Synthesis of Benzophenones and in vitro Evaluation of Their Anticancer Potential in Breast and Prostate Cancer Cells

Breast and prostate cancers are frequently treated with chemotherapy. Several novel chemicals are being reported for this purpose, particularly synthetic and natural benzophenones. This work reports the synthesis of substituted 2-hydroxybenzophenones through 1,4-conjugate addition/intramolecular cycloaddition/dehydration of nitromethane on key intermediate chromones. Structures were extensively studied by means of 2D NMR spectroscopy and single-crystal XRD. Their cytotoxicity was evaluated in vitro in two breast cancer cell lines (MDA-MB-231 and T47-D) and one prostate cancer cell line (PC3). The most potent compound exhibited good cytotoxic effects against the three cancer cell lines (IC₅₀ values ranging from 12.09 to 26.49 μm ) and induced cell-cycle retardation only on prostate cancer cells, which suggested that it might exert cell-type-specific effects.     

Spectral studies of zinc octacarboxyphthalocyanine aggregation

The association of zinc octacarboxyphthalocyanine, was studied using UV–vis absorption and fluorescence emission spectroscopy; the effects of dye concentration, pH and solvents on spectra were discussed. Calculations showed that the dye dimerized in aqueous solutions ranging from 5.0 × 10^?7 to 5.0 × 10^?5 mol/dm³, at 25 °C. The dimerization constant of 10⁶ dm³/mol and the spectral Q band shift of 1185 cm^?1 imparted by dimerization indicated strong π–π interactions between phthalocyanine molecules. Red S₁ fluorescence of the dye monomer was observed in various solutions which was quenched owing to molecular association and other factors. The strong influence of pH on both aggregation and fluorescence was discussed. At pH < 5.0, only dye aggregates were present in solution; monomers appeared at pH ≥ 5.0 and, in alkaline solution, only the monomeric anions of phthalocyanine existed. The spectral absorption and emission data for the dye in binary solvents revealed that at concentrations ranging from 0.5 × 10^?5 to 1.0 × 10^?5 mol/dm³, the dye can be used in photosensitised oxidation reactions.     

Attaching Different Kinds of Proteinaceous Nanospheres to a Variety of Fabrics Using Ultrasound Radiation

The application of a rapid, non-destructive, cost-effective technique such as ultrasonic emulsification for the coating of different textiles was explored. The technical benefits for this research were the generation of multifunctional materials and their combinations through environmentally friendly processing technologies. We have shown for the first time that ultrasonic waves can be used to coat proteinaceous micro- and nanospheres (PM) of BSA (Bovine Serum Albumin) protein and casein on the surface of cotton and polyester (PE) fabrics. The creation and the anchoring of the microbubbles to the fabrics were performed by a one-step reaction, and the process is usually stopped after 3 min. The PM of bovine serum albumin (BSA) bonded to cotton and polyester fabrics has shown stability for ∼9 months. The PMs were shown to be attached more strongly to the polyester than to the cotton, and sustained stronger washing conditions on PE. The diameter of the BSA and the casein spheres on cotton was in the range of 0.8–1.0 μm, while on the PE it varied between 60 and 120 nm.     

PPAR-Gamma Activation May Inhibit the In Vivo Degeneration of Bioprosthetic Aortic and Aortic Valve Grafts under Diabetic Conditions

Background: We aimed to examine the anti-calcification and anti-inflammatory effects of pioglitazone as a PPAR-gamma agonist on bioprosthetic-valve-bearing aortic grafts in a rat model of diabetes mellitus (DM). Methods: DM was induced in male Wistar rats by high-fat diet with an intraperitoneal streptozotocin (STZ) injection. The experimental group received additional pioglitazone, and controls received normal chow without STZ (n = 20 each group). Cryopreserved aortic donor grafts including the aortic valve were analyzed after 4 weeks and 12 weeks in vivo for analysis of calcific bioprosthetic degeneration. Results: DM led to a significant media proliferation at 4 weeks. The additional administration of pioglitazone significantly increased circulating adiponectin levels and significantly reduced media thickness at 4 and 12 weeks, respectively (p = 0.0002 and p = 0.0107, respectively). Graft media calcification was highly significantly inhibited by pioglitazone after 12 weeks (p = 0.0079). Gene-expression analysis revealed a significant reduction in relevant chondro-osteogenic markers osteopontin and RUNX-2 by pioglitazone at 4 weeks. Conclusions: Under diabetic conditions, pioglitazone leads to elevated circulating levels of adiponectin and to an inhibition of bioprosthetic graft degeneration, including lower expression of chondro-osteogenic genes, decreased media proliferation, and inhibited graft calcification in a small-animal model of DM.     

Electrocombustion of humic acid and removal of algae from aqueous solutions

This paper reports experiments involving the electrochemical combustion of humic acid (HA) and removal of algae from pond water. An electrochemical flow reactor with a boron-doped diamond film anode was used and constant current experiments were conducted in batch recirculation mode. The mass transfer characteristics of the electrochemical device were determined by voltammetric experiments in the potential region of water stability, followed by a controlled current experiment in the potential region of oxygen evolution. The average mass transfer coefficient was 5.2 × 10⁻⁵ m s⁻¹. The pond water was then processed to remove HA and algae in the conditions in which the reaction combustion occurred under mass transfer control. To this end, the mass transfer coefficient was used to estimate the initial limiting current density applied in the electrolytic experiments. As expected, all the parameters analyzed here—solution absorbance at 270 nm, total phenol concentration and total organic carbon concentration—decayed according to first-order kinetics. Since the diamond film anode successfully incinerated organic matter, the electrochemical system proved to be predictable and programmable.     

High concentration of phosphorus is a distinctive feature of myelin. An X‐Ray elemental microanalysis study using freeze‐fracture scanning electron microscopy of rat sciatic nerve

We have used rat sciatic nerves submitted to freezing and freeze‐fracture to determine the elemental composition of small domains of the peripheral nerve studied at high resolution by scanning electron microscopy. We found that myelin of Schwann cells is unique in its high content in phosphorus (P) that was more than 10 times higher than P measured in any other cells. This high concentration in P makes myelin chemistry suitable of monitoring at the subcellular level using the herein described methodology. Microsc. Res. Tech. 78:537–539, 2015. © 2015 Wiley Periodicals, Inc.     

Wetting Behavior and Reactivity of Molten Silicon with h-BN Substrate at Ultrahigh Temperatures up to 1750 °C

For a successful implementation of newly proposed silicon-based latent heat thermal energy storage systems, proper ceramic materials that could withstand a contact heating with molten silicon at temperatures much higher than its melting point need to be developed. In this regard, a non-wetting behavior and low reactivity are the main criteria determining the applicability of ceramic as a potential crucible material for long-term ultrahigh temperature contact with molten silicon. In this work, the wetting of hexagonal boron nitride (h-BN) by molten silicon was examined for the first time at temperatures up to 1750 °C. For this purpose, the sessile drop technique combined with contact heating procedure under static argon was used. The reactivity in Si/h-BN system under proposed conditions was evaluated by SEM/EDS examinations of the solidified couple. It was demonstrated that increase in temperature improves wetting, and consequently, non-wetting-to-wetting transition takes place at around 1650 °C. The contact angle of 90° ± 5° is maintained at temperatures up to 1750 °C. The results of structural characterization supported by a thermodynamic modeling indicate that the wetting behavior of the Si/h-BN couple during heating to and cooling from ultrahigh temperature of 1750 °C is mainly controlled by the substrate dissolution/reprecipitation mechanism.     

Bioactive extracts of orange (Citrus sinensis L. Osbeck) pomace obtained by SFE and low pressure techniques: Mathematical modeling and extract composition

The objective of this study was to obtain orange (Citrus sinensis L. Osbeck) pomace extract using supercritical fluid extraction (SFE) with CO₂ and with CO₂ and co-solvent. In order to evaluate the high pressure method in terms of process yield, extract composition and biological activity, low pressure methods were also applied to obtain orange extracts, such as ultrasound (UE) and soxhlet (SOX), with different organic solvents, and hydrodistillation (HD). The SFE conditions were temperatures of 313.15 K and 323.15 K and pressures from 100 to 300 bar. The SFE kinetics and mathematical modeling of the overall extraction curves (OEC) were also investigated. The antioxidant potential of the extracts was evaluated by the DPPH method, by the Folin-Ciocalteau method and by the β-carotene/linoleic acid bleaching method. The antimicrobial activity of the extracts was also studied. The main compounds identified were l-limonene, palmitic and oleic acids, n-butyl benzenesulfonamide and β-sitosterol.     

Vitamin D Compounds PRI-2191 and PRI-2205 Enhance Anastrozole Activity in Human Breast Cancer Models

1,25-Dihydroxycholecalciferol, the hormonally active vitamin D₃ metabolite, is known to exhibit therapeutic effects against breast cancer, mainly by lowering the expression of estrogen receptors and aromatase activity. Previously, the safety of the vitamin D active metabolite (24R)-1,24-dihydroxycholecalciferol (PRI-2191) and 1,25(OH)₂D₃ analog PRI-2205 was tested, and the in vitro activity of these analogs against different cancer cell lines was studied. We determined the effect of the two vitamin D compounds on anastrozole (An) activity against breast cancer based on antiproliferative activity, ELISA, flow cytometry, enzyme inhibition potency, PCR, and xenograft study. Both the vitamin D active metabolite and synthetic analog regulated the growth of not only estrogen receptor-positive cells (T47D and MCF-7, in vitro and in vivo), but also hormone-independent cancer cells such as SKBR-3 (HER-2-positive) and MDA-MB-231 (triple-negative), despite their relatively low VDR expression. Combined with An, PRI-2191 and PRI-2205 significantly inhibited the tumor growth of MCF-7 cells. Potentiation of the antitumor activity in combined treatment of MCF-7 tumor-bearing mice is related to the reduced activity of aromatase by both An (enzyme inhibition) and vitamin D compounds (switched off/decreased aromatase gene expression, decreased expression of other genes related to estrogen signaling) and by regulation of the expression of the estrogen receptor ERα and VDR.     

Simple approach for the plasma treatment of polymeric membranes and investigation of the aging effect

The modification of the surface characteristics after treatment with plasma in polymeric materials, such as the aging phenomenon, calls the attention of research in the area of nonthermal plasma technology. In this work, a direct treatment with dielectric-barrier discharge plasma was used on the surfaces of ultrafiltration membranes. The measurements of the contact angle with water, attenuated total reflectance accessory, zeta potential, atomic force microscopy and scanning electron microscopy-MEV were performed on the surfaces to verify changes after plasma treatment and to understand the occurrence and timing of the plasma aging effect. In the analysis of the membrane performance, hydraulic permeation and protein retention tests were performed. The results showed an improvement in wettability and hydrophilic properties in the post-treated membranes. The study of reversibility/aging of the post-plasma surface is important for research that deals with the modification of polymeric membranes. Changes in surface morphology, topography and wettability of the membranes were observed up to seven days after treatment, with a tendency to return to the initial characteristics of the membranes.