Sustainable Access to Acridin-9-(10H)ones with an Embedded m-Terphenyl Moiety Based on a Three-Component Reaction

A Ce(IV)-catalyzed three-component reaction between chalcones, anilines and β-ketoesters followed by a microwave-assisted thermal cyclization afforded 1,3-diaryl-1,2-dihydroacridin-9(10H)-ones. Their microwave irradiation in nitrobenzene, acting both as solvent and oxidant, afforded fully unsaturated 1,3-diarylacridin-9(10H)-ones, which combine acridin-9-(10H)one and m-terphenyl moieties. Overall, the route generates three C-C and one C-N bond and has the advantage of requiring a single chromatographic separation.     

Fano varieties in index one Fano complete intersections

Let be a smooth complex complete intersection such that . Let f : S → X be a generically finite morphism from a smooth projective variety to X. Under some positivity assumption on the anticanonical divisor of S, if 2 ≤ dim S ≤ dim X − 2 we prove that the deformations of f are contained in a subvariety of codimension at least 2.     

Syzygies of Multi-Variable Higher Spin Dirac Operators on $$\mathbb{R}^{3}$$

This paper is a short report on the generalization of some results of our previous paper [12] to the case of spin j/2 Dirac operators in real dimension three for arbitrary odd integer j. We use an explicit formula for the local expression of such operators to study their algebraic properties, construct the compatibility conditions of the overdetermined system associated to the operator in several spatial variables, and we prove that its associated algebraic complex, dual do the BGG sequence coming from representation theory, has substantially the same pattern as the Cauchy-Fueter complex. The author is a member of the Eduard Čech Center and his research is supported by the relative grants.     

An investigation on the nature of the peptide at m/z 904, overexpressed in plasma of patients with colorectal cancer and familial adenomatous polyposis

In an investigation devoted to the search for plasma markers for colorectal cancer (CRC), carried out by matrix-assisted laser desorption/ionization (MALDI) mass spectrometry, a series of overexpressed peptides were identified in the plasma of patients. Among them the peptide with molecular weight 903 Da was the most abundant one, with a mean +/- (SD) relative abundance of 37 +/- 17% and a frequency over 60%. Interestingly, also in plasma samples of ten subjects affected by familial adenomatous polyposis (FAP), the peptide with molecular weight 903 was overexpressed. In this investigation, MALDI/MS/MS experiments were carried out on the ion at m/z 904 detected in the MALDI mass spectra of CRC and FAP patients. The data analysis by SwissProt.2007.01.09 indicates that this peptide is due to the sequence RPPGFSPF, found in the kininogen-1 precursor, which is an alpha-2-thiol proteinase inhibitor. In the case of subjects affected by a particular FAP syndrome, the MALDI/MS/MS spectra were quite different from those obtained from CRC and FAP patients. In fact, two sequences have been evidenced: RPPGFSPF belonging to kininogen-1 precursor, and PRKSSSSR belonging to Forkhead box protein 01A.     

A chemometric approach to the investigation of major and minor ion chemistry in Lake Como (Lombardia, Northern Italy

A chemometric approach based on Principal Component Analysis (PCA) has been proposed, in order to study chemical features (major and minor ions, total alkalinity, dissolved silica) of surface and deep waters of Lake Como (Northern Italy). The method allowed us to investigate the correlations between the analyzed ions in an easy-to-see way, using bi-dimensional graphs. In wintertime, the ionic composition of Lake Como waters seems to be mainly related to the geological composition of the lake basin, with a crystalline bedrock on the northern side and a sedimentary cover in the southern part. The presence of contaminants such as bromide and nitrite in water columns is also evidenced and discussed.     

Local Unit Roots and Global Stationarity of TARMA Models

In this paper the (strict and weak) stationarity of threshold autoregressive moving average models is discussed. After examining the strict stationarity, mainly based on the random coefficient autoregressive representation of the model, we provide sufficient conditions for its weak stationarity that allow to obtain a wider stationarity region with respect to some previous results given in the literature. These conditions are discussed to distinguish between global and local stationarity, whose relation has been considered in detail. The threshold process has been further evaluated to face the problem related to the so called existence of a threshold structure in the data generating process that is strictly related to the stationarity and has significant relevance when the parameters of the model have to be estimated.     

Anti-Staphylococcal Activity of the Auranofin Analogue Bearing Acetylcysteine in Place of the Thiosugar: An Experimental and Theoretical Investigation

Auranofin (AF, hereafter) is an orally administered chrysotherapeutic agent approved for the treatment of rheumatoid arthritis that is being repurposed for various indications including bacterial infections. Its likely mode of action involves the impairment of the TrxR system through the binding of the pharmacophoric cation [AuPEt₃]⁺. Accordingly, a reliable strategy to expand the medicinal profile of AF is the replacement of the thiosugar moiety with different ligands. Herein, we aimed to prepare the AF analogue bearing the acetylcysteine ligand (AF-AcCys, hereafter) and characterize its anti-staphylococcal activity. Biological studies revealed that AF-AcCys retains an antibacterial effect superimposable with that of AF against Staphylococcus aureus, whereas it is about 20 times less effective against Staphylococcus epidermidis. Bioinorganic studies confirmed that upon incubation with human serum albumin, AF-AcCys, similarly to AF, induced protein metalation through the [AuPEt₃]⁺ fragment. Additionally, AF-AcCys appeared capable of binding the dodecapeptide Ac-SGGDILQSGCUG-NH₂, corresponding to the tryptic C-terminal fragment (488–499) of hTrxR. To shed light on the pharmacological differences between AF and AF-AcCys, we carried out a comparative experimental stability study and a theoretical estimation of bond dissociation energies, unveiling the higher strength of the Au–S bond in AF-AcCys. From the results, it emerged that the lower lipophilicity of AF-AcCys with respect to AF could be a key feature for its different antibacterial activity. The differences and similarities between AF and AF-AcCys are discussed, alongside the opportunities and consequences that chemical structure modifications imply.     

Amperometric Glucose Determination by Means of Glucose Oxidase Immobilized on a Cellulose Acetate Film: Dependence on the Immobilization Procedures

Glucose microelectrodes were prepared by immobilizing glucose oxidase onto a cellulose acetate film coating a platinum wire. Hexamethylenediamine (HMDA) and Glutaraldehyde (GA) were employed as spacer and coupling agent, respectively. Sensitivities and linear response ranges were studied as a function of the relative amounts of HMDA and GA. The best sensitivity was found when HMDA and GA were 5% and 2.5% in aqueous solutions, respectively. Taking as a reference the functioning of this biosensor, the roles of HMDA and GA percentages appear to be opposed when the extension of the linear response range is considered. Indeed, an increase of one unit in HMDA percentage (from 5 to 6 %) induces an increase in the extension of the linear response range equal to that obtained with a decrease of one unit of GA percentage (from 2.5 to 1.5%).