Methane aromatization over Mo/H-ZSM-5: on the reaction pathway

Rates of benzene formation on Mo/HZSM-5, H-ZSM-5 and Mo/SiO₂ were measured with different reactants: methane, mixture of C₂H₄/H₂/N₂ and mixture of C₂H₂/H₂/N₂. Since the rate of benzene formation starting from C₂H₄/H₂/N₂ is higher on Mo/H-ZSM-5 compared to H-ZSM-5 it is concluded that the aromatization of methane on Mo/H-ZSM-5 is not going via ethylene which is aromatized over acid sites. Another reaction pathway is proposed. This revised version was published online in July 2006 with corrections to the Cover Date.     

Modified Fluoroquinolones as Antimicrobial Compounds Targeting Chlamydia trachomatis

Chlamydia trachomatis causes the most common sexually transmitted bacterial infection and trachoma, an eye infection. Untreated infections can lead to sequelae, such as infertility and ectopic pregnancy in women and blindness. We previously enhanced the antichlamydial activity of the fluoroquinolone ciprofloxacin by grafting a metal chelating moiety onto it. In the present study, we pursued this pharmacomodulation and obtained nanomolar active molecules (EC₅₀) against this pathogen. This gain in activity prompted us to evaluate the antibacterial activity of this family of molecules against other pathogenic bacteria, such as Neisseria gonorrhoeae and bacteria from the ESKAPE group. The results show that the novel molecules have selectively improved activity against C. trachomatis and demonstrate how the antichlamydial effect of fluoroquinolones can be enhanced.     

Role of ERAB/L-3-hydroxyacyl-coenzyme A dehydrogenase type II activity in Abeta-induced cytotoxicity

Endoplasmic reticulum-associated amyloid beta-peptide (Abeta)-binding protein (ERAB)/L-3-hydroxyacyl-CoA dehydrogenase type II (HADH II) is expressed at high levels in Alzheimer's disease (AD)-affected brain, binds Abeta, and contributes to Abeta-induced cytotoxicity. Purified recombinant ERAB/HADH II catalyzed the NADH-dependent reduction of S-acetoacetyl-CoA with a Km of approximately 68 microM and a Vmax of approximately 430 micromol/min/mg. The contribution of ERAB/HADH II enzymatic activity to Abeta-mediated cellular dysfunction was studied by site-directed mutagenesis in the catalytic domain (Y168G/K172G). Although COS cells cotransfected to overexpress wild-type ERAB/HADH II and variant beta-amyloid precursor protein (betaAPP(V717G)) showed DNA fragmentation, cotransfection with Y168G/K172G-altered ERAB and betaAPP(V717G) was without effect. We thus asked whether the enzyme might recognize alcohol substrates of which the aldehyde products could be cytotoxic; ERAB/HADH II catalyzed oxidation of a variety of simple alcohols (C2-C10) to their respective aldehydes in the presence of NAD+ and NAD-dependent oxidation of 17beta-estradiol. Addition of micromolar levels of synthetic Abeta(1-40) to purified ERAB/HADH II inhibited, in parallel, reduction of S-acetoacetyl-CoA (Ki approximately 1.6 microM), as well as oxidation of 17beta-estradiol (Ki approximately 3.2 microM) and (-)-2-octanol (Ki approximately 2.6 microM). Because micromolar levels of Abeta were required to inhibit ERAB/HADH II activity, whereas Abeta binding to ERAB/HADH II occurred at much lower concentrations (Km approximately 40-70 nM), the latter more closely simulating Abeta levels within cells, Abeta perturbation of ERAB/HADH II was likely to result from mechanisms other than the direct modulation of enzymatic activity. Cells cotransfected to overexpress ERAB/HADH II and betaAPP(V717G) generated malondialdehyde-protein and 4-hydroxynonenal-protein epitopes, which were detectable only at the lowest levels in cells overexpressing either ERAB/HADH II or betaAPP(V717G) alone. Generation of such toxic aldehydes was not observed in cells contransfected to overexpress Y168G/K172G-altered ERAB and betaAPP(V717G). We conclude that the generalized alcohol dehydrogenase activity of ERAB/HADH II is central to the cytotoxicity observed in an Abeta-rich environment.     

Determinants of right–left and top–bottom prevalence for two-dimensional spatial compatibility.

When stimulus and response sets vary along horizontal and vertical dimensions, the horizontal dimension is more dominant than the vertical one, an effect called right–left prevalence. Three accounts have been proposed that attribute the effect to a reduced ability to code vertical locations when horizontal codes are also present, the use of right–left effectors, or a difference in salience of the 2 dimensions. The accounts differ in terms of whether the ability to code and process the 2 dimensions is of limited capacity and whether the prevalence effect is a consequence of the effectors used for responding. The authors report 4 experiments that evaluated these issues. Results indicate that use of right–left effectors is important to the right–left prevalence effect because it increases the salience of the horizontal dimension. However, a top–bottom prevalence effect can be obtained if the vertical dimension is made more salient. (PsycINFO Database Record (c) 2010 APA, all rights reserved)     

压缩系统对温度突升响应的动态分析

基于时间滞后概念,建立了压缩系统动态响应分析的通用模型,并对温度突升条件下多级轴流压缩系统的动态响应及气动稳定性进行了详细的数值分析。对两个算例的分析,结果表明了本文新模型的可行性。     

Cyclic stretch down-regulates calcium transporter gene expression in neonatal rat ventricular myocytes

Abnormal intracellular Ca2+ handling in hypertrophied and failing hearts is partly due to changes in Ca2+ transporter gene expression, but the mechanisms responsible for these alterations remain largely unknown. We previously showed that intrinsic mechanical load (i.e. spontaneous contractile activity) induced myocyte hypertrophy, and down-regulated SR Ca2+ ATPase (SERCA2) gene expression in cultured neonatal rat ventricular myocytes (NRVM). In the present study, we examined whether extrinsic mechanical load (i.e. cyclic stretch) also induced NRVM hypertrophy, and led to down-regulation of SERCA2 and other Ca2+ transporter genes which have been associated with cardiac hypertrophy and failure in vivo. NRVM were maintained in serum-free culture medium under control conditions, or subjected to cyclic mechanical deformation (1.0 Hz, 20% maximal strain, 48 h). Under these conditions, cyclic stretch induced NRVM hypertrophy, as evidenced by significant increases in total protein/DNA ratio, myosin heavy chain (MHC) content, and atrial natriuretic factor (ANF) secretion. Cyclic stretch also induced the MHC isoenzyme "switch" which is characteristic of hemodynamic overload of the rat heart in vivo. Cyclic stretch significantly down-regulated SERCA2 and ryanodine receptor (RyR) mRNA and protein levels, while simultaneously increasing ANF mRNA. In contrast, Na+-Ca2+ exchanger and phospholamban mRNA levels were unaffected. Load-dependent SERCA2 and RyR down-regulation was independent of Ca2+ influx via voltage-gated, L-type Ca2+ channels, as cyclic stretch down-regulated SERCA2 and RyR mRNA levels in both control and verapamil-treated NRVM. These results indicate that extrinsic mechanical load (in the absence of other exogenous stimuli) induces NRVM hypertrophy and causes down-regulation of Ca2+ transporter gene expression. This in vitro model system should prove useful to dissect the intracellular signaling pathways responsible for transducing this phenotype during cardiac hypertrophy and heart failure in vivo.     

Efficient and accurate multilayer solid‐shell element: non‐linear materials at finite strain

We present in this paper an efficient and accurate low‐order solid‐shell element formulation for analyses of large deformable multilayer shell structures with non‐linear materials. The element has only displacement degrees of freedom (dofs), and an optimal number of enhancing assumed strain (EAS) parameters to pass the patch tests (both membrane and out‐of‐plane bending) and to remedy volumetric locking. Based on the mixed Fraeijs de Veubeke‐Hu‐Washizu (FHW) variational principle, the in‐plane and out‐of‐plane bending behaviours are improved and the locking associated with (nearly) incompressible materials is avoided via a new efficient enhancement of strain tensor. Shear locking and curvature thickness locking are resolved effectively by using the assumed natural strain (ANS) method. Two non‐linear 3‐D constitutive models (Mooney–Rivlin material and hyperelastoplastic material at finite strain) are applied directly without requiring the enforcement of the plane‐stress assumption. In particular, we give a simple derivation for the hyperelastoplastic model using spectral representations. In addition, the present element has a well‐defined lumped mass matrix, and provides double‐side contact surfaces for shell contact problems. With the dynamics referred to a fixed inertial frame, the present element can be used to analyse multilayer shell structures undergoing large overall motion. Numerical examples involving static analyses and implicit/explicit dynamic analyses of multilayer shell structures with both material and geometric non‐linearities are presented, and compared with existing results obtained from other shell elements and from a meshless method. It is shown that elements that did not pass the out‐of‐plane bending patch test could not provide accurate results, as compared to the present element formulation, which passed the out‐of‐plane bending patch test. The present element proves to be versatile and efficient in the modelling and analyses of general non‐linear composite multilayer shell structures. Copyright © 2005 John Wiley & Sons, Ltd.     

The stress stability of olanzapine: studies of interactions with excipients in solid state pharmaceutical formulations

Stress stability testing represents an important part of the drug development process. It is used as an important tool for the identification of degradation products and degradation pathways, as well as for the assessment of changes in physical form of drug molecules. The impact of excipients on the stability of olanzapine confirms that levels of impurities and degradants are limiting parameters and are therefore used for stability evaluation. The major degradation product of olanzapine was identified as 2-methyl-5,10-dihydro-4H-thieno[2,3-b][1,5]benzodiazepine-4-one (III). The structure of III was determined by using LC-MS, IR and NMR. Compatibility and stress stability results demonstrated that tablet formulations of olanzapine are sensitive to temperature and moisture. In samples protected from moisture, the increase in concentration of III was shown to be highly temperature dependent and the degradation followed zero-order kinetics. In addition, studies of olanzapine with excipients and in formulated tablets revealed polymorphic phase changes in some samples, influenced by a combination of stress temperature and humidity conditions. Polymorphic transitions were monitored using x-ray powder diffraction (XRPD) analysis and exhibited no correlation between the phase change (appearance of a new polymorph) and the degradation process.     

A four‐node corotational quadrilateral elastoplastic shell element using vectorial rotational variables

A four‐node corotational quadrilateral elastoplastic shell element is presented. The local coordinate system of the element is defined by the two bisectors of the diagonal vectors generated from the four corner nodes and their cross product. This local coordinate system rotates rigidly with the element but does not deform with the element. As a result, the element rigid‐body rotations are excluded in calculating the local nodal variables from the global nodal variables. The two smallest components of each nodal orientation vector are defined as rotational variables, leading to the desired additive property for all nodal variables in a nonlinear incremental solution procedure. Different from other existing corotational finite‐element formulations, the resulting element tangent stiffness matrix is symmetric owing to the commutativity of the local nodal variables in calculating the second derivative of strains with respect to these variables. For elastoplastic analyses, the Maxwell–Huber–Hencky–von Mises yield criterion is employed, together with the backward‐Euler return‐mapping method, for the evaluation of the elastoplastic stress state; the consistent tangent modulus matrix is derived. To eliminate locking problems, we use the assumed strain method. Several elastic patch tests and elastoplastic plate/shell problems undergoing large deformation are solved to demonstrate the computational efficiency and accuracy of the proposed formulation. Copyright © 2013 John Wiley & Sons, Ltd.     

Software development for the 8052AH-basic microcontroller

Application software for Intel's 8052AH-basic microcontroller can be developed in MCS basic-52, an enhanced version of basic, using the onchip basic interpreter. The paper explores the 8052AH-basic device and its language in comparison with the standard Microsoft basic and presents some software routines and other guidelines for programmers. Control-oriented applications, as opposed to conventional number-crunching applications, are emphasized. The paper also discusses how the resources of the Intellec development system can be used to facilitate the development of application software.