Evaluation of 4-(4-Fluorobenzyl)piperazin-1-yl]-Based Compounds as Competitive Tyrosinase Inhibitors Endowed with Antimelanogenic Effects

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.     

3D floor plan recovery from overlapping spherical images

Computational Visual Media - We present a novel approach to automatically recover, from a small set of partially overlapping spherical images, an indoor structure representation in terms of a 3D...     

HLA antigens and erythrocyte glucose-6-phosphate dehydrogenase (G-6-PD) deficiency in Sardinia

Wind enhances the carcinogenic effect of chronic Iltraviolet radiation (UVL). This was demonstrated in hairless mice that were irradiated for 42 weeks with mercury are lamps. One group of animals was exposed to continuous wind flow of 2.7 m/s except for the daily I-2 min time interval when they were removed from the wind tunnel and irradiated. Another group of animals received identical irradiation but were protected from wind. The first tumour appeared in the UVL and wind group after 105 days of irradiation, and at 164 days of irradiation all surviving mice in the group had developed tumours. The group of mice receiving identical irradiation but protected from wind had their first tumour appear at 154 days of irradiation, and by 164 days of irradiation only 40% of the mice had developed tumours.     

Sardinian honeys as sources of xanthine oxidase and tyrosinase inhibitors

Sardinian honeys obtained from different floral sources (Arbutus, Asphodelus, Eucalyptus, Thistle, and Sulla) were evaluated for their ability to inhibit tyrosinase and xanthine oxidase enzymes and for their antioxidant activity. Physicochemical parameters, total phenolic, and flavonoids content were also determined. Honey from Arbutus flowers had the highest antioxidant activity followed by Eucalyptus and Thistle ones. These three honeys showed good tyrosinase and xanthine oxidase inhibition properties. Thus, these Sardinian honeys could have a great potential as antioxidant sources for pharmaceutical and cosmetic applications.     

Effects of sheep alpha s1-casein CC, CD and DD genotypes on milk composition and cheesemaking properties.

The effects of sheep alpha s1-casein CC, CD and DD genotypes on milk composition and cheese yield were studied. Processed bulk milk was collected from three groups of 15 ewes, carrying alpha s1-casein CC, CD and DD genotypes. CC milk was higher in casein content than CD or DD milk (+3.5 and +8.6% respectively), and had a higher protein: fat ratio and a smaller casein micelle diameter. In addition, DD milk had a significantly lower alpha s1-casein content. The main differences were in curd formation: CC milk had better renneting properties. Cheesemaking trials, carried out in a pilot plant, showed that CC milk had better cheesemaking characteristics than DD milk, while CD milk was intermediate. Both 1 d old and fully ripened cheeses had different fat: dry matter ratios and alpha s1-I-casein electrophoretic mobilities: these were lower for DD cheese. As a consequence, these genotypes could be considered as markers of milk and/or cheese quality.     

MBE growth of silicon films on diamond substrates

Si(111) 7 × 7 films are grown by MBE on clean (111) diamond surfaces. It is shown that the film structure can be controlled in real time by varying the substrate temperature and Si flux. Modes of growth are identified that provide Si films of higher crystalline quality.Translated from Mikroelektronika, Vol. 34, No. 1, 2005, pp. 37–42.Original Russian Text Copyright © 2005 by Karasev, Kryukov, Kuznetsov, Pintus, Lamin, Pchelyakov, Sokolov.     

Shape enhancement for rapid prototyping

Many applications, for instance, in the reverse engineering and cultural heritage field, require building a physical replica of 3D digital models. Recent 3D printers can easily perform this task in a relatively short time and using color to reproduce object textures. However, the finite resolution of printers and, most of all, some peculiar optical and physical properties of the used materials reduce their perceptual quality. The contribution of this paper is a shape enhancing technique which allows users to increase readability of the tiniest details in physical replicas, without requiring manual post-reproduction interventions.     

High brightness GaN LEDs degradation during dc and pulsed stress

This paper reports an analysis of InGaN/GaN LEDs degradation under dc and pulsed current conditions. The analysis was carried out by means of current-voltage and optical power measurements, scanning electron microscopy and EDS maps. Identified degradation modes were leakage and generation/recombination current increase, series resistance increase and output power decrease, related to the high temperatures reached by the devices during stress. Failure analysis revealed degradation of anode contacts and Ti-W reflector, which can be related to the measured series resistance increase. Comparison between dc and pulsed stress carried out with the same average current indicated that pulsed driving does not imply an acceleration in the degradation rate, except for the lowest duty cycles.     

Purification and characterisation of a soluble nucleotide pyrophosphatase/phosphodiesterase from prickly pear (Opuntia ficus indica) fruits

A glycosylated metallo-protein, nucleotide pyrophosphatase/phosphodiesterase, in a soluble form was purified to homogeneity from prickly pear (Opuntia ficus indica) fruits. The native protein had a molecular mass of 105 ± 8 kDa and was formed by two apparently identical subunits each containing 1 Ca²⁺ and 1 Mg²⁺ ion. The Opuntia enzyme exhibited hydrolytic activities toward pyrophosphate/phosphodiester bonds of a broad range of natural substrates, but among these, only NAD(P) and NAD(P)H were hydrolysed very efficiently. Moreover, Opuntia pyrophosphatase/phosphodiesterase hydrolysed the artificial substrate thymidine 5′-monophosphate 4-nitrophenyl ester, whereas it did not show any catalytic activity toward bis-4-nitrophenyl phosphate, which is a substrate of other pyrophosphatase/phosphodiesterase enzymes. We observed an increase of enzyme activity from the green to the red stage of fruits development, suggesting that ONPP activity might be related to the ripening of prickly pears. The protein was shown to be resistant to 75 °C for 30 min. Other biochemical characteristics were investigated and are reported here.     

New vistas for diamond as an electronic material

A novel technique of surface treatment is described, involving excitation of coherent traveling elastic waves on the surface. It enables one to produce diamond crystals with high-quality faces whatever the crystallographic orientation. The technique is shown to provide prescribed smooth convex faces of degree 2 (conical, ellipsoidal, or paraboloidal). Future applications of diamonds thus processed are discussed.