations suggest that rippled β-sheet assemblies are stabilized by interactions between β-sheet layers rather than interactions within these layers.     

Effect of glassy bonding materials on the properties of LAS/SiC porous ceramics with near zero thermal expansion

Near zero thermal expansion porous ceramics were fabricated by using SiC and LiAlSiO₄ as positive and negative thermal expansion materials, respectively, bonded by glassy material. The coefficient of thermal expansion value of a desired porous composite can be easily controlled by choosing the appropriate ratios of the different phases. It was shown that some of LiAlSiO₄ was decomposed to LiAlSi₂O₆ and LiAlO₂, some of LiAlSiO₄ reacted with SiO₂ to form LiAlSi₂O₆ during sintering. With increasing the content of glassy materials, the reaction between LiAlSiO₄ and SiO₂ was accelerated. The Young's modulus increased due to the neck growth between the SiC grains. The 52.5 vol% LiAlSiO₄ (LAS)/SiC ceramics with ∼36% porosity had a combination of near zero coefficient of thermal expansion ∼0.39 × 10⁻⁶ K⁻¹ at room temperature and relatively high Young's modulus ∼59 GPa.     

Effects of Grinding with Microcrystalline Cellulose and Cyclodextrins on the Ketoprofen Physicochemical Properties

Ground mixtures of ketoprofen (KETO) with native crystalline β-cyclodextrin, amorphous statistically substituted methyl-β-cyclodextrin, and microcrystalline cellulose were investigated for both solid phase characterization (differential scanning calorimetry (DSC) powder X-ray diffractometry, and infrared (IR) spectrometry) and dissolution properties (dispersed amount and rotating disk methods) to evaluate the role of the carrier on the performance of the final product. The effects of different grinding conditions, partial sample dehydration, and 1 year storage at room temperature were also investigated. The results pointed out the importance of the carrier nature on the efficiency of the cogrinding process. Both cyclodextrins were much more effective than was microcrystalline cellulose, even though no true inclusion complex formation occurred by mechanochemical activation. The best results were obtained from ground mixtures with methyl-β-cyclodextrin, which showed the best amorphizing and solubilizing power toward the drug and permitted an increase of approximately 100 times its intrinsic dissolution rate constant, in comparison with the approximate 10 times increase obtained from ground mixtures with β-cyclodextrin.     

High temperature bending creep behavior of a multi-cation doped α/β-SiAlON composite

SiAlON ceramics with high hardness and high toughness can be made through designing α/β-SiAlON composites. An important advantage of α-SiAlON phase is that the amount of intergranular phase is reduced by the transient liquid phase being absorbed into the matrix of α-SiAlON phase during sintering. But, the thermal stability of the α-SiAlON phase is an important concern for α/β-SiAlON composites especially at high temperatures. The use of different types of single or multiple cations during fabrication directly affects resultant microstructures and mechanical behavior of α/β-SiAlON composites. In this study, the creep behavior of a multi-cation (Y, Sm and Ca) doped α/β-SiAlON composite, in which aluminum-containing nitrogen melilite solid solution phase was designed as intergranular phase, was investigated by four-point bending creep tests under stresses from 50 to 150 MPa and at temperatures from 1300 °C to 1400 °C in air. The stress exponent was determined to be 1.6 ± 0.13 at 1400 °C and the creep activation energy was calculated to be 692 ± 37 kJ/mol⁻¹. Grain boundary sliding coupled with diffusion was identified as the rate-controlling creep mechanism for the α/β-SiAlON composite.     

A new method for the synthesis of tetrahydrothiophene-S,S-dioxide derivatives: the Michael ring closure reaction between halomethyl (E)-β-styryl sulfones and CH-acids

Bromomethyl and chloromethyl (E)-β-styryl sulfones enter a Michael ring closure reaction with sodium enolates prepared from dimethyl malonate, malononitrile and ethyl acetoacetate. The condensation results in formation of substituted tetrahydrothiophene-S,S-dioxides. It is a new instance of α-haloalkyl sulfones transformations, which are not connected with Ramberg–Bäcklund reaction.     

Immunomodulatory effect of mushrooms on cytotoxic activity and cytokine production of intestinal lamina propria leukocytes does not necessarily depend on β-glucan contents

We evaluated the effects of seven mushroom extracts (Grifola frondosa, Pholiota nameko, Panellus serotinus, Hypsizygus marmoreus, Pleurotus cornucopiae, Armillaria mellea, and Flammulina velutipes) on cytotoxic activity and cytokine production of lamina propria leukocytes (LPLs) isolated from rat small (S) and large (L) intestinal mucosa. Boiling water extracts from seven species of mushrooms showed no direct cytotoxicity against the YAC-1 target cells. However, prominent increases of cytotoxicity were observed in S- and L-LPLs co-cultured with P. serotinus extract. Cytokine production (TNFα, IFNγ, IL-12 p70, and IL-4) of S- and L-LPLs was stimulated in response to P. cornucopiae extract. Mushroom extracts contributed to target cell adhesion and/or cytokine production in the effector cells. The promotion of cytotoxic activity in S- and L-LPLs was not necessarily related to β-glucan content of the mushroom.     

长春西汀通过Wnt/GSK3β/β-catenin信号通路改善七氟醚麻醉诱导幼鼠远期学习记忆功能

目的：探讨长春西汀对七氟醚麻醉对幼鼠远期学习与记忆功能的影响及机制。方法：60只SD幼鼠,随机分为对照组、麻醉组、长春西汀低剂量组（5 mg/kg）、长春西汀高剂量组（10 mg/kg）和GSK3β抑制剂组（10 mg/kg）,每组12只。麻醉前2 h,各组幼鼠腹腔注射对应剂量药物。除对照组,各组持续吸入4%七氟醚4 h。8周后开始水迷宫实验,应用免疫荧光双染检测幼鼠脑中神经元增殖,Western blot检测海马组织中各蛋白表达。结果：训练初期各组幼鼠潜伏期没有统计学差异,第三天训练中,与对照组相比,麻醉组幼鼠到达平台潜伏期显著增加（P<0.05）;第四天训练中,与麻醉组相比,长春西汀与SB216763干预显著减少了幼鼠到达平台潜伏期（P<0.05）。且测试中,与麻醉组相比,10 mg/kg长春西汀与SB216763干预幼鼠首次达到平台潜伏期显著减少（P<0.05）,穿越平台次数显著增加（P<0.05）。与此同时,七氟醚麻醉介导了幼鼠BrdU/NeuN阳性细胞数显著减少（P<0.05）。此外,七氟醚介导海马中Wnt3a表达降低、p-GSK3β表达增加、β-catenin表达降低（P<0.05）。而长春西汀与SB216763干预显著逆转了这些细胞与蛋白表达。 结论：长春西汀通过Wnt/GSK3β/β-catenin信号通路改善七氟醚麻醉诱导幼鼠远期学习记忆功能。     

Functional Peptide Monolayers at Interfaces

Amphiphilic peptides can be designed to form ordered supramolecular structures at hydrophilic-hydrophobic interfaces. These systems rely on the ability of peptides to fold into certain secondary structures at interfaces. This review focuses on the design of amphiphilic β-sheet peptide assemblies in monolayers at interfaces, and their relevance to inducing mineralization and interactions with specific ions. In addition, the review discusses recent studies demonstrating the applicability of designed amphiphilic β-sheet peptides to detection of specific small molecules and to elucidating intermolecular interactions relevant to drug delivery and enzyme catalysis systems.     

β-FeSi_2(n)/c-Si(p)HIT型太阳能电池的模拟与优化

运用afors-het软件对β-FeSi2(n)/a-Si(i)/c-Si(p)结构的太阳能电池进行模拟,依次讨论了本征层、发射层、界面态对电池性能的影响。结果表明:添加本征层电池性能提高,但随着本征层厚度的增加载流子收集率下降、串联电阻增大,造成电池光电转化效率下降;发射层厚度的增加使得载流子的收集率下降造成光电转化效率下降,同时发射层掺杂浓度增大虽然使得内建电场强度增大,但载流子的复合也会加大,最终使得电池性能保持稳定;界面态使得电池性能下降,为使电池获得较好性能,界面态密度应尽可能小于1011 cm–2·e V–1。通过优化,最终使得该结构的太阳能电池光电转化效率达到17.00%。