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 Electron-withdrawn groups as well as long unsaturated chains were hazardous to the activity.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.     

Thermokinetic parameters analysis for 1,1-bis-(tert-butylperoxy)-3,3,5-trimethylcyclohexane at isothermal conditions for safety assessment

The rapid development of the petrochemical industry of Taiwan over the past four decades has resulted in a booming economy in Taiwan that drives derived industries to develop progressively. However, it has also caused many runaway reaction accidents, such as toxic gas release, fire, and explosion. It is crucial to eliminate those potential hazard factors which can induce consequent runaway reaction accidents during the life span of the manufacturing process. In response to this crucial issue, we performed a thermokinetic parameter analysis for 1,1-bis-(tert-butylperoxy)-3,3,5-trimethylcyclohexane at isothermal conditions to conduct a thermal safety assessment of chemical materials. The five isothermal temperatures, 90, 100, 110, 120, 130, and 140 °C, measured by DSC, were adopted in this study to calculate process safety parameters, including TMR_ad, T _NR, and SADT, which can be employed in process safety parameters for the manufacturing process. A novel, green kinetic approach accompanied with non-isothermal DSC results is used to derive thermokinetic parameters in safety protocol in this study.     

Redox Chemistry of a Hydroxyphenyl‐Substituted Borane

Chemical reduction of a hydroxyphenyl‐substituted borane triggers a sequential electron‐ and intramolecular hydrogen‐atom‐transfer process to afford a hydridoborate phenoxide dianion. On the other hand, hydrogen‐atom abstraction of the borane leads to the isolation of a neutral borylated phenoxyl radical, which can be transformed to the corresponding benzoquinone borataalkene derivative by reduction with cobaltocene.     

D3R grand challenge 4: blind prediction of protein–ligand poses,affinity rankings,and relative binding free energies

Journal of Computer-Aided Molecular Design - The Drug Design Data Resource (D3R) aims to identify best practice methods for computer aided drug design through blinded ligand pose prediction and...     

Hermetic Seal of Organic Light Emitting Diode with Glass Frit

The components of OLED encapsulation with hermetic sealing and a 1026-day lifetime were measured by PXI-1033. The optimal characteristics were obtained when the thickness of the TPBi layer was 20 nm. This OLED obtained a maximum luminance (Lmax) of 25,849 cd/m² at a current density of 1242 mA/cm², an external quantum efficiency (EQE) of 2.28%, a current efficiency (CE) of 7.20 cd/A, and a power efficiency (PE) of 5.28 lm/W. The efficiency was enhanced by Lmax 17.2%/EQE 0.89%/CE 42.1%/PE 41.9%. The CIE coordinates of 0.32, 0.54 were all green OLED elements with wavelengths of 532 nm. The shear strain and leakage test gave results of 16 kgf and 8.92 × 10⁻⁹ mbar/s, respectively. The reliability test showed that the standard of MIL-STD-883 was obtained.     

Analyses of preservatives by capillary electrochromatography using methacrylate ester-based monolithic columns

Five common food preservatives were analyzed by capillary electrochromatography, utilizing a methacrylate ester-based monolithic capillary as separation column. In order to optimize the separation of these preservatives, the effects of the pore size of the polymeric stationary phase, the pH and composition of the mobile phase on separation were examined. For all analytes, it was found that an increase in pore size caused a reduction in retention time. However, separation performances were greatly improved in monolithic columns with smaller pore sizes. The pH of the mobile phase had little influence on separation resolution, but a dramatic effect on the amount of sample that was needed to be electrokinetically injected into the monolithic column. In addition, the retention behaviors of these analytes were strongly influenced by the level of acetonitrile in the mobile phase. An optimal separation of the five preservatives was obtained within 7.0 min with a pH 3.0 mobile phase composed of phosphate buffer and acetonitrile 35:65 v/v. Finally, preservatives in real commercial products, including cold syrup, lotion, wine, and soy sauces, were successfully determined by the methacrylate ester-based polymeric monolithic column under this optimized condition.     

A Microbial Sensor Based on Direct Electron Transfer at Shewanella Sp. Drop‐Coated Screen‐Printed Carbon Electrodes

Aerobically grown Shewanella sp. bacterial suspension drop‐coated on a disposable screen‐printed carbon electrode was found to possess electroactivity without the aid of redox mediator. Cyclic voltammetric studies revealed the characteristics of a mixed diffusion adsorption‐controlled electrochemical process for direct electron transfer at the bacteria‐modified electrode. Both FE‐SEM and ATR FT‐IR experiments were carried out to investigate the surface characteristics. The electroanalytical applicability was further demonstrated for electrocatalytic reduction of arsenite, hydrogen peroxide and nitrite. Low cost and very simple manufacturing procedure allow for the proposed bacterial sensor to be applied as disposable devices.     

Charmed andϕmeson decay constants from 2+1-flavor lattice QCD

On a lattice with 2+1-flavor dynamical domain-wall fermions at the physical pion mass,we calculate the decay constants of D_s^* , D^* ,and φ .The lattice size is 48^3×96 ,which corresponds to a spatial extension of -5.5 fm,with a lattice spacing of a\approx a≈0.114 fm.For the valence light,strange,and charm quarks,we use overlap fermions at several mass points close to their physical values.Our results at the physical point are f_D=213(5) MeV, f_Ds=249(7) MeV, f_D^*=234(6) MeV, f_Ds^*=274(7) MeV,and f_Ds=241(9) MeV.The couplings of D^* and D_s^* to the tensor current( f_V^T )can be derived from ratios f_D^*^T/f_D^*=0.91(4) and f_Ds^*^T/f_Ds^*=0.92(4) ,respectively,which are the first lattice quantum chromodynamics(QCD)results.We also obtain ratios f_D^*/f_D=1.10(3) and f_Ds^*/f_Ds=1.10(4) ,which reflect the size of heavy quark symmetry breaking in charmed mesons.Ratios f_Ds/f_D=1.16(3) and f_Ds^*/f_D^*=1.17(3) can be taken as a measure of SU(3)flavor symmetry breaking.     

Simultaneous measurement of curvature and temperature based on PCF-based interferometer and fiber Bragg grating

A sensor head consisting of a photonic crystal fiber (PCF)-based Mach-Zehnder interferometer (MZI) and a fiber Bragg grating (FBG) is proposed and experimentally demonstrated for simultaneous measurement of curvature and temperature. The MZI fabricated by splicing a short length of PCF between two single-mode fibers with the air-hole structure that completely collapsed near the splicing points, is sensitive to fiber bending and surrounding temperature, while the FBG is only sensitive to the later. Simultaneous measurement of curvature and temperature is therefore obtained. Sensitivities of 4.06 nm/m^− 1 and 6.30 pm/°C are achieved experimentally for curvature and temperature, respectively. And the corresponding resolutions are 5.2 × 10^− 4 m^− 1 and 1.25 °C for curvature and temperature, respectively, based on the wavelength measurement resolution of 10 pm.