200 research outputs found
Synthesis and supramolecular assembly of 1,3-bis(1′-uracilyl)-2- propanone
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RSC Advances
Volume 4, Issue 54, 2014, Pages 28691-28698
Synthesis and supramolecular assembly of 1,3-bis(1′-uracilyl)-2- propanone (Article)
Roviello, G.N.a , Roviello, G.b, Musumeci, D.c, Capasso, D.d, Di Gaetano, S.a, Costanzo, M.d, Pedone, C.d
a Istituto di Biostrutture e Bioimmagini-CNR, Via Mezzocannone 16, 80134 Napoli, Italy
b Department of Science and Technology, University of Naples Parthenope, Centro Direzionale, 80143 Napoli, Italy
c Department of Chemical Science, University of Naples Federico II, Via Cinthia, 80126 Napoli, Italy
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Abstract
In this research work, we investigated the properties of a novel heterocyclic molecule, named by us U2CO, whose structure consists of two uracil rings connected by a 2-propanone moiety. We studied by UV the spectroscopic characteristics of U2CO as a function of temperature and ionic strength of the solution. Furthermore, dynamic light scattering (DLS) studies conducted on samples containing the uracil-containing derivative indicated the formation of non-covalent supramolecular networks based on multiple U2CO units. These aggregates contained hydrophobic cavities able to encapsulate drugs such as doxorubicin, as evidenced by fluorescence studies. This property, together with the good stability in human serum of U2CO, determined by HPLC analysis, could be an interesting feature in developing new drug delivery systems. Interestingly, UV studies suggested that U2CO is able to form complexes with copper(ii) cations, which is a useful characteristic in view of potential anti-oxidant approaches
Editorial: Special Issue “Galectins: Structure, Function and Therapeutic Inhibitors”
No full textGalectins, β-galactoside-binding proteins, play relevant roles in different biological processes; therefore, they are becoming emerging targets for diagnostic and therapeutic approaches [...
Adaptation of Zemplén's conditions for a simple and highly selective approach to methyl 1,2−trans glycosides
No full text1,2-trans methyl glycosides can be readily obtained from peracetylated sugars through their initial conversion into glycosyl iodide donors and subsequent exposure of these latter to a slight excess of sodium methoxide in methanol. Under these conditions a varied set of mono- and disaccharide precursors afforded the corresponding 1,2-trans glycosides with concomitant de-O-acetylation in satisfying yields (in the range 59–81%). A similar approach also proved effective when using GlcNAc glycosyl chloride as the donor
Domenica Bruni, Storia naturale dell'amore, Carocci, Roma 2010, pp. 144
No full textThe text offers a Critical Review of "Storia naturale dell'amore" by Domenica Bruni. The author critically reflects on the book by considering its methodologies, its arguments, and its relation with other books of the same type and on the same subject.Il testo propone una Lettura Critica del libro "Storia naturale dell'amore" di Domenica Bruni. L'autrice riflette criticamente sul libro considerandone le metodologie, gli argomenti e il nesso con altri libri dello stesso tipo e sullo stesso argomento
Alternate dab-aegPNAs: synthesis, nucleic acid binding studies and biological activity
No full textAs part of our research on new oligonucleotide analogs for therapeutic and diagnostic use, here we explored the ability of an alternate dab-aegPNA oligomer to bind complementary natural nucleic acids. The alternate homothymine dab-aegPNA, synthesized following a chirally safe procedure and fully characterized by ESIMS and CD, was capable of forming hybrids with complementary DNA and RNA with enhanced thermal stability in comparison to natural oligomers, as shown by CD and UV spectroscopies. The stoichiometry of the complexes formed was determined by CD titration experiments that suggested triple helices formation. With respect to an analogous t(12) strand composed entirely of aegPNA, the chiral alternate t(12) oligomer presented an enhanced solubility in aqueous medium and did not form aggregates. Human serum stability assays performed on the new alternate oligomer evidenced a noteworthy enzymatic resistance. Moreover, the efficiency of dab-aegPNA in interfering with the reverse transcription of eukaryotic mRNA, and the absence of cytotoxic effects of the new analog were demonstrated, encouraging us to further study this chiral PNA analog in view of its possible in vivo/in vitro biotechnological applications
BENZODIFURAN DERIVATIVES AS POTENTIAL ANTIPROLIFERATIVE AGENTS: POSSIBLE CORRELATION BETWEEN THE BIOACTIVITY AND THEIR AGGREGATION PROPERTIES
No full textNotwithstanding the wide variety of applications of benzodifuran derivatives, especially in the field of innovative organic materials with particular properties, the biological activity of this class of compounds has been scarcely investigated. Aiming at further exploring the properties and bioactivity of benzodifurans, we here synthesized three compounds belonging to this class, and characterized them using spectroscopic and spectrometric techniques, also using SEM and thermogravimetric analysis. The obtained compounds showed interesting antiproliferative activity on different human cancer cells, while no relevant cytotoxic effect was observed on healthy cells used as control. In order to explore the possible mechanism of action of the benzodifuran molecules, we investigated their ability to bind DNA ‒ studying their interaction with various DNA model systems ‒ and evaluated their aggregation properties and ability to bind biologically relevant metal ions
gH625 is a viral derived peptide for effective delivery of intrinsically disordered proteins
No full textGiovanni Smaldone,1,2 Annarita Falanga,3 Domenica Capasso,4 Daniela Guarnieri,5,6 Stefania Correale,1,7 Massimiliano Galdiero,8 Paolo A Netti,4 Massimo Zollo,9 Stefania Galdiero,1,2 Sonia Di Gaetano,1 Emilia Pedone1 1Institute of Biostructures and Bioimaging, National Research Council, Naples, Italy; 2Department of Pharmacy and Interuniversity Research Center on Bioactive Peptides, Federico II University of Naples, Naples, Italy; 3Molecular Diagnostics and Pharmaceuticals Scarl, Naples, Italy; 4Special Center for Biotechnology, Federico II University of Naples, Naples, Italy; 5Center for Advanced Biomaterials for Health Care, Interdisciplinary Research Centre on Biomaterials, Italian Institute of Technology, Naples, Italy; 6Interdisciplinary Research Centre on Biomaterials, Federico II University of Naples, Naples, Italy; 7Kedrion S.p.A, Sant'antimo, Naples, Italy; 8Department of Experimental Medicine, Federico II University of Naples, Naples, Italy; 9CEINGE – Advanced Biotechnology Scarl, Naples, Italy Abstract: A genetically modified recombinant gH625-c-prune was prepared through conjugation of c-prune with gH625, a peptide encompassing 625–644 residues of the glycoprotein H of herpes simplex virus 1, which has been proved to possess the ability to carry cargo molecules across cell membranes. C-prune is the C-terminal domain of h-prune, overexpressed in breast, colorectal, and gastric cancers, interacting with multiple partners, and representing an ideal target for inhibition of cancer development. Its C-terminal domain results in an intrinsically disordered domain (IDD), and the peculiar properties of gH625 render it an optimal candidate to act as a carrier for this net negatively charged molecule by comparison with the positively charged TAT. A characterization of the recombinant gH625-c-prune fusion protein was conducted by biochemical, cellular biology and confocal microscopy means in comparison with TAT-c-prune. The results showed that the gH625-c-prune exhibited the ability to cross biomembranes, opening a new scenario on the use of gH625 as a novel multifunctional carrier. Keywords: delivery, ID
A straightforward synthetic access to symmetrical glycosyl disulfides and biological evaluation thereof.
No full textNew therapeutic targets for endometrial cancer: a glimpse into the preclinical sphere
No full textIntroductionEndometrial cancer (EC) is the only gynecologic malignancy showing increasing trends in incidence and mortality. While standard treatment has been effective primarily for early-stage EC, precision medicine with tailored therapy has revolutionized the management of this disease. Genome sequencing analyses have identified four sub-types of EC. Treatments for primary and metastatic disease can now be tailored more accurately to achieve better oncologic results.Areas coveredThis review provides an overview of the most relevant and updated evidence in the literature regarding EC molecular analysis and its role in risk classification, prognostication, and guidance for tailored and target therapies in early and advanced/metastatic stages. In addition, it provides updated information on optimal surgical management based on molecular classification and highlights key advances and future strategies.Expert opinionEC molecular analysis yields the potential of tailoring adjuvant treatment by escalating or deescalating therapy, as shown for POLE-mutated and p53-mutated tumors. Moreover, the expression of specific molecular signatures offers the possibility to employ novel target therapies, such as immune-checkpoint inhibitors that have demonstrated a significant benefit on prognosis. New treatment guidelines are still being established, and ongoing studies are exploring the potential prognostic role of further sub-stratifications of the four molecular classes and treatment options.Endometrial cancer (EC) is the only female cancer that is increasing among women. While the usual treatments work best when the disease is caught early, new advances in genetic studies have greatly improved the management of the disease. Four sub-types of EC have been identified. They are called: POLE-mutated, MMR-deficient, p53-abnormal, and no specific molecular profile. Treatments for EC can now be tailored more accurately to achieve better results. This review gives an overview of the most new and important evidence in the scientific literature about the molecular analysis of EC and how it can be used to help tailor the best treatments and surgeries for women with EC
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