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排序方式: 共有4082条查询结果,搜索用时 31 毫秒
811.
Giuseppe Toscani 《Entropy (Basel, Switzerland)》2022,24(10)
Inequality indices are quantitative scores that take values in the unit interval, with a zero score denoting complete equality. They were originally created to measure the heterogeneity of wealth metrics. In this study, we focus on a new inequality index based on the Fourier transform that demonstrates a number of intriguing characteristics and shows great potential for applications. By extension, it is demonstrated that other inequality measures, such as the Gini and Pietra indices, can be usefully stated in terms of the Fourier transform, allowing us to illuminate characteristics in a novel and straightforward manner. 相似文献
812.
Rosa Sparaco Ewa Kdzierska Agnieszka A. Kaczor Anna Bielenica Elisa Magli Beatrice Severino Angela Corvino Ewa Gibua-Tarowska Jolanta H. Kotliska Giorgia Andreozzi Paolo Luciano Elisa Perissutti Francesco Frecentese Marcello Casertano Anna Leniak Magdalena Bujalska-Zadrony Magorzata Ozibo Raffaele Capasso Vincenzo Santagada Giuseppe Caliendo Ferdinando Fiorino 《Molecules (Basel, Switzerland)》2022,27(19)
A new series of 5-norbornene-2-carboxamide derivatives was prepared and their affinities to the 5-HT1A, 5-HT2A, and 5-HT2C receptors were evaluated and compared to a previously synthesized series of derivatives characterized by exo-N-hydroxy-5-norbornene-2,3-dicarboximidenucleus, in order to identify selective ligands for the above-mentioned subtype receptors. Arylpiperazines represents one of the most important classes of 5-HT1AR ligands, and recent research concerning new derivatives has been focused on the modification of one or more portions of such pharmacophore. The combination of structural elements (heterocyclic nucleus, propyl chain and 4-substituted piperazine), known to be critical to the affinity to 5-HT1A receptors, and the proper selection of substituents led to compounds with high specificity and affinity towards serotoninergic receptors. The most active compounds were selected for further in vivo assays to determine their functional activity. Finally, to rationalize the obtained results, molecular docking studies were performed. The results of the pharmacological studies showed that Norbo-4 and Norbo-18 were the most active and promising derivatives for the serotonin receptor considered in this study. 相似文献
813.
Giusy Rita Caponio Miriam Cofano Tamara Lippolis Isabella Gigante Valentina De Nunzio Graziana Difonzo Mirella Noviello Luigi Tarricone Giuseppe Gambacorta Gianluigi Giannelli Maria De Angelis Maria Notarnicola 《Molecules (Basel, Switzerland)》2022,27(20)
Grape pomace (GP)—the major by-product of winemaking processes—still contains bioactive molecules with known beneficial properties for human health, such as an antiradical scavenging activity or an antiproliferative activity of tumors. In vitro studies have demonstrated that GP polyphenols specifically influence colon cancer cell proliferation. In addition to previously published work, we tested the phenolic compounds of Aglianico GP following an in vitro simulated gastrointestinal digestion on colorectal cancer cell lines at different degrees of differentiation. Our experiments, using HT29 and SW480 cells, confirmed the anti-proliferative effect of GP gastrointestinal digested extract and provided intriguing insights on the way it influences the cancer cell features (i.e., viability, proliferation, and apoptosis). We observed that Aglianico GP extract showed a great ability to affect cell proliferation and apoptosis. Interestingly, both HT29 and SW480 cells produced a significant increase in Bax, and a significant increase in the Bax/Bcl-2 ratio and caspase-3. The gastrointestinal digested GP extract was previously characterized both for antioxidant activity and phenolic composition. As a result, the TPC and the antioxidant activity reached high values in the Aglianico GP digested extract, and the main compounds assessed by UHPLC-DAD were anthocyanins, phenolic acids, and flavonoids. This work shed light on the use of digested GP extract as a dietary ingredient, a very sustainable source of nutritional compounds with potential health benefits for colon cancer cell proliferation. 相似文献
814.
Norberto Masciocchi Vincenzo Mirco Abbinante Marco Zambra Giuseppe Barreca Massimo Zampieri 《Molecules (Basel, Switzerland)》2022,27(21)
Tafamidis, chemical formula C14H7Cl2NO3, is a drug used to delay disease progression in adults suffering from transthyretin amyloidosis, and is marketed worldwide under different tradenames as a free acid or in the form of its meglumine salt. The free acid (CAS no. 594839-88-0) is reported to crystallize as distinct (polymorphic) crystal forms, the thermal stability and structural features of which remained thus far undisclosed. In this paper, we present—by selectively isolating highly pure batches of Tafamidis Form 1 and Tafamidis Form 4—the full characterization of these solids, in terms of crystal structures (determined using state-of-the-art structural powder diffraction methods) and spectroscopic and thermal properties. Beyond conventional thermogravimetric and calorimetric analyses, variable-temperature X-ray diffraction was employed to measure the highly anisotropic response of these (poly)crystalline materials to thermal stimuli and enabled the determination of the linear and volumetric thermal expansion coefficients and of the related indicatrix. Both crystal phases are monoclinic and contain substantially flat and π-π stacked Tafamidis molecules, arranged as centrosymmetric dimers by strong O-H···O bonds; weaker C-H···N contacts give rise, in both polymorphs, to infinite ribbons, which guarantee the substantial stiffness of the crystals in the direction of their elongation. Complete knowledge of the structural models will foster the usage of full-pattern quantitative phase analyses of Tafamidis in drug and polymorphic mixtures, an important aspect in both the forensic and the industrial sectors. 相似文献
815.
Giuseppe Antonio Malfa Marinella De Leo Rosa Tundis Alessandra Braca Monica Rosa Loizzo Claudia Di Giacomo Francesco Maria Raimondo Anahi Elena Ada Bucchini Rosaria Acquaviva 《Molecules (Basel, Switzerland)》2022,27(23)
Brassica villosa subsp. drepanensis (Caruel) Raimondo & Mazzola, belonging to the Brassica oleracea complex, is a wild edible plant endemic to western Sicily and a relative of modern cultivated Brassica crops. In this study, the antioxidant properties, anti-inflammatory activities, enzymatic inhibition, and cytotoxicity in cancer cells of B. villosa subsp. drepanensis leaf ethanolic extract were analysed for the first time. In addition, its chemical profile was investigated partitioning the total 70% ethanol extract among ethyl acetate, n-butanol, and water to obtain three residues that were subjected to chromatographic separation. Two flavonol glycosides, a phenol glucoside, two amino acids, and purine/pyrimidine bases were obtained. The presence of the glucosinolate glucoiberin was detected in the water extract by UHPLC-MS analysis. The total polyphenol and flavonoid content of the 70% ethanol extract showed good antioxidant capacities and anti-inflammatory properties by reducing nitric oxide release and reactive oxygen species levels and increasing glutathione in lipopolysaccharide-stimulated RAW 264.7 cells. The extract inhibited the enzymatic activity of α-amylase, α-glucosidase, and, significantly, of lipase. The MTT assay showed that the extract did not affect the viability of normal HFF-1 and RAW 264.7 cells. Among the cancer cell lines tested, an antiproliferative action was only observed in CaCo-2. The cytotoxicity of the extract was further confirmed by LDH release assay and by the destabilization of the oxidative balance. Results confirmed the antioxidant properties of the crude extract responsible for the anti-inflammatory effect on healthy cells and cytotoxicity in cancer cells. 相似文献
816.
Eleonora Colombo Davide Andrea Coppini Laura Polito Umberto Ciriello Giuseppe Paladino Mariafrancesca Hyeraci Maria Luisa Di Paolo Giulia Nordio Lisa Dalla Via Daniele Passarella 《Molecules (Basel, Switzerland)》2023,28(1)
Cannabidiol (CBD) is a biologically active compound present in the plants of the Cannabis family, used as anticonvulsant, anti-inflammatory, anti-anxiety, and more recently, anticancer drug. In this work, its use as a new self-assembly inducer in the formation of nanoparticles is validated. The target conjugates are characterized by the presence of different anticancer drugs (namely N-desacetyl thiocolchicine, podophyllotoxin, and paclitaxel) connected to CBD through a linker able to improve drug release. These nanoparticles are formed via solvent displacement method, resulting in monodisperse and stable structures having hydrodynamic diameters ranging from 160 to 400 nm. Their biological activity is evaluated on three human tumor cell lines (MSTO-211H, HT-29, and HepG2), obtaining GI50 values in the low micromolar range. Further biological assays were carried out on MSTO-211H cells for the most effective NP 8B, confirming the involvement of paclitaxel in cytotoxicity and cell death mechanism 相似文献
817.
Dr. Andrea Chiminazzo Dr. Giuseppe Borsato Alessia Favero Dr. Chiara Fabbro Prof. Dr. Charles E. McKenna Prof. Luca Giuseppe Dalle Carbonare Prof. Dr. Maria Teresa Valenti Prof. Dr. Fabrizio Fabris Prof. Dr. Alessandro Scarso 《Chemistry (Weinheim an der Bergstrasse, Germany)》2019,25(14):3617-3626
The synthesis of a conjugate molecule between an unusual red-fluorescent diketopyrrolopyrrole (DPP) unit and a bis-phosphonate (BP) precursor by a click-chemistry strategy to target bone tissue and monitor the interaction is reported. After thorough investigation, conjugation through a triazole unit between a γ-azido rather than a β-azido BP and an alkyne-functionalized DPP fluorophore group turned out to be the winning strategy. Visualization of the DPP-BP conjugate on osteoclasts and specific antiresorption activity were successfully demonstrated. 相似文献
818.
Dr. Antonio Magrì Dr. Giovanni Tabbì Dr. Giuseppe Di Natale Prof. Diego La Mendola Dr. Adriana Pietropaolo Prof. Maria Antonietta Zoroddu Dr. Massimiliano Peana Prof. Enrico Rizzarelli 《Chemistry (Weinheim an der Bergstrasse, Germany)》2020,26(57):13072-13084
Islet amyloid polypeptide (IAPP) is a hormone co-secreted with insulin and zinc from pancreatic β-cells. To overcome the low solubility of human IAPP, we characterized zinc complexes species formed with 1) a mutated form of rat-IAPP(1–37; R18 H) able to mimic the human IAPP, 2) the r-IAPP(1–37) and the IAPP(1–8) fragment. Stoichiometry, speciation and coordination features of zinc(II) complexes were unveiled by ESI-MS, potentiometry and NMR measurements combined with DFT and free-energy simulations. Mononuclear species start to form around pH 6; Zn2+ binds both His18 and N-amino terminus in rat-IAPP(1–37; R18 H). The in silico study allows us to assess not only a structured turn compact domain in r-IAPP(1–37) and r-IAPP(1–37; R18 H) featured by a different free energy barrier for the transition from the compact to elongated conformation upon the coordination of Zn2+, but also to bring into light a coordination shell further stabilized by noncovalent interactions. 相似文献
819.
Carlo Dal Lin Laura Acquasaliente Sabino Iliceto Vincenzo De Filippis Giuseppe Vitiello Francesco Tona 《Entropy (Basel, Switzerland)》2021,23(4)
Background and aim: Mental stress represents a pivotal factor in cardiovascular diseases. The mechanism by which stress produces its deleterious ischemic effects is still under study but some of the most explored pathways are inflammation, endothelial function and balancing of the thrombotic state. In this scenario, von Willebrand factor (vWF) is a plasma glycoprotein best known for its crucial hemostatic role, also acting as key regulatory element of inflammation, being released by the activated vascular endothelium. Antistress techniques seem to be able to slow down inflammation. As we have recently verified how the practice of the Relaxation Response (RR), which counteracts psychological stress, causes favorable changes in some inflammatory genes’ expressions, neurotransmitters, hormones, cytokines and inflammatory circulating microRNAs with coronary endothelial function improvement, we aimed to verify a possible change even in serum levels of vWF. Experimental procedure: We measured vWF multimers and the total protein carbonyl contents in the sera of 90 patients with ischemic heart disease (and 30 healthy controls) immediately before and after an RR session, three times (baseline, 6 months, 12 months), during a one-year follow-up study. Results: According to our data, large vWF multimers decrease during the RR, as does the plasma total carbonyl content. Conclusion: vWF levels seem to vary rapidly between anti-inflammatory and antithrombotic behaviors dependent on psychological activity, leading to relaxation and also possibly changes in its quaternary structure. 相似文献
820.