Therapeutic Potential of Highly Selective A3 Adenosine Receptor Ligands in the Central and Peripheral Nervous System

Ligands of the G_i protein-coupled adenosine A₃ receptor (A₃R) are receiving increasing interest as attractive therapeutic tools for the treatment of a number of pathological conditions of the central and peripheral nervous systems (CNS and PNS, respectively). Their safe pharmacological profiles emerging from clinical trials on different pathologies (e.g., rheumatoid arthritis, psoriasis and fatty liver diseases) confer a realistic translational potential to these compounds, thus encouraging the investigation of highly selective agonists and antagonists of A₃R. The present review summarizes information on the effect of latest-generation A₃R ligands, not yet available in commerce, obtained by using different in vitro and in vivo models of various PNS- or CNS-related disorders. This review places particular focus on brain ischemia insults and colitis, where the prototypical A₃R agonist, Cl-IB-MECA, and antagonist, MRS1523, have been used in research studies as reference compounds to explore the effects of latest-generation ligands on this receptor. The advantages and weaknesses of these compounds in terms of therapeutic potential are discussed.     

Neutron-rich isotope production using the uranium carbide multi-foil SPES target prototype

In the framework of the R&D program for the SPES (Selective Production of Exotic Species) project of the Istituto Nazionale di Fisica Nucleare (INFN), production yields of neutron-rich isotopes have been measured at the Holifield Radioactive Ion Beam Facility (HRIBF, Oak Ridge National Laboratory, USA). This experiment makes use of the multi-foil SPES target prototype composed of 7 uranium carbide discs, with excess of graphite (ratio C/U = 4 . 77 isotopes of medium mass (between 72 and 141amu), produced via proton-induced fission of uranium using a 40MeV proton beam, have been collected and analyzed for the target heated at 2000 ^° C target temperature.     

Bisursodeoxycholate(ethylenediamine)platinum(II): a new autofluorescent compound. Cytotoxic activity and cell cycle analysis in ovarian and hematological cell lines

The present paper describes for the first time an intrinsic fluorescent square-planar platinum(II) complex carrying two ursodeoxycholate ligands ([Pt(UDC)2(en)], where UDC(-) = ursodeoxycholate), that emits at room temperature once free in solution. Kinetic studies were carried out in aqueous solution and in the presence of different NaCl concentrations: 4 mM (similar to cytoplasmic concentration) and 150 mM (similar to plasmatic concentration). This novel compound was synthesized from a [PtCl2(en)] complex and shows increased cytotoxic activity against both resting and cycling HeLa cells, with no toxicity for cell lines derived from neoplastic haematopoietic cells.     

The ISOLPHARM project: ISOL-based production of radionuclides for medical applications

Radionuclides for radiopharmaceuticals can be produced in cyclotrons or nuclear reactors. Each of these production modes has serious issues, such as high target costs, production of long-lived wastes and contaminants, expensive separation. For this reason, new methods are under consideration for the production of highly pure radionuclides. The ISOL (Isotope Separation On-Line) method is the major technique for the production of radioactive ion beams for nuclear physics applications. The SPES-ISOLPHARM project at INFN-LNL (Istituto Nazionale di Fisica Nucleare-Laboratori Nazionali di Legnaro) is a feasibility study for the production of medical isotopes exploiting the ISOL method. The ongoing activities concerning a recent experiment focused on ¹¹¹Ag, a study performed in collaboration with Padova and Trento Universities, is presented.

     

Temperature dependence of yields from multi-foil SPES target

The temperature dependence of neutron-rich isotope yields was studied within the framework of the HRIBF-SPES Radioactive Ion Beams (RIB) project. On-line release measurements of fission fragments from a uranium carbide target at $\ensuremath 1600 {}^{\circ}\mathrm{C}$\ensuremath 1600 {}^{\circ}\mathrm{C} , 1800 ^°C\ensuremath 1800 {}^{\circ}\mathrm{C} and 2000 ^°C\ensuremath 2000 {}^{\circ}\mathrm{C} were performed at ORNL (USA). The fission reactions were induced by a 40MeV proton beam accelerated into a uranium carbide target coupled to a plasma ion source. The experiments allowed for tests of performance of the SPES multi-foil target prototype loaded with seven UC₂/graphite discs (ratio C/U = 4 with density about 4g/cm³.     

Reliability assessment of a gas chromatographic method for polycyclic aromatic hydrocarbons in olive oil.

A quality control test was developed for a gas chromatographic method to determine polycyclic aromatic hydrocarbons in olive oil. Fifteen oil specimens were fortified with eight three- to six-ring polycyclic aromatic hydrocarbons at levels of between 3.0 (approximate detection limit) and 360 micrograms/kg. Three sets of five equally fortified specimens were obtained and assayed at random by three operators. For each fortification level, the means of recovery yield were in the range 56-107%, and were independent of the polycyclic aromatic hydrocarbon congener specificity and the operator's capability. Excluding subsets of data associated with both the fortification level at the detection limit and a deviant polycyclic aromatic hydrocarbon term (benzo[ghi]perylene), an overall mean accuracy of 96% and a precision of 7% were achieved.