Euphorbiasteroid Abrogates EGFR and Wnt/β-Catenin Signaling in Non-Small-Cell Lung Cancer Cells to Impart Anticancer Activity

EGFR and Wnt/β-catenin signaling pathways play a prominent role in tumor progression in various human cancers including non-small-cell lung carcinoma (NSCLC). Transactivation and crosstalk between the EGFR and Wnt/β-catenin pathways may contribute to the aggressiveness of cancers. Targeting these oncogenic pathways with small molecules is an attractive approach to counteract various types of cancers. In this study, we demonstrate the effect of euphorbiasteroid (EPBS) on the EGFR and Wnt/β-catenin pathways in NSCLC cells. EPBS induced preferential cytotoxicity toward A549 (wildtype EGFR-expressing) cells over PC-9 (mutant EGFR-expressing) cells. EPBS suppressed the expression of EGFR, Wnt3a, β-catenin, and FZD-1, and the reduction in β-catenin levels was found to be mediated through the activation of GSK-3β. EPBS reduced the phosphorylation of GSK-3β^S9 with a parallel increase in β-TrCP and phosphorylation of GSK-3β^Y216. Lithium chloride treatment increased the phosphorylation of GSK-3β^S9 and nuclear localization of β-catenin, whereas EPBS reverted these effects. Forced expression or depletion of EGFR in NSCLC cells increased or decreased the levels of Wnt3a, β-catenin, and FZD-1, respectively. Overall, EPBS abrogates EGFR and Wnt/β-catenin pathways to impart its anticancer activity in NSCLC cells.     

Role of method of synthesis on the size of flakes,dispersion stability and thermophysical properties of aqua based reduced graphene oxide nanofluids

Journal of Thermal Analysis and Calorimetry - The role of method of synthesis on the size of flakes, dispersion stability and thermophysical properties of aqua based reduced graphene oxide (rGO)...     

Synthesis and biological evaluation of some new class of benzothiazole–pyrazole ligands containing arene ruthenium,rhodium and iridium complexes

Transition Metal Chemistry - Metal complexes 1–9 have been synthesized by reacting the benzothiazole–pyrazole derivative ligands (L1, L2 and L3) with the metal precursors of ruthenium...     

H-β-zeolite catalyzed synthesis of β-bromostyrenes from styrene bromohydrins

Synthesis of β-bromostyrenes from styrene bromohydrins using H-β-zeolite as catalyst under moderate conditions is reported. The catalyst could be regenerated and reused up to three consecutive cycles.     

Synthesis and applications of a novel supramolecular polymer network with multiple H‐bonded melamine pendants and uracil crosslinkers

A conjugated main‐chain copolymer ( PBT ) consisting of bithiazole, dithieno[3,2‐b:2′,3′‐d]pyrroles (DTP), and pendent melamine units was synthesized by Stille polymerization, which can be hydrogen‐bonded (H‐bonded) with proper molar amounts of bi‐functional π‐conjugated crosslinker F (i.e., two uracil motifs covalently attached to a fluorene core through triple bonds symmetrically) to develop a novel supramolecular polymer network ( PBT/F ). The effects of multiple H‐bonds on light harvesting capabilities, HOMO levels, and photovoltaic properties of polymer PBT and H‐bonded polymer network PBT/F are investigated. The formation of supramolecular polymer network ( PBT/F ) between PBT and F was confirmed by FTIR and XRD measurements. Because of the stronger light absorption, lower HOMO level, and higher crystallinity of H‐bonded polymer network PBT/F , the solar cell device containing PBT/F showed better photovoltaic properties than that containing polymer PBT . The preliminary results show that the solar cell device containing 1:1 weight ratio of PBT/F and [6,6]‐phenyl C₇₁ butyric acid methyl ester (PC₇₁BM) offers the best power conversion efficiency (PCE) value of 0.86% with a short‐circuit current density (J_sc) of 4.97 mA/cm², an open circuit voltage (V_oc) of 0.55 V, and a fill factor (FF) of 31.5%. © 2011 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem, 2012     

Click chemistry‐based synthesis of azo polymers for second‐order nonlinear optics

Four linear polymers containing pendant azo moiety were synthesized through click chemistry for second‐order nonlinear optical study. The polymers were found soluble in most of the polar organic solvents such as tetrahydrofuran (THF), chloroform, and dimethyl formamide (DMF). The polymers showed thermal stability up to 300 °C and glass transition temperatures (T_g) in the range of 120–140 °C. The molecular weights (M_w) of these polymers (measured by gel permeation chromatography) were in the range 37,900–55,000 g/mol. The polymers were found to form optically transparent films by solution casting from THF solution. Order parameters were calculated from UV–vis absorption spectra. The morphology changes in the films after poling were characterized by atomic force microscopy. The angular dependence, temperature dependence, and time dependence of second harmonic generation (SHG) intensity were obtained by using 1064 nm Nd:YAG laser. The SHG intensity remained unchanged up to 95 °C. At room temperature, it remained stable up to 8 days after initial drop of about 14%. © 2012 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem, 2012     

Flower-shaped ZnO nanoparticles as an efficient, heterogeneous and reusable catalyst in the synthesis of N-arylhomophthalimides and benzannelated isoquinolinones

A simple and green protocol, developed utilizing an efficient, heterogeneous and recyclable catalyst, i.e. zinc oxide nanoparticles (ZnO NPs)-mediated synthesis of N-arylhomophthalimides and benzannelated isoquinolinones, is reported. The structures of the desired products were characterized by FTIR, ¹H NMR, ¹³C NMR, and HRMS techniques. The ZnO NPs exhibited excellent catalytic activity and the proposed methodology is capable of providing the desired products in good yield and purity.     

Interactions with herring sperm DNA and biological studies of sparfloxacin drug‐based copper(II) compounds

Copper(II) complexes of the type [Cu(SPF)(Lⁿ)Cl] (where SPF is sparfloxacin and Lⁿ = substituted terpyridines) were synthesized and found to have a distorted octahedral geometry. Superoxide dismutase‐like activity of the complexes was measured using a nitroblue tetrazolium/reduced nicotinamide adenine dinucleotide/phenazine methosulfate system and expressed in terms of the concentration of complex which terminates the formation of formazan by 50% (IC₅₀ value), which was found to range from 0.572 to 1.522 µm . Interactions of the complexes with herring sperm DNA were studied by absorption titration, viscosity measurement and gel electrophoresis under physiological conditions. The antimicrobial efficiency of the complexes was tested against five different microorganisms and showed good biological activity. All the complexes showed good cytotoxic activity, with LC₅₀ values ranging from 4.01 to 9.64 µg ml^?1. Copyright © 2012 John Wiley & Sons, Ltd.