Studies of Coumarin Derivatives for Constitutive Androstane Receptor (CAR) Activation

Constitutive androstane receptor (CAR) activation has found to ameliorate diabetes in animal models. However, no CAR agonists are available clinically. Therefore, a safe and effective CAR activator would be an alternative option. In this study, sixty courmarin derivatives either synthesized or purified from Artemisia capillaris were screened for CAR activation activity. Chemical modifications were on position 5,6,7,8 with mono-, di-, tri-, or tetra-substitutions. Among all the compounds subjected for in vitro CAR activation screening, 6,7-diprenoxycoumarin was the most effective and was selected for further preclinical studies. Chemical modification on the 6 position and unsaturated chains were generally beneficial. Electron-withdrawn groups as well as long unsaturated chains were hazardous to the activity. Mechanism of action studies showed that CAR activation of 6,7-diprenoxycoumarin might be through the inhibition of EGFR signaling and upregulating PP2Ac methylation. To sum up, modification mimicking natural occurring coumarins shed light on CAR studies and the established screening system provides a rapid method for the discovery and development of CAR activators. In addition, one CAR activator, scoparone, did showed anti-diabetes effect in db/db mice without elevation of insulin levels.     

Synthesis of a benzoxazine with precisely two phenolic OH linkages and the properties of its high‐performance copolymers

A phenolic OH‐containing benzoxazine ( F‐ap ), which cannot be directly synthesized from the condensation of bisphenol F, aminophenol, and formaldehyde by traditional procedures, has been successfully prepared in our alternative synthetic approach. F‐ap was prepared by three steps including (a) condensation of 4‐aminophenol and 5,5'‐methylenebis(2‐hydroxybenzaldehyde) (1) , (b) reduction of the resulting imine linkage by sodium borohydride, and (c) ring closure condensation by formaldehyde. The key starting material, (1) , was prepared from 2‐hydroxybenzaldehyde and s‐trioxane in the presence of sulfuric acid. F‐ap is structurally similar to bis(3,4‐dihydro‐2H‐3‐phenyl‐1,3‐benzoxazinyl)methane ( F‐a, a commercial benzoxazine based on bisphenol F/aniline/formaldehyde) except for two phenolic OHs. The phenolic OHs can provide reaction sites with epoxy and 1,1'‐(methylenedi‐p‐phenylene)bismaleimide (BMI). The structure–property relationships between the thermosets of F‐ap /epoxy, F‐a /epoxy, F‐ap /BMI, and F‐a /BMI were discussed. Experimental data showed that thermosets based on F‐ap /epoxy and F‐ap /BMI provided much better thermal properties than those based on F‐a /epoxy and F‐a /BMI. © 2013 Wiley Periodicals, Inc. J. Polym. Sci., Part A: Polym. Chem. 2013, 51, 2686–2694     

Quantum-inspired space search algorithm (QSSA) for global numerical optimization

This work presents the evolutionary quantum-inspired space search algorithm (QSSA) for solving numerical optimization problems. In the proposed algorithm, the feasible solution space is decomposed into regions in terms of quantum representation. As the search progresses from one generation to the next, the quantum bits evolve gradually to increase the probability of selecting the regions that render good fitness values. Through the inherent probabilistic mechanism, the QSSA initially behaves as a global search algorithm and gradually evolves into a local search algorithm, yielding a good balance between exploration and exploitation. To prevent a premature convergence and to speed up the overall search speed, an overlapping strategy is also proposed. The QSSA is applied to a series of numerical optimization problems. The experiments show that the results obtained by the QSSA are quite competitive compared to those obtained using state-of-the-art IPOP-CMA-ES and QEA.     

Continuous-time bilinear system identification using single experiment with multiple pulses

A novel method is presented for the identification of a continuous-time bilinear system from the input?Coutput data generated by a single experiment with multiple pulses. In contrast to the conventional approach utilizing multiple experiments, the current work documents the advantage of using a single experiment and sets up a procedure to obtain bilinear system models. The special pulse inputs employed by earlier research can be avoided and accurate identification of the continuous-time system model is possible by performing a single experiment incorporating a class of control input sequences combining pulses with free-decay response. The algorithm presented herein is more attractive in practice for the identification of bilinear systems. Numerical examples presented demonstrate the methodology developed in the paper.     

Temperature dependence of excitonic emission in cubic CdSe thin film

A detailed photoluminescence investigation of the thermal redshift and broadening of the excitonic line of cubic CdSe film grown by molecular beam epitaxy is presented. Free excitonic emission from the cubic CdSe film was observed at low temperature. Temperature-dependent measurement was performed to obtain material parameters related to exciton-phonon interaction by fitting the experimental data to the phenomenological model. The relative contribution of both acoustic and optical phonon to the band gap shrinkage and exciton linewidth broadening are discussed. Exciton binding energy of 16±1.5 meV was determined from the Arrhenius analysis.     

Immiscibility,upper critical solution temperature,and miscibility in blends of poly(vinyl ether)s with polyacrylics: Effects of pendant groups

Various phase behavior of blends of poly(vinyl ether)s with homologous acrylic polymers (polymethacrylates or polyacrylates) were examined using differential scanning calorimetry, optical microscopy (OM), and Fourier‐transformed infrared spectroscopy. Effects of varying the pendant groups of either of constituent polymers on the phase behavior of the blends were analyzed. A series of interestingly different phase behavior in the blends has been revealed in that as the pendant group in the acrylic polymer series gets longer, polymethacrylate/poly(vinyl methyl ether) (PVME) blends exhibit immiscibility, upper critical solution temperature (UCST), and miscibility, respectively. This study found that the true phase behavior of poly(propyl methacrylate)/PVME [and poly(isopropyl methacrylate)/PVME)] blend systems, though immiscible at ambient, actually displayed a rare UCST upon heating to higher temperatures. Similarly, as the methyl pendant group in PVE is lengthened to ethyl (i.e., PVME replaced by PVEE), phase behavior of its blends with series of polymethacrylates or polyacrylates changes correspondingly. Analyses and quantitative comparisons on four series of blends of PVE/acrylic polymer were performed to thoroughly understand the effects of pendant groups in either polyethers (PVE's) or acrylic polymers on the phase behavior of the blends of these two constituents. © 2007 Wiley Periodicals, Inc. J Polym Sci Part B: Polym Phys 45: 1521–1534, 2007     

Resistance-in-series analysis in cross-flow ultrafiltration of fermentation broths of Bacillus subtilis culture

Quantitative analysis of various resistances that lead to flux decline during cross-flow ultrafiltration (UF) of the fermentation broth of Bacillus subtilis ATCC (American Type Culture Collection) 21332 culture was studied. Polyethersulfone membrane with a molecular weight cut-off (MWCO) of 100 kDa was used. Prior to cross-flow UF, the broth was treated by acid precipitation (pH 4.0) and centrifugation, and the precipitate was re-dissolved in NaOH solution. Experiments were performed at a feed pH of 7.0, a feed surfactin concentration of 1.48 g L⁻¹, and a cross-flow velocity of 0.32 m s⁻¹ but at different transmembrane pressures (ΔP, 20–100 kPa). The resistance-in-series model was used to analyze the flux behavior, which involves the resistances of membrane itself and cake as well as those due to adsorption and solute concentration polarization. It was shown that the resistance due to solute concentration polarization and of membrane dominated under the conditions examined. The resistances due to cake formation and solute adsorption were comparable, and their sum contributed below 20% of the overall resistance.