Evaluation of Potential Xanthine Oxidase Inhibitors by Molecular Docking and Bioassays

For decades, the inhibition of the enzyme xanthine oxidase (XO) by compounds such as allopurinol has been used as an effective treatment of gout. More recently, XO has been implicated in ischemia-reperfusion injury and has emerged as a target for drugs against hyperuricemia and cancer. For the structure-based design of novel XO inhibitors, a validated docking protocol and a reliable bioassay are needed. We successfully docked the structure of the XO inhibitors lumazine and febuxostat into the X-ray crystal structure of XO. Furthermore, we established a bioassay that monitors XO’s activity by measuring the rate of urate production at 290 nm. The assay was performed on a 96-well microplate that permitted the simultaneous testing of eight compounds at twelve different inhibitor concentrations. In order to develop structure-activity relationships, analogues of known inhibitors were identified for experimental testing via similarity and substructure searches of several compound libraries

Microwave transparent catalytic falling-film microreactor for automated operation

Falling‐film microreactors at different scales were developed to study heterogeneously catalyzed gas‐liquid reactions under microwave irradiation, as part of the EU FP7 project MAPSYN. At pilot scale, this device formed the core part of a fully automated demonstration plant which was used for semi‐hydrogenation reactions at an industrial site. The microchannels of the reaction plate were coated with novel selective catalysts. A special fiber‐optical sensor applicable under microwave irradiation and needed for controlling the liquid level in the sump via the flow rate of the discharge pump was developed and electrically connected with the automation system

Mitochondrial DNA analyses of the saltwater crocodile (Crocodylus porosus) from the Northern Territory of Australia

The saltwater crocodile is distributed throughout south-east Asia and Australia. In Australia, it is most abundant in the Northern Territory and Queensland, where it is sustainably farmed for its skins and meat. The aim of this study was to elucidate the relationships and genetic structure among saltwater crocodiles from the Northern Territory of Australia using mitochondrial control region sequences from 61 individuals, representing nine river basins and six of unknown origin, as well as published sequences from other regions. Eight mitochondrial control region haplotypes were identified among both published and novel sequences. Three of the haplotypes appear to be restricted to specimens from northern Australia, with a single haplotype being the most widely dispersed across all river basins. Although Analysis of Molecular Variance provides some support for differentiation among river basins, the frequency of shared haplotypes among these geographical units and median-joining network analysis do not support a clear genetic structure or phylogeographic pattern for saltwater crocodiles in the Northern Territory. The results of this study will assist in furthering our understanding of the genetic diversity of wild saltwater crocodile populations used for ranching in the Northern Territory, as well as providing a framework for assessing the origin of unknown specimens in the future.8 page(s