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31.
Salvatore Mirabile Dr. Serena Vittorio Prof. Maria Paola Germanò Dr. Ilenia Adornato Dr. Laura Ielo Prof. Antonio Rapisarda Prof. Rosaria Gitto Francesca Pintus Dr. Antonella Fais Prof. Laura De Luca 《ChemMedChem》2021,16(19):3083-3093
There is a considerable attention for the development of inhibitors of tyrosinase (TYR) as therapeutic strategy for the treatment of hyperpigmentation disorders in humans. Continuing in our efforts to identify TYR inhibitors, we describe the design, synthesis and pharmacophore exploration of new small molecules structurally characterized by the presence of the 4-fluorobenzylpiperazine moiety as key pharmacophoric feature for the inhibition of TYR from Agaricus bisporus (AbTYR). Our investigations resulted in the discovery of the competitive inhibitor [4-(4-fluorobenzyl)piperazin-1-yl]-(3-chloro-2-nitro-phenyl)methanone 26 (IC50=0.18 μM) that proved to be ∼100-fold more active than reference compound kojic acid (IC50=17.76 μM). Notably, compound 26 exerted antimelanogenic effect on B16F10 cells in absence of cytotoxicity. Docking analysis suggested its binding mode into AbTYR and into modelled human TYR. 相似文献
32.
Antonella Ilenia Alfano Prof. Elisabetta Buommino Prof. Maria Grazia Ferraro Prof. Carlo Irace Prof. Angela Zampella Prof. Heiko Lange Prof. Margherita Brindisi 《ChemMedChem》2021,16(24):3795-3809
The generation of peptidomimetic substructures for medicinal chemistry purposes requires effective and divergent synthetic methods. We present in this work an efficient flow process that allows quick modulation of reagents for Joullié-Ugi multicomponent reaction, using spiroindolenines as core motifs. This sterically hindered imine equivalent could successfully be diversified using various isocyanides and amino acids in generally good space-time yields. A telescoped flow process combining interrupted Fischer reaction for spiroindolenine synthesis and subsequent Joullié-Ugi-type modification resulted in product formation in very good overall yield in less than 2 hours compared to 48 hours required in batch mode. The developed protocol can be seen as a general tool for rapid and facile generation of peptidomimetic compounds. We also showcase preliminary biological assessments for the prepared compounds. 相似文献
33.
Vincenza Ferraro Ruben Ferreira Jorge Isabel B. Cruz Filipa Antunes Bruno Sarmento Paula M. L. Castro Manuela E. Pintado 《International Journal of Food Science & Technology》2014,49(1):27-33
This study reports on the intestinal permeability of salt‐containing mixtures of amino acids extracted from codfish salting wastewater. Permeability was evaluated in vitro using the Caco‐2 cell line model; cell integrity during exposure to mixtures of amino acids was estimated by measuring the transepithelial electrical resistance (TEER). The effect of salt (NaCl) on the permeability and on the intestinal cell's integrity was also examined. Permeation rate (i.e. transport) was ≥95% for all amino acids except for creatine, for which it was 6%. Values for apparent permeability coefficients, Papp > 10?5 cm s?1, for mixture with isotonic concentration of NaCl suggest that amino acids are very likely to be absorbed in humans. Mixture with a hypertonic level of NaCl exerts a cytotoxic effect in intestinal cells resulting in a loss of epithelium integrity. Results show that isotonic mixture of amino acids extracted from codfish salting wastewater could be used in food, feed, cosmetic and pharmaceutical formulations. These applications could contribute to the fish industry sustainability. 相似文献
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Explicit controlled-NOT gate sequences between two qubits of different types are presented in view of applications for large-scale quantum computation. Here, the building blocks for such composite systems are qubits based on the electrostatically confined electronic spin in semiconductor quantum dots. For each system the effective Hamiltonian models expressed by only exchange interactions between pair of electrons are exploited in two different geometrical configurations. A numerical genetic algorithm that takes into account the realistic physical parameters involved is adopted. Gate operations are addressed by modulating the tunneling barriers and the energy offsets between different couple of quantum dots. Gate infidelities are calculated considering limitations due to unideal control of gate sequence pulses, hyperfine interaction and charge noise. 相似文献
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Elena Bresciani Nicola Squillace Valentina Orsini Roberta Piolini Laura Rizzi Laura Molteni Ramona Meanti Alessandro Soria Giuseppe Lapadula Alessandra Bandera Andrea Gori Paolo Bonfanti Robert John Omeljaniuk Vittorio Locatelli Antonio Torsello 《International journal of molecular sciences》2022,23(7)
Combined AntiRetroviral Treatments (cARTs) used for HIV infection may result in varied metabolic complications, which in some cases, may be related to patient genetic factors, particularly microRNAs. The use of monozygotic twins, differing only for HIV infection, presents a unique and powerful model for the controlled analysis of potential alterations of miRNAs regulation consequent to cART treatment. Profiling of 2578 mature miRNA in the subcutaneous (SC) adipose tissue and plasma of monozygotic twins was investigated by the GeneChip® miRNA 4.1 array. Real-time PCR and ddPCR experiments were performed in order to validate differentially expressed miRNAs. Target genes of deregulated miRNAs were predicted by the miRDB database (prediction score > 70) and enrichment analysis was carried out with g:Profiler. Processes in SC adipose tissue most greatly affected by miRNA up-regulation included (i) macromolecular metabolic processes, (ii) regulation of neurogenesis, and (iii) protein phosphorylation. Furthermore, KEGG analysis revealed miRNA up-regulation involvement in (i) insulin signaling pathways, (ii) neurotrophin signaling pathways, and (iii) pancreatic cancer. By contrast, miRNA up-regulation in plasma was involved in (i) melanoma, (ii) p53 signaling pathways, and (iii) focal adhesion. Our findings suggest a mechanism that may increase the predisposition of HIV+ patients to insulin resistance and cancer. 相似文献
39.
Alberto Bencini Vittorio Duchi Antonio Casatello Nikolaos Kolios Michalis Fytikas Luca Sbaragli 《Geothermics》2004,33(5):141
Sixty-five water samples and seven associated gas samples have been collected on Lesbos island. The lithology and structural setting have resulted in two main types of hydrological circulation: a shallow circulation hosting low-salinity cold waters and a deeper one, hosting high-salinity hot waters that often emerge in thermal springs near the coast. The cold waters are characterized by Ca(Mg)-HCO3(SO4) composition, while the thermal waters generally have an Na-Cl composition. The chemical features of the former can be explained by their circulation in the ophiolite-bearing phyllitic basement and volcanic rocks. Waters circulating in the ultramafic layers of the basement are richer in Mg than the waters whose circulation is mainly within marble levels or volcanic rocks. The Na-Cl thermal waters are characterized by salinities ranging from 1910 to 35,700 mg/kg. As indicated by previous hydrogeochemical and isotopic studies, the Na-Cl composition of the thermal waters on Lesbos is the result of mixing between shallow meteoric waters and marine waters. While interacting with the minerals of the geothermal reservoir, the saline waters retain the Na/Cl sea water ratio but become enriched in Ca2+ and depleted in Mg2+ with respect to sea water.Processes of hydrothermal alteration at depth are activated by a gas phase enriched in CO2, which reaches the geothermal reservoir by rising along the deep fractures of the basement. Thermodynamic calculations based on hydrothermal alteration processes occurring at the estimated temperatures of the geothermal reservoir (about 120 °C) indicate that the thermal waters of Lesbos are in equilibrium with talc and dolomite. 相似文献
40.
Biosurfactants from Urban Wastes for Detergent Formulation: Surface Activity and Washing Performance
Piero Savarino Enzo Montoneri Giorgia Musso Vittorio Boffa 《Journal of surfactants and detergents》2010,13(1):59-68
To promote biobased products for industry, six biosurfactants (BS) isolated from green and food urban residues aged under
aerobic digestion for 0–60 days were investigated for their chemical composition, surface activity properties and detergent
performance in fabric washing in comparison with commercial anionic and nonionic surfactants (CS). The BS exhibited a range
of chemical composition and surface activity properties presumably related to their different biomass sources. Surface tension
data for these substances correlated meaningfully with performance data in fabric washing. It was found that BS have similar
performances as CS when used neat, but the 1:1 w/w BS–CS mixes are characterized by significant synergy. High sensitivity
to water hardness and fabric yellowing were found to be the main deficiencies for the BS. However, both effects are minimized
or are not critically evident when the BS are used together with CS and/or in common detergents formulations. The results
indicate that when used above critical micellar concentration, no significant or critical performance differences are evident
within the whole group of BS or between BS and CS. These facts encourage expectations for industrial production and real commercialization
of BS as components of detergents formulations. 相似文献