Synthesis,structure–activity relationship and molecular docking of 3-oxoaurones and 3-thioaurones as acetylcholinesterase and butyrylcholinesterase inhibitors

The present study describes efficient and facile syntheses of varyingly substituted 3-thioaurones from the corresponding 3-oxoaurones using Lawesson’s reagent and phosphorous pentasulfide. In comparison, the latter methodology was proved more convenient, giving higher yields and required short and simple methodology. The structures of synthetic compounds were unambiguously elucidated by IR, MS and NMR spectroscopy. All synthetic compounds were screened for their inhibitory potential against in vitro acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. Molecular docking studies were also performed in order to examine their binding interactions with AChE and BChE human proteins. Both studies revealed that some of these compounds were found to be good inhibitors against AChE and BChE.     

Essential roles of core starvation-stress response loci in carbon-starvation-inducible cross-resistance and hydrogen peroxide-inducible adaptive resistance to oxidative challenge in Salmonella typhimurium

The starvation-stress response (SSR) of Salmonella typhimurium encompasses the physiological changes that occur upon starvation for an essential nutrient, e.g. C-source. A subset of SSR genes, known as core SSR genes, are required for the long-term starvation survival of the bacteria. Four core SSR loci have been identified in S. typhimuriumrpoSstiAstiB, and stiC. Here we report that in S. typhimurium C-starvation induced a greater and more sustainable cross-resistance to oxidative challenge (15 mM hydrogen peroxide (H₂O₂) for 40 min) than either N- or P-starvation. Of the four core SSR loci, only rpoS and stiC mutants exhibited a defective C-starvation-inducible cross-resistance to H₂O₂ challenge. Interestingly, (unadapted) log-phase S. typhimurium rpoS and stiA mutants were very sensitive to oxidative challenge. Based on this, we determined if these core SSR loci were important for H₂O₂ resistance developed during a 60 min adaptive exposure to 60 μM H₂O₂ (adapted cells). Both unadapted and adapted rpoS and stiA mutants were hypersensitive to a H₂O₂ challenge. In addition, a stiB mutant exhibited normal adaptive resistance for the first 20 mins of H₂O₂ challenge but then rapidly lost viability, declining to a level of about 1.5% of the wild-type strain. The results of these experiments indicate that: (i) the rpoS and stiC loci are essential for the development of C-starvation-inducible cross-resistance to oxidative challenge, and (ii) the rpoSstiA, and, in a delayed effect, stiB loci are needed for H₂O₂-inducible adaptive resistance to oxidative challenge. Moreover, we found that both stiA and stiB are induced by a 60 μM H₂O₂ exposure, but only stiA was regulated (repressed) by (reduced form) OxyR.     

An oxygenase enzyme system for Trametes versicolor

Abstract An oxygenase enzyme was isolated from the basidiomycete fungus Trametes versicolor , that is capable of attacking lignin and a large number of di- and tri-substituted benzene rings containing at least one hydroxy group. This enzyme system was produced late in the growth cycle without the requirement for any inducer. This non-selective enzyme system is thermophilic and operates at pH 3–5 in the presence of air or oxygen. The action of this enzyme system caused the loss of UV absorption in ferulic acid solution, the formation of hydroxy muconic semialdehyde from catechol, and transformation with the production of CO₂ from a number of hydroxy aromatics as well as lignin.     

Identification of chalcone synthase genes and their expression patterns reveal pollen abortion in cotton

Chalcone synthase (CHS) is a key enzyme and producing flavonoid derivatives as well play a vital roles in sustaining plant growth and development. However, the systematic and comprehensive analysis of CHS genes in island cotton (G. barbadense) has not been reported yet especially response to cytoplasmic male sterility (CMS). To fill this knowledge gap, a genome-wide investigation of CHS genes were studied in island cotton. A total of 20 GbCHS genes were identified and grouped into five GbCHSs. The gene structure analysis revealed that most of GbCHS genes consisted of two exons and one intron, and 20 motifs were identified. Twenty five pairs duplicated events (12 GbCHS genes) were identified including 23 segmental duplication pairs and two tandem duplication events, representing that GbCHS gene family amplification mainly owned to segmental duplication events and evolving slowly. Gene expression analysis exhibited that the GbCHS family genes presented a diversity expression patterns in various organs of cotton. Coupled with functional predictions and gene expression, the abnormal expression of GbCHS06, 10, 16 and 19 might be associated with pollen abortion of CMS line in island cotton. Conclusively, GbCHS genes exhibited diversity and conservation in many aspects, which will help to better understand functional studies and a reference for CHS research in island cotton and other plants.     

Effect of Bracteoles on Seed Germination and Dispersal of Two Species of Atriplex

The influence of bracteoles on the germination response of asalt marsh annual, Atriplex prostrata, and a salt desert perennial,A. griffithii, was determined. Attached bracteoles did not inhibitgermination of A. prostrata but completely inhibited germinationof A. griffithii seeds. Germination of seeds ofA. griffithiiwas also somewhat inhibited in the presence of detached bracteoles.The osmotic potential of dissolved substances in water-saturatedbracteoles was -4.8 ± 0.05 MPa for A. griffithii and-2.4 ± 0.15 MPa for A. prostrata. Ash content of bracteoleson a dry weight basis was 28.7 ± 0.37% for A. prostrataand 30.0 ± 0.29% for A. griffithii. The presence of relativelyhigh concentrations of dissolved salts in bracteoles may explainthe reduced germination of A. griffithii. Germination of seedsof the perennial A. griffithii may also be inhibited mechanicallyby the presence of persistent bracteoles, whereas the annualA. prostrata has ephemeral bracteoles that may serve to limitgermination in the autumn but are not present during the normalspring germination period. Bracteoles could affect the dispersalof seeds by water since some fruiting structures of A. griffithiiand A. prostrata are able to float in 1.0% NaCl solutions for5 and >30 d, respectively, compared with a maximum of 4 and3 d for seeds without bracteoles. Fruiting structures of A.prostrata floated for longer over a range of salinities thandid those ofA. griffithii ; this may play a significant rolein the dispersal of this salt marsh species. Copyright 2001Annals of Botany Company Atriplex, bracteoles, dispersal, flotation, germination, salinity, temperature     

Unsteady Magnetohydrodynamic Free Convection Flow of a Second Grade Fluid in a Porous Medium with Ramped Wall Temperature

Magnetic field influence on unsteady free convection flow of a second grade fluid near an infinite vertical flat plate with ramped wall temperature embedded in a porous medium is studied. It has been observed that magnitude of velocity as well as skin friction in case of ramped temperature is quite less than the isothermal temperature. Some special cases namely: (i) second grade fluid in the absence of magnetic field and porous medium and (ii) Newtonian fluid in the presence of magnetic field and porous medium, performing the same motion are obtained. Finally, the influence of various parameters is graphically shown.     

Perspective Texture Synthesis Based on Improved Energy Optimization

Perspective texture synthesis has great significance in many fields like video editing, scene capturing etc., due to its ability to read and control global feature information. In this paper, we present a novel example-based, specifically energy optimization-based algorithm, to synthesize perspective textures. Energy optimization technique is a pixel-based approach, so it’s time-consuming. We improve it from two aspects with the purpose of achieving faster synthesis and high quality. Firstly, we change this pixel-based technique by replacing the pixel computation with a little patch. Secondly, we present a novel technique to accelerate searching nearest neighborhoods in energy optimization. Using k- means clustering technique to build a search tree to accelerate the search. Hence, we make use of principal component analysis (PCA) technique to reduce dimensions of input vectors. The high quality results prove that our approach is feasible. Besides, our proposed algorithm needs shorter time relative to other similar methods.     

Proteomic Profiling of the TRAF3 Interactome Network Reveals a New Role for the ER-to-Golgi Transport Compartments in Innate Immunity

Tumor Necrosis Factor receptor-associated factor-3 (TRAF3) is a central mediator important for inducing type I interferon (IFN) production in response to intracellular double-stranded RNA (dsRNA). Here, we report the identification of Sec16A and p115, two proteins of the ER-to-Golgi vesicular transport system, as novel components of the TRAF3 interactome network. Notably, in non-infected cells, TRAF3 was found associated with markers of the ER-Exit-Sites (ERES), ER-to-Golgi intermediate compartment (ERGIC) and the cis-Golgi apparatus. Upon dsRNA and dsDNA sensing however, the Golgi apparatus fragmented into cytoplasmic punctated structures containing TRAF3 allowing its colocalization and interaction with Mitochondrial AntiViral Signaling (MAVS), the essential mitochondria-bound RIG-I-like Helicase (RLH) adaptor. In contrast, retention of TRAF3 at the ER-to-Golgi vesicular transport system blunted the ability of TRAF3 to interact with MAVS upon viral infection and consequently decreased type I IFN response. Moreover, depletion of Sec16A and p115 led to a drastic disorganization of the Golgi paralleled by the relocalization of TRAF3, which under these conditions was unable to associate with MAVS. Consequently, upon dsRNA and dsDNA sensing, ablation of Sec16A and p115 was found to inhibit IRF3 activation and anti-viral gene expression. Reciprocally, mild overexpression of Sec16A or p115 in Hec1B cells increased the activation of IFNβ, ISG56 and NF-κB -dependent promoters following viral infection and ectopic expression of MAVS and Tank-binding kinase-1 (TBK1). In line with these results, TRAF3 was found enriched in immunocomplexes composed of p115, Sec16A and TBK1 upon infection. Hence, we propose a model where dsDNA and dsRNA sensing induces the formation of membrane-bound compartments originating from the Golgi, which mediate the dynamic association of TRAF3 with MAVS leading to an optimal induction of innate immune responses.