Inclusion complexation of (11-ferrocenylundecyl)trimethylammonium bromide by β-cyclodextrin and its effects on electrochemical behavior of the surfactant

This report describes the influence of β-cyclodextrin complexation on thermodynamic and kinetic parameters of the electrode reaction of (11-ferrocenylundecyl)trimethylammonium bromide in aqueous media. The host attracted the reduced form having a less positive charge more strongly than the corresponding oxidized one. Thus, a hydrophobic interaction between the non-polar host cavity and the ferrocene moiety plays an important role in the inclusion complexation. Fast-scan voltammetric behavior of the amphiphilic ion suggested that inclusion-ejection processes practically attain equilibrium in the scan-rate range below 10 V s⁻¹, because of their fast rates. The relation between the peak current and peak potential leads to the conclusion that the enveloped guest exchanges no electrons directly with an electrode. The mean diffusion coefficient of the surfactant can be written as a linear combination of the contributions from a free monomolecular, a micelle-forming, and a host-bound surfactant. Since the binding affinity of the ferrocene moiety for the host cavity is much stronger than the aggregation force between the amphiphilic molecules in aqueous media, the host disrupts the micelles by incorporating the surfactant molecule into its cavity.     

Electrochemical investigation of uranium β-diketonates for all-uranium redox flow battery

The redox flow battery using uranium as the negative and the positive active materials in polar aprotic solvents was proposed. In order to establish the guiding principle for the uranium compounds as the active materials, the investigation of uranium β-diketonate complexes was conducted on (i) the solubility of active materials, (ii) the electrode reaction of U(VI) and U(IV) β-diketonate complexes and (iii) the estimation of the open circuit voltage of the battery. The solubilities of higher than 0.8 mol dm⁻³ of U(VI) complexes and higher than 0.4 mol dm⁻³ of a U(IV) complex were obtained in the solvents. The electrode reactions of U(pta)₄, UO₂(dpm)₂, UO₂(fod)₂ and UO₂(pta)₂ were first studied and the redox potentials of uranium β-diketonates were thermodynamically discussed. The open circuit voltage is estimated more than 1 V by using Hacac or Hdpm. The larger open circuit voltage is expected when a ligand with the larger basicity is used.     

缺氧诱导因子-1α与Wnt/β-catenin信号通路在缺氧胃癌细胞中的相互作用

目的在缺氧环境下,探讨缺氧诱导因子-1α(Hypoxia-inducible factor-1α,HIF-1α)与Wnt/β-catenin信号通路在胃癌细胞SGC-7901中的相互作用。方法将质粒β-catenin-micRNA转染SGC-7091细胞,筛选稳定转染细胞株SGC-7901-β-catenin-micRNA。将SGC-7901细胞分为对照组、脂质体组和阴性对照组,对照组:常氧培养48 h;脂质体组:常氧培养24 h后,加入10μl脂质体,培养24 h;阴性对照组:常氧培养24 h后,转染阴性对照质粒,培养24 h;设稳定转染细胞株为干扰组,常氧培养48 h。采用倍增时间试验、平板克隆形成试验及流式细胞术检测各组细胞倍增时间、平板克隆集落数及细胞周期的变化。另取SGC-7901细胞,分为对照组、缺氧组、双重缺氧组;对照组:常氧培养48 h;缺氧组:常氧培养32 h,物理缺氧培养16 h;双重缺氧组:常氧培养24 h,化学缺氧培养8 h后,再同时物理缺氧培养16 h。同时取稳定转染细胞株,分为对照干扰组、缺氧干扰组和双重缺氧干扰组。对照干扰组:常氧培养48 h;缺氧干扰组:常氧培养32 h,物理缺氧培养16 h;双重缺氧干扰组:常氧培养24 h,化学缺氧培养8 h后,再同时物理缺氧培养16 h。采用RT-PCR和Western blot法检测各组细胞中HIF-1α、β-catenin的mRNA及蛋白的表达水平。结果与对照组、脂质体组、阴性对照组比较,干扰组倍增时间延长,平板克隆集落数减少,细胞阻滞在G1期比例增加,S期减少,差异均有统计学意义(P<0.05)。缺氧组与对照组、双重缺氧组与缺氧组、缺氧干扰组与对照干扰组及双重缺氧干扰组与缺氧干扰组相比,HIF-1α、β-catenin的mRNA及蛋白表达水平均升高,差异有统计学意义(P均<0.05)。缺氧干扰组与缺氧组及双重缺氧干扰组与双重缺氧组比较,β-catenin、HIF-1α的mRNA及蛋白表达水平均降低,差异有统计学意义(P均<0.05)。结论 HIF-1α激活可调控Wnt/β-catenin通路,但也受控于Wnt/β-catenin通路,二者之间相互影响,相互调节。     

Halogenation of β-keto-sulfones using KX/H2O2 in aqueous medium: Synthesis of α-halo β-keto-sulfones and α-halomethyl sulfones

Synthesis of α-halo β-keto-sulfones and α-halomethyl sulfones is described by the reaction of β-keto-sulfones with potassium halides in the presence of hydrogen peroxide in aqueous acidic medium afforded the corresponding α-halo β-keto-sulfones at room temperature in excellent yields. Further the α-halo β-keto-sulfones on treatment of aqueous alkali underwent base-induced cleavage to yield α-halomethyl sulfones.     

Calcium phosphate bioceramics synthesized from eggshell powders through a solid state reaction

Everyday millions of tons of eggshells are produced as biowaste around the world. Most of this waste is disposed of in landfills without any pretreatment. Eggshells in landfills produce odors and promote microbial growth as they biodegrade. The present invention provides an environmentally beneficial and cost-effective method of producing calcium phosphate bioceramics (hydroxyapatite or tricalcium phosphate) from eggshell waste. In this investigation, heat treatment produced solid state reactions between eggshell powders and dicalcium phosphate dihydrate (CaHPO₄·2H₂O, DCPD) or calcium pyrophosphate (Ca₂P₂O₇). When eggshell powders (CaO) and DCPD were heat treated at 1150 °C for 3 h, only a single hydroxyapatite (HA) phase was found; no diffraction peaks of starting materials and no β-TCP were observed. The XRD patterns of the product fabricated from raw eggshell powders (CaCO₃) and Ca₂P₂O₇ heat treated at 1100 °C for 3 h showed that almost only pure β-TCP remained with a trace amount of HA. The calcium phosphate ceramic synthesized from eggshell powders contains several important trace elements such as Na, Mg and Sr.     

Growth and microstructure of Ba β-alumina films by laser chemical vapor deposition

Ba β-alumina films were prepared by laser chemical vapor deposition. Mostly single-phase Ba β-alumina films were obtained at 1125–1200 K and for an Al/Ba molar ratio of 12.4–16.6. BaAl₂O₄ and α-Al₂O₃ were codeposited with Ba β-alumina under Ba- and Al-rich conditions, respectively. The Ba β-alumina films consisted of hexagonal grains, and the (1 1 0)-oriented Ba β-alumina films had a fin-like columnar structure. The highest deposition rate reached 120 μm h^?1 at around 1200 K. A thin layer of Ba-rich superstructure was formed on the surface of the (1 1 0)-oriented columnar grains.     

Cefuroxime-impregnated calcium phosphates as an implantable delivery system in experimental osteomyelitis

The study aimed to investigate the effectiveness of porous calcium phosphates viz., hydroxyapatite (HAp) and a bi-phasic calcium phosphate (BCP) with predominately β-tricalcium phosphate (β-TCP) prepared by aqueous solution combustion method impregnated with cefuroxime axetil for the treatment of experimental osteomyelitis and compared with parenteral treatment. In vitro release of the drug was tested for its sustained elution characteristics for 21 days in PBS (pH 7.2) and measured by HPLC. In the in vivo study, bone infection was induced in tibia of rabbits by inoculation of 1 ml (3 × 10⁶) CFU Staphylococcus aureus. On the 21st day, after the development of osteomyelitis, six animals were treated by filling the cavity with cefuroxime-impregnated HAp blocks (Group II), six animals with the same drug-impregnated β-TCP (Group III) and in six others, only cefuroxime (15 mg/kg twice daily) was injected parenterally 6 weeks (Group IV). Group I with six animals was kept untreated. Histologically, the signs of infection were found to subside by 3 and 6 weeks. Radiological evaluation with cefuroxime-impregnated HAp and β-TCP pointed out the disappearance of sequestrum and existence of newly formed bony specules. Concentration of cefuroxime in bone and serum as estimated by HPLC showed highest value on day 21 itself which reduced marginally by day 42 in both the groups and these values were higher than minimum inhibitory concentration (MIC) against S. aureus. Our findings suggest that bi-phasic calcium phosphates with predominately β-TCP content is a very efficient carrier material for antibiotic compounds even for refractory infections by S. aureus.     

β-七叶皂苷钠在脑缺血再灌注大鼠体内药代动力学的研究

目的: 研究β-七叶皂苷钠在脑缺血再灌注大鼠体内的药代动力学规律。方法: 应用酶联免疫吸附分析(ELISA, enzyme-linked immunosorbent assay) 检测方法, 测定正常大鼠及脑缺血大鼠经静脉注射β-七叶皂苷钠5 mg·kg^-1后β-七叶皂苷钠的血药浓度,并对其药物代谢动力学参数进行研究。结果: 脑缺血再灌注及正常大鼠静脉注射β-七叶皂苷钠5mg·kg^-1后, 其药代动力学模型符合二室模型。正常大鼠在静脉注射β-七叶皂苷钠后, 血药浓度迅速下降, 大约20 min 后, 其血浆药物浓度已下降50 %,T_1/2α=0.343 h, T_1/2β =23.325 h 。约2 h 后, 血浆药物浓度下降速率减慢。而脑缺血再灌注大鼠脑缺血30 min 后, 静脉注射β-七叶皂苷钠后, 其体内药物代谢规律与正常大鼠不同, 药物的代谢速率减慢, 且在3 h 出现一个较低的血药浓度峰, 随后血浓下降。结论: β-七叶皂苷钠在脑缺血再灌注大鼠体内的消除较正常大鼠慢, 在体内停留的时间较长。提示β-七叶皂苷钠在临床的对症治疗时应考虑其药代动力学的特点。     

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.     

Exogenous Integrin αIIbβ3 Inhibitors Revisited: Past,Present and Future Applications

The integrin αIIbβ3 is the most abundant integrin on platelets. Upon platelet activation, the integrin changes its conformation (inside-out signalling) and outside-in signalling takes place leading to platelet spreading, platelet aggregation and thrombus formation. Bloodsucking parasites such as mosquitoes, leeches and ticks express anticoagulant and antiplatelet proteins, which represent major sources of lead compounds for the development of useful therapeutic agents for the treatment of haemostatic disorders or cardiovascular diseases. In addition to hematophagous parasites, snakes also possess anticoagulant and antiplatelet proteins in their salivary glands. Two snake venom proteins have been developed into two antiplatelet drugs that are currently used in the clinic. The group of proteins discussed in this review are disintegrins, low molecular weight integrin-binding cysteine-rich proteins, found in snakes, ticks, leeches, worms and horseflies. Finally, we highlight various oral antagonists, which have been tested in clinical trials but were discontinued due to an increase in mortality. No new αIIbβ3 inhibitors are developed since the approval of current platelet antagonists, and structure-function analysis of exogenous disintegrins could help find platelet antagonists with fewer adverse side effects.