2-Phenyloxazole-4-carboxamide as a Scaffold for Selective Inhibition of Human Monoamine Oxidase B

A series of 2-phenyloxazoles bearing an amide group at position 4 were designed and synthesized for evaluation as potential inhibitors of human recombinant monoamine oxidases (hrMAOs). Results of kinetics experiments demonstrated that all compounds behave as competitive MAO inhibitors, with good selectivity toward the MAO-B isoform. The most potent and selective derivatives are characterized by inhibition constant (K_i) values in the sub-micromolar range and a good selectivity index (K_{i MAO-A}/K_{i MAO-B}>50). Some derivatives were also found to be able to inhibit MAO activity in nerve growth factor (NGF)-differentiated PC12 cells, taken as a model of neuronal cells. In particular, 2-(2-hydroxyphenyl)-N-phenyloxazole-4-carboxamide (compound 4 a ) may be a promising new scaffold, exerting the highest selectivity and inhibitory effect toward MAOs in NGF-differentiated PC12 cell lysates, without compromising cell viability. Molecular docking analysis allowed a rationalization of the experimentally observed binding affinity and selectivity.     

Vacuum-u.v. circular dichroism of optically active isotactic poly-α-olefins

Summary Circular dichroism of isotactic samples of poly-(S)-4-methyl-1-hexene and poly-(R)-3,7-dimethyl-1-octene, have been measured in the vacuum ultraviolet spectral region (200-140 nm). The c.d. band at about 160. nm accounts for the optical activity in the visible region and reflects the presence of one screw sense helical conformation of the sample examined.The authors thank Prof. W.C. Johnson, Jr., Department of Biochemistry and Biophysics, Oregon State University, for allowing them to use the vacuum u.v. spectrometer. This work has been partially supported by a N.A.T.O. grant, and by Ministero Pubblica Istruzione (MPI), Roma — Italy.     

A visual news processing environment

CPP-TRS (Tonfoni 1989–94) is both a methodology and a language. Through the methodology (CPP — Communicative Positioning Program) those invisible aspects of communication are identified and represented by the meta-language (TRS — Text Representation Systems), which complements natural language. CPP-TRS is a new paradigm which applies to any communicative context.Icons in CPP-TRS are not intended to represent words or sentences in order to substitute them; they are rather intended to represent visually what natural language does not convey naturally. The improvement of communication is a challenge of the present and the future: CPP-TRS is designed explicitly for it.The CPP-TRS system thus is able to support the user with a set of visual tools, that are specifically suited to structuring text and communicating effectively.The same tools can support communication very effectively in situations where ambiguity can highly compromise the final result.The system may be used in a way that is either opaque or transparent to the reader of the text.Author of CPP-TRS¢ and CPP-TRS¢ Applications Designer.     

A porosimetric study of calcium sulfoaluminate cement pastes cured at early ages

Calcium sulfoaluminate and Portland cement pastes, both prepared with a water/solid mass ratio equal to 0.5 and cured for time periods comprised between 2 h and 28 days, show completely different pore size distributions by mercury intrusion. Portland cement pastes aged at 12 h and 1 day exhibit a unimodal distribution of pore sizes related to a continuous network of capillary pores with a threshold pore radius decreasing from nearly 650 to 350 nm. After 7 and 28 days of curing, this parameter shifts to about 150 nm and a region having smaller pores appears (with a second threshold pore radius roughly comprised between 10 and 30 nm), made discontinuous by blockages of hydration products which occlude the interconnected pore system and isolate the interior space. For calcium sulfoaluminate cement pastes, a bimodal distribution is rapidly established, in which the regions with a lower porosity (threshold pore radii up to about 25 nm) are dominant, while the decrease of total porosity almost ceases at later ages. The porosimetric behaviour of calcium sulfoaluminate-based cement is related to its very fast hydration rate and to the lack of water needed to continue the hydration reactions.     

PRILJ: an efficient two-step method based on embedding and clustering for the identification of regularities in legal case judgments

In an era characterized by fast technological progress that introduces new unpredictable scenarios every day, working in the law field may appear very difficult, if not supported by the right tools. In this respect, some systems based on Artificial Intelligence methods have been proposed in the literature, to support several tasks in the legal sector. Following this line of research, in this paper we propose a novel method, called PRILJ, that identifies paragraph regularities in legal case judgments, to support legal experts during the redaction of legal documents. Methodologically, PRILJ adopts a two-step approach that first groups documents into clusters, according to their semantic content, and then identifies regularities in the paragraphs for each cluster. Embedding-based methods are adopted to properly represent documents and paragraphs into a semantic numerical feature space, and an Approximated Nearest Neighbor Search method is adopted to efficiently retrieve the most similar paragraphs with respect to the paragraphs of a document under preparation. Our extensive experimental evaluation, performed on a real-world dataset provided by EUR-Lex, proves the effectiveness and the efficiency of the proposed method. In particular, its ability of modeling different topics of legal documents, as well as of capturing the semantics of the textual content, appear very beneficial for the considered task, and make PRILJ very robust to the possible presence of noise in the data.

     

Supervised Multivariate Analysis of Hyper-spectral NIR Images to Evaluate the Starch Index of Apples

Fruit maturity indexes are crucial in harvest time determination and commercial context. The harvest time of apples, matching the desired commercial characteristics, is assessed through starch–iodine test in practice. Fruit halves are dipped into iodine solution and patterns are visually evaluated by experts comparing them to reference charts. Aim of the work was to study the relationships of near infrared (NIR) spectral images (1,000–1,700 nm), starch/starch-free patterns visually assessed and RGB color images. Spectral images of 88 Golden Delicious Klon B apples were sampled at seven different maturity stages. Partial least-squares discriminant analysis (PLSDA) technique was used on hyper-spectral NIR images to classify single pixels using its NIR reflectance spectrum. The response variable (i.e. the classification for each pixel) was identified through the matching of single pixel obtained with the color images, segmented in two classes (starch and starch-free), and the NIR hyper-spectral matrix. Mean hyper-spectral classification obtained through PLSDA modeling on individual apple correctly classified 80.81% of the total pixels, while the unique model, i.e. a single model including all the fruits, resulted in 66.33%. In the latter case, the relationship with the RGB classification showed high values (Pearson correlation coefficient r = 0.95). The present work shows the feasibility of NIR imaging spectroscopy as a tool for apple fruit maturity determination, avoiding expert’s subjective interpretation by traditional starch index assignments.     

Colloidal lithography and Metal-Organic Chemical Vapor Deposition process integration to fabricate ZnO nanohole arrays

A complete set up of optimal process conditions for an effective colloidal lithography/catalyst assisted MOCVD process integration is presented. It mainly focuses on the determination of the deposition temperature threshold for ZnO Metal-Organic Chemical Vapour Deposition (MOCVD) as well as the concentration of metal-organic silver (Ag) catalyst. Indeed, the optimization of such process parameters allows to tailor the ZnO film morphology in order to make the colloidal lithography/catalyst assisted MOCVD approach a valuable bottom up method to fabricate bi-dimensional ordered ZnO nanohole arrays.     

Critical Review of the Evolution of Extracellular Vesicles’ Knowledge: From 1946 to Today

Extracellular vesicles (EVs) are a family of particles/vesicles present in blood and body fluids, composed of phospholipid bilayers that carry a variety of molecules that can mediate cell communication, modulating crucial cell processes such as homeostasis, induction/dampening of inflammation, and promotion of repair. Their existence, initially suspected in 1946 and confirmed in 1967, spurred a sharp increase in the number of scientific publications. Paradoxically, the increasing interest for EV content and function progressively reduced the relevance for a precise nomenclature in classifying EVs, therefore leading to a confusing scientific production. The aim of this review was to analyze the evolution of the progress in the knowledge and definition of EVs over the years, with an overview of the methodologies used for the identification of the vesicles, their cell of origin, and the detection of their cargo. The MISEV 2018 guidelines for the proper recognition nomenclature and ways to study EVs are summarized. The review finishes with a “more questions than answers” chapter, in which some of the problems we still face to fully understand the EV function and potential as a diagnostic and therapeutic tool are analyzed.     

Image Analysis Techniques for Automated Hazelnut Peeling Determination

According to FAO statistics, in 2000, Italy was the second largest hazelnut (Corylus avellana, L. 1753) producer in the world. The price of the stock depends on the nut quality (kernel/nut ratio, nut and seed defect, percentage of peeling, and taste panel scores). The evaluation of peeling efficiency after toasting is generally conducted by trained operators in sight on 100 kernels. This work tests two alternative objective methods of after toasting peeling evaluation based on image analysis. Eleven hazelnut cultivars were analyzed and results were compared with the ones assessed by trained operators. Images were analyzed with two statistical approaches: fixed values of RGB thresholding and trained K Nearest Neighbors (KNN). Root mean squared error (RMSE), estimating the comparison between operators and the two image analysis-based techniques, shows better results for KNN (6.6) with respect to fixed threshold (15.9).