Web-based monitoring tool of the Atlantic Ocean observing system (Europe)

Web-based service tool that monitor data flow and key performance indicators of the Atlantic observing system. The focus here is on the monitoring of European contributions, including the EuroGOOS Atlantic ROOSES

Growth and dissection of a fold and thrust belt: the geological record of the High Agri Valley, Italy

We present a 130 km2 wide geological map for the NE side of the fault-bounded High Agri Valley Southern Italy, that formed in the Quaternary in response to extensional tectonics dissecting the folds and thrusts of the Lucanian Apennine. To prepare the map, at 1:25,000 scale, we integrated information obtained through field surveys and the review of pre-existing geological data. Our work describes a number of significant map-scale structures, which can be related to well-constrained tectonic episodes. The new geological map provides important constraints that can be used to distinguish ancient structures from those that were active during the Quaternary, allowing a more detailed reconstruction of the processes that operate during the development of a post-orogenic trough. We expect that the new map will be used for different types of geological investigations, including studies of inversion tectonics, active tectonics, geosite mapping, 3D modelling of geological structures. © 2020, © 2020 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group on behalf of Journal of Maps

Reaction between quinone and thiazolidine. A study on the formation mechanism of new antiproliferative quinolindiones

Reaction between quinolinquinone and thiazolidine in basic medium was investigated. 2-Arylthiazolidine-4-carboxylic acid ethyl esters undergo two different cleavages in basic medium, yielding the 1-aryl-2-azadiene and a thiolic species. In the presence of quinolinquinone, the isomeric 1-aryl-3-ethoxycarbonyl-pyridoisoquinolin-5,10-diones and 3-amino-3-ethoxycarbonyl-dihydrothienoquinolin- 4,9-diones are formed by a hetero-Diels–Alder reaction and 1,4-Michael addition reaction, respectively. A mechanism for the formation of the reaction products is presented

Discovery of a Novel Small Molecule Inhibitor Targeting the Frataxin/Ubiquitin Interaction via Structure-Based Virtual Screening and Bioassays

Friedreich ataxia (FRDA) is an autosomal recessive neuro- and cardiodegenerative disorder for which there are no proven effective treatments. FRDA is caused by decreased expression and/or function of the mitochondrial protein frataxin. Here, we report findings that frataxin is degraded via the ubiquitin-proteasomal pathway and that it is ubiquitinated at residue K147 in Calu-6 cells. A theoretical model of the frataxin-K147/Ub complex, constructed by combining bioinformatics interface predictions with information-driven docking, revealed a hitherto unnoticed, potential ubiquitin-binding domain in frataxin. Through structure-based virtual screening and cell-based assays, we discovered a novel small molecule (compound (+)-11) able to prevent frataxin ubiquitination and degradation. (+)-11 was synthesized and tested for specific binding to frataxin by an UF-LC/MS based ligand-binding assay. Follow-up scaffold-based searches resulted in the identification of a lead series with micromolar activity in disrupting the frataxin/Ub interaction. This study also suggests that frataxin could be a potential target for FRDA drug development

Exploiting the indole scaffold to design compounds binding to different pharmacological targets

Several indole derivatives have been disclosed by our research groups that have been collaborating for nearly 25 years. The results of our investigations led to a variety of molecules binding selectively to different pharmacological targets, specifically the type A γ-aminobutyric acid (GABAA) chloride channel, the translocator protein (TSPO), the murine double minute 2 (MDM2) protein, the A2B adenosine receptor (A2B AR) and the Kelch-like ECH-associated protein 1 (Keap1). Herein, we describe how these works were conceived and carried out thanks to the versatility of indole nucleus to be exploited in the design and synthesis of drug-like molecules

Design and pharmacological evaluation of Ibuprofen amides derivatives as dual FAAH/COX inhibitors

Fatty acid amide hydrolase (FAAH) is a serine hydrolase enzyme responsible of the hydrolytic degradation of N-acylethanolamine endocannabinoids, such as the Arachidonoylethanolamide (anandamide, AEA), which it has been shown to alleviate pain and inflammation (1). In particular, the anti-nociceptive and anti-inflammatory effects of AEA could be enhanced by the simultaneous block of FAAH and COX enzymes (2). For this reason, several studies have been carried out in order to develop new FAAH/COX inhibitors (2). In 1997 it was reported that the NSAID ibuprofen inhibited FAAH, although with a modest potency (3), and successively the first dual inibhitor, the amide derivative of ibuprofen with a 2-amino-3-methylpyridine side chain (Ibu-AM5) was reported (4). -5). Benzylamides and piperazinoamides analogs of Ibuprofen have been also designed as less potent FAAH inhibitors than Ibu-AM5 (5). Here, I discuss the computational studies and the structure–activity relationships leading to the design, of novel Ibuprofen amide derivatives with a higher inhibition potency of FAAH and COX, which represent novel powerful anti-nociceptive agents

Installation of Passive Radar Corner Reflectors at the SENSE study site; Hatfield Moors, Doncaster.

This report describes the installation of Radar Corner Reflectors (CRs) at the SENSE study site on Hatfield Moors near Doncaster, Yorkshire, England. It describes the need for the CRs on the study site, the specification, painting and modifications required for this site. It then describes the installation procedure and presents preliminary results in the satellite radar data

Genotoxicity assessment of three nutraceuticals containing natural antioxidants extracted from agri-food waste biomasses

Grapes and apples are the most cultivated fruits in the Mediterranean basin and their agricultural processing is responsible for the production of a large amount of bio-waste. The reuse of this food biomass would increase the volume of recyclable/renewable biomaterial and lower the environmental impact due to the increasing demand for these biological products. To this purpose, agri-food waste from grape and apple processing have become an important source of phytochemicals, and many pharmaceutical industries are using it as starting material to produce dietary supplements, functional foods, and food additives for human consumption. In virtue of the chemical diversity and complexity of agri-food biowaste, developers and producers of nutraceuticals are advised to assess the safety of their final nutraceutical products, in compliance with European Food Safety Authority regulation. Here, we use the Ames test to assess the mutagenicity of three nutraceuticals obtained from agri-food waste biomasses: Taurisolo® from grape pomace of Vitis vinifera L. cv 'Aglianico', AnnurComplex® from Malus pumila M. cv 'Annurca' and Limoncella Apple Extract from Malus domestica B. cv 'Limoncella'. The results showed that all three nutraceuticals were non-mutagenic

A bottom-up building stock quantification methodology for construction minerals using Earth Observation. The case of Hanoi

Increasing demand for significant volumes of construction materials, especially sand for use in concrete, in rapidly developing urban environments is becoming a significant socio-economic and environmental issue. The consumption of concrete (comprised of sand, aggregates and cement) is especially concerning on a city level as vast volumes of materials are extracted within the urban hinterland, causing direct impacts locally and the potential for supply issues directly impacting city level metabolism. Excessive consumption and poor management of these materials make it increasingly hard for society to ensure new urban development and infrastructure projects, essential for maintaining the health of cities, meet sustainable development objectives. However, it is difficult to implement suitable resource management policies without first understanding how materials are produced and consumed at an appropriate spatial level. For many areas, especially on a city level, such data is absent, especially so for sand and aggregates which can further exacerbate these local supply issues and environmental impacts. This study attempts to address this data gap via combining earth observation datasets with estimates of materials contained within urban infrastructure (material intensities) to calculate the rapid increase of construction material stocks in Hanoi. Spatial data on buildings have been gathered using, producing, and collating a variety of spaceborne open-source datasets on built up areas (GlobalMLBuildingFootpint, World Settlement Footprint 3D, Open Street Map) and land use classification maps. Linking this spatial data with estimated quantities of sand, gravel, cement and concrete in typical buildings in Hanoi enables quantification of building stocks for a range of building types over a time series. The results show that for every new km2 of urban infrastructure approximately 520,000 tonnes of concrete, or 360,000 tonnes of sand, 580,000 tonnes of gravel and 115,000 tonnes of cement are required. If the Hanoi Masterplan is to be achieved by 2030, then the material demand is likely to be for 106 million tonnes of concrete or 73 million tonnes of sand, 118 million tonnes of gravel and 24 million tonnes of cement. These all exceed historical consumption trends and are far in excess of current extraction rates and therefore careful planning is required to ensure access to sustainable resources into the future

May Polyphenols Have a Role Against Coronavirus Infection? An Overview of in vitro Evidence

The coronavirus infection is constantly diffusing worldwide and the incidence of death is dramatically increasing, representing one of the greatest disasters in human history. Nowadays, no effective therapeutic approaches have been licensed, despite the rising interest of the scientific research in this specific field, and the daily growing number of publications, while the need to find novel strategies is urgent. Evidence in the literature reported the antiviral activity of polyphenols, the largest class of bioactive compounds in nature. Interestingly, a limited number of studies investigated the efficacy of polyphenols from different raw materials, directly against coronaviruses. The present manuscript aimed to report this evidence and provide a viewpoint on the possibility to use it as a start point for the development of novel natural approaches against this viral infection, eventually designing further appropriate researches