Lectins,trypsin and α-amylase inhibitors in dietary supplements containing <Emphasis Type="Italic">Phaseolus vulgaris</Emphasis>

Some dietary supplements used to control overweight are based on protein concentrates from Phaseolus vulgaris, or kidney bean, known to contain high levels of α-amylase inhibitor, which may reduce the adsorption and prevent the digestion of carbohydrates. These concentrates of kidney bean also contain significant levels of antinutritional factors such as lectins and trypsin inhibitors. In recent years the concentrates of kidney bean have been processed to inactivate lectins and trypsin-inhibitor activity while preserving substantial α-amylase inhibitor activity. The aim of this study was to investigate and to compare the activity of the α-amylase inhibitor in some commercial supplements, and to determine the levels of residual lectins and trypsin inhibitors. The results show that the technological treatment used to reduce the levels of lectins and trypsin inhibitors partially decreases the activity of the amylase inhibitor. This study suggests the need for better standardization of the technological treatment of protein concentrates to ensure both the efficacy and safety of these dietary supplements.     

LOCAL++: A C++ framework for local search algorithms

Local search is an emerging paradigm for combinatorial search which has recently been shown to be very effective for a large number of combinatorial problems. It is based on the idea of navigating the search space by iteratively stepping from one solution to one of its neighbors, which are obtained by applying a simple local change to it. In this paper we present LOCAL++, an object‐oriented framework to be used as a general tool for the development and implementation of local search algorithms in C++. The framework comprises a hierarchy of abstract template classes, one for each local search technique taken into account (i.e. hill‐climbing, simulated annealing and tabu search). Each class specifies and implements the invariant part of the algorithm built according to the technique, and is supposed to be specialized by a concrete class once a given search problem is considered, so as to implement the problem‐dependent part of the algorithm. LOCAL++ comprises also a set of abstract classes for creating new techniques by combining different search techniques and different neighborhood relations. The architecture of LOCAL++ provides a principled modularization for the solution of combinatorial search problems, and helps the designer deriving a neat conceptual scheme of the application, thus facilitating the development and debugging phases. LOCAL++ proved to be flexible enough for the implementation of the algorithms solving various scheduling problems. Copyright © 2000 John Wiley & Sons, Ltd.     

Characterisation of mineral waters by pattern recognition methods

Eighty-three samples of mineral water from four different wells in the same district were analysed for 23 parameters. Nineteen parameters were chosen for multivariate analysis. Principal components analysis provided a feature reduction to two or three dimensions without substantial loss of information. The data set is well separated into four clusters using hierarchical and non-hierarchical methods; samples from different wells are generally assigned to different clusters. © 1998 SCI.     

Linear networks depending polynomially on parameters: dynamic behaviour for large values subject to tolerance errors

This paper is concerned with linear networks depending polynomially on parameters, when considering large values of the parameters, and their corresponding ideal networks—i.e. the networks in which all parameters are set equal to infinity. It has been taken into account that only the specification of nominal values and tolerances—and not of actual values—is physically meaningful. The stability of the ideal networks and the least hypotheses that allow us to use a previous algorithm to find monomial functions—in a single suitable variable—that describe arbitrarily large nominal values which ensure stability within a suitable constant tolerance are assumed. An integer h such that while these nominal values go to infinity then for any smooth causal excitations bounded together with their first h derivatives—in particular, for any smooth eventually periodic causal excitations—the zero‐state response of the actual networks converges uniformly on the whole time axis to that of the ideal networks is proved to exist. The proof may be used as an algorithm. An example which proves that the found class of excitations may be not the widest is given. The application of the results to the evaluation of the synchronization error due to high but finite values of the parameters in an ideally synchronizing linear network is shown. Copyright © 1999 John Wiley & Sons, Ltd.     

Verteporfin-Loaded Mesoporous Silica Nanoparticles’ Topical Applications Inhibit Mouse Melanoma Lymphangiogenesis and Micrometastasis In Vivo

Photodynamic therapy (PDT) has been pointed out as a candidate for improving melanoma treatment. Nanotechnology application in PDT has increased its efficacy by reducing side effects. Herein, mesoporous silica nanoparticles (MSNs) conjugated with verteporfin (Ver-MSNs), in use with PDT, were administered in mice to evaluate their efficacy on lymphoangiogenesis and micrometastasis in melanoma. Melanoma was induced in mice by the subcutaneous injection of B16-F10 cells. The mice were transcutaneously treated with MSNs, Ver-MSNs, or glycerol and exposed to red light. The treatment was carried out four times until day 20. Lymphangiogenesis and micrometastasis were identified by the immunohistochemical method. Lymphoangiogenesis was halved by MSN treatment compared with the control animals, whereas the Ver-MSN treatment almost abolished it. A similar reduction was also observed in lung micrometastasis. PDT with topically administrated Ver-MSNs reduced melanoma lymphoangiogenesis and lung micrometastasis, as well as tumor mass and angiogenesis, and therefore their use could be an innovative and useful tool in melanoma clinical therapy.     

Design and synthesis of cyclopeptide analogues of the potent histone deacetylase inhibitor FR235222

Various structurally modified analogues of FR235222 (1), a natural tetrapeptide inhibitor of mammalian histone deacetylases, were prepared in a convergent approach. The design of the compounds was aimed to investigate the effect of structural modifications of the tetrapeptide core involved in enzyme binding in order to overcome some synthetic difficulties connected with the natural product 1. The modifications introduced could also help identify key structural features involved in the mechanism of action of these compounds. The prepared molecules were subjected to in vitro pharmacological tests, and their potency was tested on cultured cells. Two of the components of the array were found to be more potent than the parent compound 1 and almost as efficient as trichostatin A (TSA). These results demonstrate that it is possible to synthesize highly active cyclic tetrapeptides using commercially available amino acids (with the exception of 2-amino-8-oxodecanoic acid, Ahoda). The nature of the residue in the second position of the cyclic peptide and the stereochemistry of the Ahoda tail are important for the inhibitory activity of this class of cyclic tetrapeptide analogues.     

2,3-oxidosqualene cyclase: From azasqualenes to new site-directed inhibitors

2,3-Oxidosqualene cyclases (OSC) are enzymes which convert 2,3-oxidosqualene (OS) into polycyclic triterpenoids such as lanosterol, cycloartenol, and α-and β-amyrin. Our interest in the study of OSC is the development of new OSC inhibitors for potential use as hypocholesterolemic, antifungal, or phytotoxic drugs. In particular, we describe the biological activity and the mechanism of a series of acyclic azasqualene derivatives mimicking the C-2, C-8, and C-20 carbonium ions formed during OS cyclization. Some of these carbonium ion analogues are very promising as specific hypocholesterolemic agents. The toxicity, the biodistribution, and the pharmacokinetics of different azasqualene derivatives in mice are also presented. In order to obtain new, site-directed irreversible inhibitors of OSC, a series of squalene derivatives containing functional groups that can link covalently to an active-site thiol group was designed. Among these compounds, squalene maleimide was the most active toward mammalian OSC, whereas squalene Ellman behaved as an irreversible inhibitor of OSC from yeast Based on a paper presented at the symposium on the “Regulation of Biosynthesis and Function of Isopentenoids” Atlanta, Georgia, May 1994.     

Enthalpy relaxation in bisphenol‐A polycarbonate/poly(methyl methacrylate) blends

Bisphenol‐A polycarbonate (PC)/poly(methyl methacrylate) (PMMA) blends (PC/PMMA) were prepared by melt mixing with and without a trans‐esterification catalyst (tetrabutylammoniun tetraphenylborate), which is able to promote inter‐exchange reactions between PC and PMMA. Evidences of the ester–ester exchange reaction taking place were pointed out via Fourier Transform Infra‐Red and size exclusion chromatography analyses. A series of enthalpy relaxation measurements were carried out for the pure polymers and for blends thereof. The data were analyzed on the basis of the Tool–Narayanaswamy–Moynihan/Kohlraush–Williams–Watts model. This model characterizes the structural relaxation in the glass transition region by means of four parameters: the apparent activation energy (Δh*), the nonlinearity (x), the nonexponentiality (β), and the pre‐exponential factor (τ₀). The apparent activation energy can be determined from the cooling rate dependence of the fictive temperature (T_f) measured using DSC. Δh* values of homogeneous blend and of the starting polymers were determined in this way, while an estimation of x, β and τ₀ was proposed. Comparisons were made between a single glass transition temperature PC/PMMA blend and homopolymers data. The experimental values of Δh* suggest that the degree of cooperativity decreases on going from the starting polymers to the blend. POLYM. ENG. SCI., 47:218–224, 2007. © 2007 Society of Plastics Engineers.     

Characterization of TiO2 coatings prepared by a modified electric arc-physical vapour deposition system

TiO₂ thin coatings were prepared, on various substrates, through evaporation of metallic titanium in an oxidizing atmosphere by modified electric arc-physical vapor deposition (EA-PVD). The coatings were characterized chemically (by means of XPS and SIMS) and from the structural point of view (by means of XRD and Raman spectroscopy), in order to understand the factors which lead to homogeneous coatings with high anatase content. The type of substrate is the main parameter that influences the crystal structure of the coatings: when stainless steel is used as substrate the coatings consist essentially of rutile, while on glass substrates coatings containing mainly anatase are obtained. The photocatalytic activity of the samples upon UVA irradiation was tested by using phenol as the target molecule. Phenol in the solution can be photocatalytically and rapidly degraded through the EA-PVD anatase TiO₂ coatings.