Borcalein: a Carborane-Based Analogue of Baicalein with 12-Lipoxygenase-Independent Toxicity

12-Lipoxygenase is crucial for tumour angiogenesis. 5,6,7-Trihydroxy-2-phenyl-4H-1-benzopyran-4-one (baicalein) is a suitable inhibitor for this enzyme but is rapidly metabolised in vivo. Thus, an improvement of the metabolic stability is necessary to enhance the therapeutic efficiency. An emerging approach to enhance metabolic stability of carbon-based pharmaceuticals is the use of metabolically stable, non-toxic boron clusters, such as dicarba-closo-dodecaborane(12)s (carboranes) as phenyl mimetics. Therefore, the unsubstituted phenyl ring of baicalein was replaced by meta-carborane, resulting in borcalein, the carborane analogue of baicalein. This substitution resulted in a decreased inhibitory activity toward 12-lipoxygenase, but led to increased toxicity in melanoma (A375, B16, B16F10) and colon cancer cell lines (SW480, HCT116, CT26CL25) with decreased tumour selectivity in comparison to baicalein. Surprisingly, borcalein displays a different mechanism of cytotoxicity with increased intracellular production of reactive oxygen species (ROS), reactive nitrogen species (RNS) and nitric oxide (NO).     

An initial study on feasible treatment of Serbian lignite through utilization of low-rank coal upgrading technologies

Despite benefiting from vast fuel reserves, combustion of low-rank coals is commonly characterized by low thermal efficiency and high pollutant emissions, partly due to high moisture content of the coals in question. Thus, removal of moisture from low-rank coals is deemed an important quality upgrading method. The paper provides an overview of the current status of low-rank coal upgrading technologies, particularly with respect to utilization of drying and dewatering procedures. In order to examine the influence of relevant parameters on the moisture removal process, a model of convective coal drying in a packed, as well as in a fluid bed combustion arrangement, is developed and presented. Product-specific data (intraparticle mass transfer, gas–solid moisture equilibrium) related to the coal variety addressed herein (lignite) are obtained through preliminary investigations. Effective thermal conductivity of the packed bed as defined by Zehner/Bauer/Schlünder is used to define heat transfer mechanisms occurring in the packed bed. Similar two-phase fluidization model has been validated for different types of biomaterials.     

The dependence of the photocatalytic activity of TiO2/carbon nanotubes nanocomposites on the modification of the carbon nanotubes

Nanostructural TiO₂/modified multi-wall carbon nanotubes photocatalysts were prepared by hydrolysis of Ti(iso-OC₃H₇)₄ providing chemical bonding of anatase TiO₂ nanoparticles onto oxidized- or amino-functionalized multi-wall carbon nanotubes (MWCNT). The processes of functionalization of the MWCNT and the deposition of TiO₂ influence the photocatalytic activity of the synthesized nanocomposites. The phase composition, crystallite size, and the structural and surface properties of the obtained TiO₂/modified-MWCNT nanocomposite were analyzed from XRD, FEG-SEM, TEM/HRTEM and FTIR data, as well low temperature N₂ adsorption. In the photocatalytic study, the TiO₂/oxidized-MWCNT catalyst showed the highest and the TiO₂/amino functionalized-MWCNT catalysts somewhat lower degradation rates, indicating that the enhancement of photocatalysis was supported by the more effective electron transfer properties of the oxygen- than amino-containing functional groups, which support the efficient charge transportation and separation of the photogenerated electron-hole pairs.     

Combined Application of Experimental Design and Artificial Neural Networks in Modeling and Characterization of Spray Drying Drug: Cyclodextrin Complexes

The aim of this study was to investigate the usefulness of combined application of quality by design tools such as central composite design (CCD), response surface methodology (RSM), and artificial neural networks (ANN) in the characterization, modeling, and optimizaton of spray drying of a poorly soluble drug : cyclodextrin complex. Models were developed by RSM and ANN from different pools of data. The model with best predictability was the ANN multilayer perceptron (MLP)1 model developed from the largest group of data (R ² for response yield 0.854, moisture content 0.886). On the other hand, analysis of equations derived from the application of RSM contributed in better understanding the complex relationships between input and output variables. By application of a desirability function approach, optimal process parameters that resulted in the best process yield (86%) and minimal moisture content in the powder (3.3%) were established (25% feed concentration, 180°C inlet air temperature, 10% pump speed).     

Wheat flour confectionery products as a source of inorganic nutrients: zinc and copper contents in hard biscuits

Cereal-based confectionery products being consumed through whole human life are considered mainly to be a source of carbohydrates, that is energy, although cereals are a rich source of minerals as well. To evaluate some hard biscuits produced in Croatia as a source of different trace elements in nutrition, in this study Zn and Cu contents were determined in classic wheat flour biscuits and in dietetic biscuits enriched with whole wheat grain flour or whole wheat grain grits, soya flour and skimmed milk. Zn was determined by flame atomic absorption spectrometry (AAS); Cu was determined by inductively coupled plasma atomic emission spectroscopy (ICP-AES). The results show that the Zn content in different kinds of biscuits ranges from 5.89 up to 17.64 mg/kg and the Cu content ranges from 1.15 up to 2.79 mg/kg depending on the type of wheat milling products and mineral content of other ingredients used. Enriched dietetic biscuits produced from wheat flour type 850 and whole wheat grain flour and/or soya flour and skimmed milk were almost 200% and 150% higher in Zn and Cu, respectively, in comparison to classic white wheat flour biscuits and can be considered as good sources of Zn and Cu in nutrition.     

Occurrence of Campylobacter spp. in poultry and poultry products for sale on the Polish retail market

In 2007 and 2008, a monitoring study was carried out in Poland to examine the occurrence of thermotolerant Campylobacter spp. in raw and cooked chicken products available on the retail market. A total of 912 samples were tested: 443 samples of raw chicken meat, 146 samples of giblets, and 323 ready-to-eat poultry products (150 samples of spit-roasted chicken, 56 samples of smoked chicken, and 117 samples of paté and cold meats). A high level of contamination of raw chicken meat (51.7% of samples) and chicken giblets (47.3% of samples) was detected. However, thermotolerant Campylobacter spp. were found in only 1.2% of the ready-to-eat poultry products.     

Application of GC–MSD and LC–MS/MS for the determination of priority pesticides in baby foods in Serbian market

Babies and small children are especially sensitive population to the exposure to environmental contaminants. Their small mass and developing systems, including brain development may show adverse health effects from even low levels of contamination on a chronic or single dose case. In this paper one extraction method and two chromatographic techniques for the determination of pesticide residues in baby food were evaluated. A liquid chromatography–tandem mass spectrometry technique combined with electrospray ionization (ESI), (LC–MS/MS) and gas chromatography–mass spectrometry detection (GC–MSD) technique were applied in the detection of 50 pesticides in baby food. So-called QuEChERS (quick, easy, cheap, effective, rugged and safe) method was used as a sample preparation procedure. The recoveries were investigated at three levels (5, 10 and 50 μg/kg) and the results obtained showed compliance with the contemporary EU requirements with a few exceptions. LOQs for most of the tested pesticides were below the EU MRLs (10 μg/kg), except deltamethrin, cypermethrin, fenvalerate, phosalone and beta-cyfluthrin (LOQs were 10 μg/kg). Both techniques were applied in the analysis of 50 samples of baby food manufactured in Serbia.     

Changes of hydrogen peroxide and radical-scavenging activity of raspberry during osmotic, convective, and freeze-drying

This study was conducted to investigate the influence of different drying treatments on antioxidant (AO) activity and phenolic content of raspberry (Rubus idaeus), cultivar Willamette. Whole raspberry fruits were dried convectively (air-drying), osmotically, and freeze-dried. Acetone-water extracts of fresh and dried raspberries were assessed for total phenolic content by standard Folin-Ciocalteau method. Two AO assays were applied, a recently developed direct current (DC) polarographic assay based on decrease of anodic oxidation current of hydrogen peroxide and widely used radical scavenge against the 1,1-diphenyl-2-picrylhydrazyl (DPPH). Strong correlation has been obtained between both AO assays and total phenolic content. In addition, some individual phenolic compounds present in raspberry have been assessed using DPPH and DC polarographic assay. Comparison and evaluation of drying methods has been based on preservation of AO activity and total phenolic content. Obtained results confirmed superiority of freeze-drying; convective drying caused slight changes while osmotic dehydration showed a significant decrease of phenolic compounds and AO activity.     

THE INFLUENCE OF PRESSURE AND TEMPERATURE ON THE KINETICS OF VACUUM DRYING OF KETOPROFEN

ABSTRACT

This paper explores the influence of temperature and pressure on drying kinetics of 2-(3-benzoylphenil propionic acid) ketoprofen, in a vacuum dryer on laboratory scale, Experimentally determined relations between moisture content and drying rate vs time, were approximated with an exponential model. Model parameters were correlated with drying conditions (temperature, pressure) and defined by functions of their potentions.

From an energy balance of the process, a mathematical model for simulating dependence of sample temperature vs drying time, and moisture content of material, has been developed.

Simulation of the drying kinetics and sample temperature, by use of those functional dependencies shows good agreement with experimental results.