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Chemical modifications to obtain hyaluronic acid derivatives as electrospun scaffolds in biomedical applications
No full textRecent Advances in Heterocyclic HIV Protease Inhibitors
No full textSince the first cases of AIDS, reported in 1980, this disease has become chronic over the
years, and researchers have been trying to keep it under control. Despite the development
and spread of mutate viruses, HIV protease remains an important pharmacological target.
In the development of new HIV protease inhibitors, heterocyclic fragments have proven to
be of great importance, owing to their rigid core structure, which may fit better into the
enzyme’s hydrophobic pockets, and the presence of a heteroatom, which may increase the
number of H-bonding interactions at the active site. According to the concept of targeting
the protein backbone, different aromatic or non-aromatic heterocyclic moieties have yielded
inhibitors with sufficient activity against mutant viruses. This paper provides an overview
of HIV protease inhibitors developed over the last fifteen years, with a focus on the presence
of heterocycles in their structure, either in the core or on the side chains, which are crucial
for their activity. The rationale behind the design of these new inhibitors, as well as the key
synthetic steps involved in their preparation, is also described
Rational Design and Biological Evaluation of Pyrrolidinone-Based ACE2 Inhibitors as Potential Therapeutic Agents Against SARS-CoV-2
No full textSARS-CoV-2, an RNA virus belonging to the Coronavirus (CoV) family [1,2], appears crown-shaped under the electron microscope. This characteristic morphology is due to the presence of spike (S) glycoproteins on its outer envelope, which are responsible for mediating entry into human host cells
[3]. Viral entry depends on the interaction between the S1 subunit of the spike protein and a cellular receptor that facilitates the virus’s attachment to the surface of target cells.
In particular, it has been demonstrated that SARS-CoV-2 utilizes the angiotensin-converting enzyme 2 (ACE2) as its entry receptor and the transmembrane serine protease 2 (TMPRSS2) for spike protein activation [4]. Our study concerns the rational design and synthesis of novel pyrrolidinone derivatives (Figure 1) targeting the ACE2 receptor, a critical entry point for SARS-CoV-2. Guided by structural insights from known inhibitors such as MLN-4760 [5], several compounds featuring a pyrrolidinone scaffold were synthesized and characterized.
Their inhibitory activity toward ACE2 was assessed in vitro and supported by molecular docking simulations [6]. Docking results (Figure 2) highlighted favorable binding interactions within the ACE2 active site, identifying N-(3-(2-oxopyrrolidin-1-yl)propyl)-1H-indole-2-carboxamide as the most promising candidate. These outcomes provide a solid foundation for future in vivo studies aimed at developing new therapeutic strategies for COVID-19 and other ACE2-associated disorders
Search for t-channel scalar and vector leptoquark exchange in the high-mass dimuon and dielectron spectra in proton-proton collisions at sqrt{s} = 13 TeV
No full textA search for t-channel exchange of leptoquarks (LQs) is performed in dimuon and dielectron spectra using proton-proton collision data collected at TeV with the CMS detector at the CERN LHC. The data correspond to an integrated luminosity of 138 fb−1. Eight scenarios are considered, in which up or down quarks couple to muons or electrons via a scalar or vector LQ exchange, for dilepton invariant masses above 500 GeV. The LQ masses are probed up to 5 TeV, beyond a regime probed by previous pair-production and single-production searches. The differential distributions of dilepton events are fit to templates that model the nonresonant LQ exchange and various standard model background processes. Limits are set on LQ-fermion coupling strengths for scalar and vector LQ masses in the 1–5 TeV range at 95% confidence level, establishing stringent limits on first- and second-generation LQs
Antiproliferative Evaluation of Dextran Polymer-Based Pomegranate Ethanolic Extract
No full textThe pomegranate peel represents an important source of secondary metabolites such as hydrolysable ellagitannins, which are recognized for their antioxidant, anticancer and neuroprotective properties. In this work, the freeze-dried pomegranate peel was extracted by a combined mild maceration at room temperature and ultrasonication at 45 °C using ethanol and acetone as green solvents. The ethanol extract, with an extraction yield of 29%, and IC50 (mg/mL) 0.1067 and 0.0414 for DPPH and ABTS, respectively, was incorporated into a polymer based on dextran, using a grafting reaction, to improve its bioavailability and preserve the chemical integrity. In addition, the potential antitumor activity against breast cancer was evaluated based on the existing literature. In vitro studies have demonstrated the safety and biocompatibility of both free pomegranate peel extract (SSE2-L) and its dextran conjugate (SSPD), with no adverse effects on fibroblasts, erythrocytes, or immune cells. Both formulations inhibited the proliferation of breast cancer cell lines (MCF-7, MDA-MB-231) in a concentration- and time-dependent manner, with SSPD consistently showing superior efficacy. This enhanced activity was corroborated by reduced clonogenic growth, G1 cell-cycle arrest, and improved stability and bioactive retention conferred by polymer conjugation. Overall, these findings highlight dextran-conjugated pomegranate polyphenols as promising candidates for next-generation nutraceuticals and phytopharmaceuticals in cancer chemoprevention and adjunctive therapy, with potential applications extending to other biomedical fields and functional foods
Osmosis, hybridisation, symbiosis – From biophilia to interspecies regenerative design
No full textThis paper offers a reflection on a broader field of investigation developed through the activities of the NatureCity LAB at the University of Basilicata. The aim of exploring three operative categories is to focus on three processes through which the relationship between Architecture and Nature can generate spatial conditions for welcoming new alliances between humans and non-humans. Osmosis, hybridisation, and symbiosis are thus the key processes through which the regenerative potential of architecture, the city, and the landscape are investigated to ensure the well-being of the individuals who inhabit them. The research draws on a hypothesis, biophilia, a point of observation, the City of Matera, and case studies to trace a research trajectory around the Nature-City paradigm to outline a design perspective: interspecies regenerative architecture
Swift-BAT GUANO Follow-up of Gravitational-wave Triggers in the Third LIGO–Virgo–KAGRA Observing Run
No full textContribution of Bio-Based Buildings Made with Seaweed and Seagrass in the Construction Industry.
No full textDue to the construction industry, the climate crisis had deepest environmental impact. In addition to consuming scarce mineral-based materials, the building industry is responsible for up to 39% of global carbon dioxide
emissions and the accumulation of solid waste in landfills, rivers, and seas. To cut carbon dioxide emissions
and mitigate the effects of climate change on the construction industry, a new, more sustainable, and
renewable production matrix must be considered. An approach is using seaweed and seagrass as bio-based
materials matrix, from macroalgae or microalgae stranded on the shore or sustainable crops. Transforming algae into usable construction materials involves a process of harvesting, processing, and refining. This article has systematically reviewed the literature about advances and the potential of using marine species as construction materials matrix. To this end, this paper explores the existing literature on architectural
projects and research on various species of seagrass and seaweed worldwide.
This review concludes that numerous case studies of dwellings around the world have demonstrated
and validated the use of seaweed for applications such as coatings, thermal insulation, and construction
additives. Among the most important construction related properties of seaweed are fire resistance, low thermal conductivity, and resistance to moisture and insect damage. For instance, prototypes incorporating Neptune grass (Posidonia oceanica) exhibited a thermal conductivity of 0.044 W/m·K comparable to that of expanded polystyrene, which typically ranges between 0.035 and 0.037 W/m·K
Feature Extraction of Point Clouds for Cultural Heritage Monitoring and Conservation
No full textIn the digital era, with the emergence of advanced reality-capture technologies, there is a growing recognition of the importance of documentation and monitoring of architectural heritage (AH) in conservation efforts. Techniques such as terrestrial laser scanning (TLS), mobile LiDAR, and photogrammetry generate high-resolution point clouds (PCs), providing detailed geometric and radiometric data for heritage structures. However, the complexity and unstructured nature of PCs can pose challenges related to data processing, segmentation, and storage. One possible step in the right direction could be the identification of relevant geometric attributes, through a process of feature extraction, with the aim of optimising segmentation and classification processes. Segmentation, i.e. the subdivision of PCs into coherent subsets, could allow the efficient analysis, interpretation and visualisation of architectural elements. This process could in turn enhance the application of Heritage-Building Information Modeling (HBIM), degradation mapping and structural assessments, facilitating non-invasive monitoring and long-term conservation strategies. Although the scientific community emphasises the use of artificial intelligence solutions and algorithms to automate processes, this contribution proposes instead the development of structured workflows for processing PCs, analysing the potential of geometric features in order to enrich 3D models with semantic information. The study is part of the Tech4You project within the National Recovery and Resilience Plan (PNRR)
An Interdisciplinary Study of the Pietra Maura Earthflow in the Marsico Nuovo Territory (Southern Italy)
No full textAbstract Landslides are a significant geomorphological factor in the natural evolution of the Southern Apennines slopes (South Italy), with earthflows being one of the most representative types. The development of large earthflows in this region is primarily due to extensive clay-rich outcrops, whose activation was facilitated by warm, humid Holocene climates. These earthflows can be very extensive, often affecting entire slopes and exhibiting numerous minor reactivations over time. This study focuses on the Pietra Maura earthflow in the Marsico Nuovo Municipality (Basilicata Region), integrating detailed geological and geomorphological investigations with geophysical techniques to characterise and better understand its evolution. The landslide extends approximately 4.2 km NW-SE, with an average width of 900 m, and affects the area below the maximum level of the Marsico Nuovo dam and two urban zones, crossing roads, power lines, and aqueducts, necessitating ongoing monitoring to prevent damage. To better understand the extent and dynamics of the Pietra Maura earthflow, a detailed geological and geomorphological survey was conducted, supported by advanced geophysical techniques, such as Interferometric Synthetic Aperture Radar (InSAR) and Electrical Resistivity Tomography (ERT). InSAR data from Copernicus Sentinel-1 satellites revealed detailed east-west ground deformation patterns, while ERT helped reconstruct the earthflow’s geometry, showing a variable thickness of up to 50–60 m and identifying sectors with high-water content. The findings provide essential insights for taking appropriate actions to stabilise the landslide and improve area management