Performance of limestone-based sorbent for sorption-enhanced gasification in dual interconnected fluidized bed reactors

A possibility to carry out sorption-enhanced gasification (SEG) is represented by its integration with the calcium looping concept in dual interconnected fluidized beds (DIFB). This article is focused on the sorbent CO₂ uptake performance and attrition/fragmentation tendency when operating conditions simulating those of a DIFB-SEG process are adopted. Experiments were carried out on a commercial Italian limestone in a laboratory-scale DIFB reactor. Carbonation was carried out in a range of test conditions, including variable temperature (600–700°C) and absence/presence of steam (10% by volume); CO₂ concentration was set at 10% by volume. The characterization is extended by investigating the behavior of preprocessed DIFB-SEG samples on impact fragmentation tests, conducted in an ex situ apparatus. Tests were carried out for impact velocities in the range 17–45 m/s. Results were discussed considering both the impact velocity value and the operating conditions under which the sample was preprocessed in the fluidized bed.     

Tocotrienol-rich fraction from palm oil affects gene expression in tumors resulting from MCF-7 cell inoculation in athymic mice

It has recently been shown that tocotrienols are the components of vitamin E responsible for inhibiting the growth of human breast cancer cells in vitro, through an estrogen-independent mechanism. Although tocotrienols act on cell proliferation in a dose-dependent manner and can induce programmed cell death, no specific gene regulation has yet been identified. To investigate the molecular basis of the effect of tocotrienols, we injected MCF-7 breast cancer cells into athymic nude mice. Mice were fed orally with 1 mg/d of tocotrienol-rich fraction (TRF) for 20 wk. At end of the 20 wk, there was a significant delay in the onset, incidence, and size of the tumors in nude mice supplemented with TRF compared with the controls. At autopsy, the tumor tissue was excised and analyzed for gene expression by means of a cDNA array technique. Thirty out of 1176 genes were significantly affected. Ten genes were down-regulated and 20 genes up-regulated with respect to untreated animals, and some genes in particular were involved in regulating the immune system and its function. The expression of the interferon-inducible transmembrane protein-1 gene was significantly up-regulated in tumors excised from TRF-treated animals compared with control mice. Within the group of genes related to the immune system, we also found that the CD59 glycoprotein precursor gene was up-regulated. Among the functional class of intracellular transducers/effectors/modulators, the c-myc gene was significantly down-regulated in tumors by TRF treatment. Our observations indicate that TRF supplementation significantly and specifically affects MCF-7 cell response after tumor formation in vivo and therefore the host immune function. The observed effect on gene expression is possibly exerted independently from the antioxidant activity typical of this family of molecules.     

Synthesis and Antiplasmodial Activity of Novel Chloroquine Analogues with Bulky Basic Side Chains

Chloroquine is commonly used in the treatment and prevention of malaria, but Plasmodium falciparum, the main species responsible for malaria‐related deaths, has developed resistance against this drug. Twenty‐seven novel chloroquine (CQ) analogues characterized by a side chain terminated with a bulky basic head group, i.e., octahydro‐2H‐quinolizine and 1,2,3,4,5,6‐hexahydro‐1,5‐methano‐8H‐pyrido[1,2‐a][1,5]diazocin‐8‐one, were synthesized and tested for activity against D‐10 (CQ‐susceptible) and W‐2 (CQ‐resistant) strains of P. falciparum. Most compounds were found to be active against both strains with nanomolar or sub‐micromolar IC₅₀ values. Eleven compounds were found to be 2.7‐ to 13.4‐fold more potent than CQ against the W‐2 strain; among them, four cytisine derivatives appear to be of particular interest, as they combine high potency with low cytotoxicity against two human cell lines (HMEC‐1 and HepG2) along with easier synthetic accessibility. Replacement of the 4‐NH group with a sulfur bridge maintained antiplasmodial activity at a lower level, but produced an improvement in the resistance factor. These compounds warrant further investigation as potential drugs for use in the fight against malaria.     

Transition Metal‐Free Direct C?H (Hetero)arylation of Heteroarenes: A Sustainable Methodology to Access (Hetero)aryl‐Substituted Heteroarenes

In recent years, environmental and economic reasons have motivated the development of transition metal‐free carbon‐carbon bond forming reactions and some excellent reviews have covered this research area of particular interest for the pharmaceutical industry. However, none of these reviews has been specifically dedicated to summarize and discuss the results achieved in the rapidly growing field of the transition metal‐free direct (hetero)arylation reactions of heteroarenes. This review, which covers the literature from 2008 to 2014, aims to provide a thorough insight into the synthetic and mechanistic aspects of these atom economic and environmentally benign reactions also highlighting their advantages and possible disadvantages compared to conventional methods for the synthesis of arylheteroarenes and biheteroaryls via transition metal‐catalyzed reactions.

     

Mixture design applied for the development of films based on starch,polyvinyl alcohol,and glycerol

Starch and polyvinyl alcohol (PVA) are biodegradable materials with potentiality to replace the conventional polymers in some applications. The aim of this work was to produce biodegradable films of PVA, cassava starch, and glycerol by thermoplastic extrusion using a mixture design to evaluate the effects of each component in the blend properties. Six formulations were prepared using a twin‐screw extruder coupled with a calender. All the materials were visually homogeneous and presented good processability. Mechanical properties were dependent on both the relative humidity conditioning and the formulation; higher relative humidities detracted the mechanical properties, which was associated to plasticizer effect of the water. Furthermore, the mechanical properties were better when higher concentrations of PVA were used, resulting in films with lower opacity, lower water vapor permeability, and higher thermal stability, according to TGA. Biodegradable materials based on starch, PVA, and glycerol have adequate mechanical and processing properties for commercial production. © 2015 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2015 , 132, 42697.     

Gold‐Catalyzed Sequential Amination/Annulation Reactions of 2‐Propynyl‐1,3‐dicarbonyl Compounds

The gold(III)‐catalyzed sequential amination/annulation reaction of 2‐propynyl‐1,3‐dicarbonyl compounds 1 with primary amines 2 produces 1,2,3,5‐substituted pyrroles 4 in moderate to high yields.     

Promising curaua fiber‐reinforced polyester composite for high‐impact ballistic multilayered armor

A typical multilayered armor system (MAS) is composed of a harder front ceramic tile, which is able to erode heavy ammunition, such as the 7.62 mm bullet, followed by a second layer to further reduce the impact energy. Aramid fabric is a common choice for the second layer. In the present work, polyester matrix composites reinforced with 10 to 30 vol% of curaua fibers, despite having much lower strength and stiffness than aramid fabric, displayed similar trauma indentation in a standard clay witness simulating the human body. Impedance matching and scanning electron microscopy analyses suggest effective energy absorption through ceramic fragment capture by curaua composites. Additionally, because of the high cost of aramid fabric, a full MAS with curaua fiber composite is much cheaper than a MAS composed of aramid fabric. Taking into consideration, both the economical and environmental advantages of natural fibers, it is concluded that curaua fiber‐reinforced polyester composite could replace aramid fabric as the second layer in MASs for personal ballistic protection. POLYM. ENG. SCI., 57:947–954, 2017. © 2016 Society of Plastics Engineers     

Identification of Hck Inhibitors As Hits for the Development of Antileukemia and Anti‐HIV Agents

Hematopoietic cell kinase (Hck) is a member of the Src family of non‐receptor protein tyrosine kinases. High levels of Hck are associated with drug resistance in chronic myeloid leukemia. Furthermore, Hck activity has been connected with HIV‐1. Herein, structure‐based drug design efforts were aimed at identifying novel Hck inhibitors. First, an in‐house library of pyrazolo[3,4‐d]pyrimidine derivatives, which were previously shown to be dual Abl and c‐Src inhibitors, was analyzed by docking studies within the ATP binding site of Hck to select the best candidates to be tested in a cell‐free assay. Next, the same computational protocol was applied to screen a database of commercially available compounds. As a result, most of the selected compounds were found active against Hck, with K_i values ranging from 0.14 to 18.4 μM , confirming the suitability of the computational approach adopted. Furthermore, selected compounds showed an interesting antiproliferative activity profile against the human leukemia cell line KU‐812, and one compound was found to block HIV‐1 replication at sub‐toxic concentrations.