Naproxen Inhibits UVB‐induced Basal Cell and Squamous Cell Carcinoma Development in Ptch1+/−/SKH‐1 Hairless Mice

Naproxen possesses anti‐proliferative and pro‐apoptotic effects besides its known anti‐inflammatory functions. Here, we demonstrate the anticancer effects of naproxen against UVB‐induced basal cell carcinoma (BCCs) and squamous cell carcinoma (SCCs) in a highly susceptible murine model of UVB carcinogenesis. Naproxen significantly inhibited UVB‐induced BCCs and SCCs in this model. Tumor number and volume were significantly decreased (P < 0.005 and P < 0.05, respectively). Inhibition in UVB‐induced SCCs and BCCs was 77% and 86%, respectively, which was associated with reduced PCNA and cyclin D1 and increased apoptosis. As expected, inflammation‐related iNOS, COX‐2 and nuclear NFκBp65 were also diminished by naproxen treatment. Residual tumors excised from naproxen‐treated animal were less invasive and showed reduced expression of epithelial‐mesenchymal transition (EMT) markers N‐cadherin, Vimentin, Snail and Twist with increased expression of E‐cadherin. In BCC and SCC cells, naproxen‐induced apoptosis and activated unfolded protein response (UPR) signaling with increased expression of ATF4, p‐eIF2α and CHOP. Employing iRNA‐based approaches, we found that naproxen‐induced apoptosis was regulated by CHOP as sensitivity of these cutaneous neoplastic cells for apoptosis was significantly diminished by ablating CHOP. In summary, these data show that naproxen is a potent inhibitor of UVB‐induced skin carcinogenesis. ER stress pathway protein CHOP may play an important role in inducing apoptosis in cancer cells.     

“On water” ultrasound-assisted one pot efficient synthesis of functionalized 2-oxo-benzo[1,4]oxazines: First application to the synthesis of anticancer indole alkaloid,Cephalandole A

For the first time, an efficient, simple, synthetic green protocol for the one-pot synthesis of functionalized 2-oxo-benzo[1,4]oxazines 24–29 in water under ultrasound irradiation is presented. As compared to conventional methods, the present protocol avoids traditional chromatography and purification steps and furnished the target molecules in excellent yields (upto 98%) with no side products. The methodology was also demonstrated on gram scale synthesis. Moreover, functionalized 2-oxo-quinoxaline analogues 31–33, another class of bio-active heterocyclic scaffolds, were also prepared using this method. For the first time, this protocol was successfully applied in the synthesis of the anticancer indole alkaloid, Cephalandole A 35.     

Sol-gel synthesis, structural and optical properties of rare earth ions (Sm or Dy) activated Ca3Ga2Si3O12 powder phosphors

Structural, morphological and optical properties of rare earth ions (RE³⁺=Sm³⁺ or Dy³⁺) activated Ca₃Ga₂Si₃O₁₂ (CaGaSi) phosphors synthesized by the sol-gel method are reported. XRD results confirmed the cubic phase structure of RE³⁺:CaGaSi phosphors. From the SEM images of RE³⁺:CaGaSi phosphors, it is observed that the particles are agglomerated. Photoluminescence spectra of Sm³⁺:CaGaSi phosphors have shown bright orange red emission at 598 nm (⁴G_5/2→⁶H_7/2) with an excitation wavelength of λ_exci=401 nm. In the case of Dy³⁺:CaGaSi phosphors bright yellow emission has been observed at 574 nm (⁴F_9/2→ ⁶H_13/2) with λ_exci=451 nm. From the PL spectral results, the rare earth ion concentration of CaGaSi phosphors is optimized.     

Synthesis of nanocrystalline Co-Ni alloys by precursor approach and studies on their magnetic properties

Nanocrystalline Co-Ni alloys with different compositions were prepared by polyol reduction of mixed cobalt nickel hydroxides. The precursors (mixed cobalt nickel hydroxides) were prepared by co-precipitation. Powder X-ray diffraction analysis indicated the formation of fcc phase in the alloys and their crystallite size in the range 17-25 nm. Scanning electron microscopy and transmission electron microscopy studies revealed the morphology of the particles as being close to spherical, and the energy dispersive X-ray analysis showed the stoichiometry of the alloys. The magnetization as a function of field and temperature of the alloys, measured using a superconducting quantum interference device, showed superparamagnetic behavior with negligible coercivity and remanence values.     

A simple isothermal model for homogeneous-heterogeneous reactions in boundary-layer flow. I Equal diffusivities

A simple model for homogeneous-heterogeneous reactions in stagnation-point boundary-layer flow is constructed in which the homogeneous (bulk) reaction is assumed to be given by isothermal cubic autocatalator kinetics and the heterogeneous (surface) reaction by first order kinetics. The possible steady states of this system are analysed in detail in the case when the diffusion coefficients of both reactant and autocatalyst are equal. Hysteresis bifurcations leading to multiple solutions are found. The temporal stability of these steady states is then discussed.     

Synthesis and photophysical studies of siloxane-tethered cyclophanes

Novel siloxane tethered para divinylarene cyclophanes, containing phenyl, biphenyl and naphthalene rings as the aromatic nuclei, were prepared by the hydrolytic condensation of the corresponding bis{[dimethyl(i-propoxy)silyl]vinyl}arenes under basic conditions.The photophysics of the cyclophanes were investigated using UV and fluorescence spectroscopy.     

Zur Strömung viskoser Flüssigkeiten durch gewellte Rohre

Zusammenfassung Die Strömung zäher nicht-newtonscher Flüssigkeiten durch gewellte kreisförmige Rohre unter Wirkung eines axialen Druckgefälles wurde theoretisch und experimentell untersucht. Das besondere Interesse galt dabei der durch die Wellung veränderten Druck-Durchsatz-Charakteristik. Die theoretischen Betrachtungen beziehen sich auf den Grenzfall hinreichend langer Wellen, wo sich der Querschnitt des Flüssigkeitsfadens in Strömungsrichtung nur langsam ändert und sowohl die Trägheit als auch die Elastizität der Flüssigkeit eine untergeordnete Rolle spielen. In dieser Näherung konnte der Durchsatz in Abhängigkeit vom Druckgefälle und den nichtlinearen Fließeigenschaften der Flüssigkeit für beliebige Wellenamplituden analytisch bestimmt werden. Die theoretischen Ergebnisse sind in Einklang mit experimentellen Befunden.

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The flow of a non-Newtonian fluid driven by an axial pressure gradient through a corrugated pipe of circular cross-section is analysed theoretically and realized experimentally. Particular attention is directed toward the pressure-discharge characteristics of the pipe which change due to the corrugation. A theory is developed for the limiting case of corrugations with long wave-length, where the cross-section of the pipe varies gradually in the flow direction and the effects of inertia and elasticity of the fluid are of minor importance. Within such a long-wave approximation the flow rate, in dependence on the applied pressure drop and on the non-linear viscous properties of the fluid, is determined analytically for arbitrary wave amplitudes. The theoretical results are in agreement with experimental findings.

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Acid Catalyzed Efficient Syntheses of Aryl‐5H‐dibenzo[b,i]xanthene‐5,7,12,14‐(13H)‐tetraones and 3,3‐(Arylmethylene)bis(2‐hydroxynaphthalene‐1,4‐diones) and In Vitro Evaluation of their Antioxidant Activity

A simple and efficient synthesis of aryl‐5H‐dibenzo[b,i]xanthene‐5,7,12,14‐(13H)‐tetraones and 3,3‐(arylmethylene)bis(2‐hydroxynaphthalene‐1,4‐diones) by the condensation of aromatic aldehydes and 2‐hydroxy‐1,4‐naphthoquinone under extremely mild conditions using catalytic amount of H₂SO₄ or in the presence of acidic ionic liquid 1‐butyl‐3‐methylimidazolium hydrogen sulphate, which could be recycled, has been reported. The radical scavenging capacity of the synthesized compounds has been examined towards the stable free radical 2,2‐diphenyl‐1‐picrylhydrazyl (DPPH), and the compounds 2 were found to scavenge DPPH free radical efficiently.     

An efficient synthesis of dexlansoprazole employing asymmetric oxidation strategy

An alternative and scalable synthesis of dexlansoprazole ((R)-(+)-1); the (R)-enantiomer of Lansoprazole with an enantiomeric excess of >99.8% is presented.     

Efficient complexation of pyrrole-bridged dizinc(II) bisporphyrin with fluorescent probe pyrene: synthesis, structure, and photoinduced singlet-singlet energy transfer

A diethylpyrrole‐bridged dizinc(II) bisporphyrin (Zn₂DEP) is reported that encapsulates fluorescent probe pyrene molecules through strong π–π interactions, which can relay information about the chemical environment in the interior of the host–guest supramolecular assembly. X‐ray structures of both Zn₂DEP and the encapsulated pyrene complex are reported, which provides a rare opportunity to investigate the structural changes upon guest binding. A comparative structural analysis demonstrated the exceptional ability of this bisporphyrin platform to open its binding pocket for pyrene encapsulation by a vertical displacement of more than 2.45 Å, although both Zn₂DEP and the pyrene complex have nearly parallel porphyrin ring orientations. The ¹H NMR spectrum of the encapsulated pyrene complex in solution shows the upfield shifts of the pyrene protons due to a strong ring current effect, which demonstrates the retention of the solid‐state structure in solution. To further assess the extent to which pyrene guests remain encapsulated in solution, a known fluorescence quencher, dimethylaniline, was added to the host–guest assembly, which shows no exciplex formation for days in nonpolar solvents. Thus, the assembly also retained the structural integrity in solution for a long time. The association constant (K_asso) for such a complexation process in solution was observed to be 1.78×10⁵ M ^?2 for 1:2 binding. Steady‐state fluorescence and lifetime studies indicate significant photoinduced singlet–singlet energy transformation from the excited state of pyrene to zinc bisporphyrin.