Synthesis of the kappa-agonist CJ-15,161 via a palladium-catalyzed cross-coupling reaction

Syntheses of CJ-15,161 (1) involving intermolecular N-arylation of an appropriately functionalized diamine, obtained from the precursor alpha-amino acids or, more conveniently, from the corresponding 1,2-amino alcohols via 1,2,3-oxathiazolidine-2,2-dioxide 22, are reported.     

Vector-Valued Tail Value-at-Risk and Capital Allocation

Enterprise risk management, actuarial science or finance are practice areas in which risk measures are important to evaluate for heterogeneous classes of homogeneous risks. We present new measures: bivariate lower and upper orthant Tail Value-at-Risk. They are based on bivariate lower and upper orthant Value-at-Risk, introduced in Cossette et al. (Insurance: Math Econ 50(2):247–256, 2012). Many properties and applications are derived. Notably, they are shown to be positive homogeneous, invariant under translation and subadditive in distribution. Capital allocation criteria are suggested. Moreover, results on the sum of random pairs are presented, allowing to use a more accurate model for dependent classes of homogeneous risks.     

On the complexation of Trolox with methyl-β-cyclodextrin: characterization, molecular modelling and photostabilizing properties

Exposure to UV radiations could reduce the efficiency of some antioxidants like Trolox (6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid), a water-soluble vitamin E analogue largely employed in cosmetic products. Accordingly, in this paper we examined the possibility of increasing the stability of Trolox towards UVB irradiation by its complexation with methyl-β-cyclodextrin. Formation of the inclusion complex was confirmed by solubility diagrams, differential scanning calorimetry (DSC), and diffusion study through hydrophilic membrane. The stability constants and docking results suggested that the complexation phenomenon was related to the pH of the medium. The photodegradation studies were carried out in different topical formulations (gel, O/W emulsion, and W/O/W emulsion) containing Trolox free or complexed with methyl-β-cyclodextrin. Results showed that in all the cases Trolox degraded following pseudo-zero order kinetics. Moreover, the host molecule increased Trolox photostability also in the presence of TiO₂, a physical sunscreen well-known as photocatalyzer.     

Optical attenuation at the 1,550-nm wavelength in a reflective mode using electrochromic ruthenium complex film

Thin films of a dinuclear ruthenium complex have been prepared on a reflective electrode. The complex is redox-active in the near infrared spectral region. Electrochromic switching between the two oxidation states of the complex film gave 80% optical contrast at the telecommunication wavelength of 1,550 nm, which translates to an intrinsic attenuation of 17.5 dB/μm of the active material. Chronoamperometric study showed excellent stability over extended switching cycles as well as retaining high attenuation with a 5-s stepping time.     

Elliptically polarized Terahertz emission through four-wave mixing in a two-color filament in air

We diagnosed the polarization characteristics of Terahertz emission from a two-color femtosecond laser filament when the polarizations of ω and 2ω beams are orthogonal. We discovered that the THz pulse is elliptically polarized. The generation mechanism could be through four-wave optical rectification inside the filament zone where the inversion symmetry of air is broken.     

Two-dimensional database of a Burkitt lymphoma cell line (DG 75) proteins: protein pattern changes following treatment with 5'-azycytidine.

Hypermethylation is an important mechanism for repression of tumor gene suppressor in cancer. The drug 5'-azacytidine (AZC) has been used as demethylating agent to induce the expression of previously silencing genes. In the present work, we attempted to determine, using proteomics, the changes in protein expression profiles following a treatment of an Epstein Barr virus (EBV)-negative Burkitt lymphoma (BL) cell line DG 75. The effects of the treatment in terms of cell viability and growth were first examined. The following observations were made: AZC treatment led to (i) a decrease in cell growth with an arrest of the cell at G0/G1 phase of the cell cycle, (ii) the expression of p16, a tumor-suppressor gene whose expression was dependent on its promoter demethylation. Proteomic study evidenced that AZC treatment affected protein expression in two different ways. Twenty-one polypeptides were down-expressed, while 14 showed an increased expression. Some of the upregulated proteins appeared related to the energy metabolism, to organization of cytoskeletal structures, and to cell viability and protein synthesis. We also established a reference map for proteins in DG 75 cell line, comprising 74 different polypeptides corresponding to 67 proteins. This map will be accessible via Internet as a resource for proteome analyses of B-cells. Taken together, the results presented here highlight new insights into lymphoma cell gene regulations following a treatment of lymphoma cells with AZC and illustrate a use of proteomics to evidence the direct and indirect effects of a drug and the pathways it possibly regulates.     

Tailoring the resonances of nonlinear mechanical systems

Nonlinear Dynamics - The objective of this paper is the realization of a desired frequency–amplitude dependence of a specific vibration mode of a nonlinear system. To this end, we introduce...