Salicylketoximes That Target Glucose Transporter 1 Restrict Energy Supply to Lung Cancer Cells

The glucose transporter GLUT1 is frequently overexpressed in most tumor tissues because rapidly proliferating cancer cells rely primarily on glycolysis, a low‐efficiency metabolic pathway that necessitates a very high rate of glucose consumption. Because blocking GLUT1 is a promising anticancer strategy, we developed a novel class of GLUT1 inhibitors based on the 4‐aryl‐substituted salicylketoxime scaffold. Some of these compounds are efficient inhibitors of glucose uptake in lung cancer cells and have a notable antiproliferative effect. In contrast to their 5‐aryl‐substituted regioisomers, the newly synthesized compounds reported herein do not display significant binding to the estrogen receptors. The inhibition of glucose uptake in cancer cells by these compounds was further observed by fluorescence microscopy imaging using a fluorescent analogue of glucose. Therefore, blocking the ability of tumor cells to take up glucose by means of these small molecules, or by further optimized derivatives, may be a successful approach in the development of novel anticancer drugs.     

Influence of sucrose on cold gelation of heat‐denatured whey protein isolate

A solution of heat‐denatured whey proteins was prepared by heating 100 g kg⁻¹ whey protein isolate (WPI) at pH 7.0 to 75 °C for 15 min in the absence of salt. Heat treatment caused the globular protein molecules to unfold, but electrostatic repulsion opposed strong protein–protein aggregation and so prevented gel formation. When the heat‐denatured whey protein solution was cooled to room temperature and mixed with 15 mM CaCl₂, it formed a gel. We investigated the influence of the presence of sucrose in the protein solutions prior to CaCl₂ addition on the gelation rate. At relatively low concentrations (0–100 g kg⁻¹), sucrose decreased the gelation rate, presumably because sucrose increased the aqueous phase viscosity. At higher concentrations (100–300 g kg⁻¹), sucrose decreased the gelation rate, probably because sugar competes for the water of hydration and therefore increases the attraction between proteins. These data have important implications for the application of cold‐setting WPI ingredients in sweetened food products such as desserts. © 2000 Society of Chemical Industry     

Gene-Delivery Ability of New Hydrogenated and Partially Fluorinated Gemini bispyridinium Surfactants with Six Methylene Spacers

The pandemic emergency determined by the spreading worldwide of the SARS-CoV-2 virus has focused the scientific and economic efforts of the pharmaceutical industry and governments on the possibility to fight the virus by genetic immunization. The genetic material must be delivered inside the cells by means of vectors. Due to the risk of adverse or immunogenic reaction or replication connected with the more efficient viral vectors, non-viral vectors are in many cases considered as a preferred strategy for gene delivery into eukaryotic cells. This paper is devoted to the evaluation of the gene delivery ability of new synthesized gemini bis-pyridinium surfactants with six methylene spacers, both hydrogenated and fluorinated, in comparison with compounds with spacers of different lengths, previously studied. Results from MTT proliferation assay, electrophoresis mobility shift assay (EMSA), transient transfection assay tests and atomic force microscopy (AFM) imaging confirm that pyridinium gemini surfactants could be a valuable tool for gene delivery purposes, but their performance is highly dependent on the spacer length and strictly related to their structure in solution. All the fluorinated compounds are unable to transfect RD-4 cells, if used alone, but they are all able to deliver a plasmid carrying an enhanced green fluorescent protein (EGFP) expression cassette, when co-formulated with 1,2-dioleyl-sn-glycero-3-phosphoethanolamine (DOPE) in a 1:2 ratio. The fluorinated compounds with spacers formed by six (FGP6) and eight carbon atoms (FGP8) give rise to a very interesting gene delivery activity, greater to that of the commercial reagent, when formulated with DOPE. The hydrogenated compound GP16_6 is unable to sufficiently compact the DNA, as shown by AFM images.     

Semi-supervised ensemble classification in subspaces

Graph-based semi-supervised classification depends on a well-structured graph. However, it is difficult to construct a graph that faithfully reflects the underlying structure of data distribution, especially for data with a high dimensional representation. In this paper, we focus on graph construction and propose a novel method called semi-supervised ensemble classification in subspaces, SSEC in short. Unlike traditional methods that execute graph-based semi-supervised classification in the original space, SSEC performs semi-supervised linear classification in subspaces. More specifically, SSEC first divides the original feature space into several disjoint feature subspaces. Then, it constructs a neighborhood graph in each subspace, and trains a semi-supervised linear classifier on this graph, which will serve as the base classifier in an ensemble. Finally, SSEC combines the obtained base classifiers into an ensemble classifier using the majority-voting rule. Experimental results on facial images classification show that SSEC not only has higher classification accuracy than the competitive methods, but also can be effective in a wide range of values of input parameters.     

Identification of spatial PH quintic Hermite interpolants with near-optimal shape measures

The problem of specifying the two free parameters that arise in spatial Pythagorean-hodograph (PH) quintic interpolants to given first-order Hermite data is addressed. Conditions on the data that identify when the “ordinary” cubic interpolant becomes a PH curve are formulated, since it is desired that the selection procedure should reproduce such curves whenever possible. Moreover, it is shown that the arc length of the interpolants depends on only one of the parameters, and that four (general) helical PH quintic interpolants always exist, corresponding to extrema of the arc length. Motivated by the desire to improve the fairness of interpolants to general data at reasonable computational cost, three selection criteria are proposed. The first criterion is based on minimizing a bivariate function that measures how “close” the PH quintic interpolants are to a PH cubic. For the second criterion, one of the parameters is fixed by first selecting interpolants of extremal arc length, and the other parameter is then determined by minimizing the distance measure of the first method, considered as a univariate function. The third method employs a heuristic but efficient procedure to select one parameter, suggested by the circumstances in which the “ordinary” cubic interpolant is a PH curve, and the other parameter is then determined as in the second method. After presenting the theory underlying these three methods, a comparison of empirical results from their implementation is described, and recommendations for their use in practical design applications are made.     

Color changes in architectural limestones from pollution and cleaning

This article investigates the impact of sulfur dioxide attack, deposition of dark particles in urban environments and laser cleaning with Nd:YAG 1064 nm on color change in a range of ornamental limestones. We have used the CIELAB and CIELCH systems to compare the relative importance of the variation of each coordinate for the color change. Sulfur dioxide and dark particle deposition seems to increase the chroma, most particularly in the yellow component. Particle deposition also leads to an obvious darkening of stone surfaces. Laser irradiation at 1064 nm affects the red component of limestone, particularly if they already possess a reddish color. In general, the more intense the original color of the stone the greater are the chromatic changes, but the direction change of the color‐parameter affected by a particular process remains the same. It has always been apparent in an atmosphere heavily polluted with soot that the main changes to light‐colored stones are the exponential decrease in the parameter L* (darkening–blackening). This has important aesthetic and social implications. However, in the near future it may be that in cleaner atmospheres, perhaps more dominated by organic pollutants, a yellowing process may be of greater concern. © 2007 Wiley Periodicals, Inc. Col Res Appl, 32, 320–331, 2007     

Physical,Chemical, and Biological Characterization of Veiled Extra Virgin Olive Oil Turbidity for Degradation Risk Assessment

Six different 300 kg batches of olive fruits are processed and the resulting six 20 kg batches of oil are collected at the end of the “decanter.” These batches of oil are subjected to four different water and solid particle separation treatments so as to obtain the following oil samples: veiled oil, filtered oil, “solid particle‐only” oil, and “water‐only” oil. The applied separation treatments show that water content has an important role in the degree of turbidity. High water content values (>0.2% w/w) are related to water activity values of >0.6 which are suitable for chemical and enzymatic reactions. The veiled oil samples are contaminated by microorganisms, but non‐proportional behavior occurs between the microbial cell count and the water and solid particle contents. Practical Applications: The results of this study recommend a multi‐approach method to characterize turbidity, based on control markers such as the degree of turbidity, water content and water activity, solid particle content, microbial contamination, and phenolic compound content. In this way, each degree of turbidity can be associated with a different level of risk of veiled extra virgin olive oil degradation during shelf life.     

Volatile components of artemisia vallesiaca all. (Mountain wormwood)

Summary The essential oil obtained by steam distillation of the leaves and flowers ofArtemisia vallesiaca All., a plant widely employed in the liqueur making industry and of almost completely unknown chemical composition, after separation on a silica gel column, was investigated by means of GLC, IR and mass spectrometry. Camphene, 1,8-cineole, camphor and borneol accounted for 67–68% of the oil. Over one hundred minor compounds were found by capillary gas chromatography and 52 were identified (Table 1).

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Die flüchtigen Aromastoffe von Artemisia vallesiaca All. (Berg-Genippi)

Zusammenfassung Das ätherische Öl — erhalten durch Wasserdampfdistillation aus Blättern und Blüten derArtemisia vallesiaca All., einer Pflanze, die in der Wermut-und Likörproduktion viel verwendet wird, aber chemisch fast unbekannt ist — wurde nach Säulenchromatographie an Kieselgel analysiert mittels GLC, IR und GLC-MS. Camphen, 1,8-Cineol, Campher und Borneol bilden 67–68% des ätherischen Öl. Mehr als 100 weitere Bestandteile wurden durch GLC gefunden und 52 von diesen wurden identifiziert (Tabelle 1).

     

Anticancer agents that counteract tumor glycolysis

Can we consider cancer to be a “metabolic disease”? Tumors are the result of a metabolic selection, forming tissues composed of heterogeneous cells that generally express an overactive metabolism as a common feature. In fact, cancer cells have increased needs for both energy and biosynthetic intermediates to support their growth and invasiveness. However, their high proliferation rate often generates regions that are insufficiently oxygenated. Therefore, their carbohydrate metabolism must rely mostly on a glycolytic process that is uncoupled from oxidative phosphorylation. This metabolic switch, also known as the Warburg effect, constitutes a fundamental adaptation of tumor cells to a relatively hostile environment, and supports the evolution of aggressive and metastatic phenotypes. As a result, tumor glycolysis may constitute an attractive target for cancer therapy. This approach has often raised concerns that antiglycolytic agents may cause serious side effects toward normal cells. The key to selective action against cancer cells can be found in their hyperbolic addiction to glycolysis, which may be exploited to generate new anticancer drugs with minimal toxicity. There is growing evidence to support many glycolytic enzymes and transporters as suitable candidate targets for cancer therapy. Herein we review some of the most relevant antiglycolytic agents that have been investigated thus far for the treatment of cancer.