Development of a Glassy Carbon Electrode Modified with Graphene/Au Nanoparticles for Determination of Acetaminophen in Pharmaceutical Preparation

Russian Journal of Electrochemistry - A graphene/Au nanoparticles composite modified glassy carbon electrode (GR/AuNPs/GCE) was developed. Electrochemical behavior of acetaminophen (ACOP) at this...     

Screening and identification of Caulis Sinomenii bioactive ingredients with dual‐target NF‐κB inhibition and β2‐AR agonizing activities

Caulis Sinomenii (CS) is a valuable traditional medicine in China. Its extract can act as an anti‐inflammatory agent and a vascular smooth muscle relaxant. However, the underlying mechanisms remain unknown. In this study, we developed a simple dual‐target method based on ultra‐performance liquid chromatography/quadrupole time‐of‐flight mass spectrometry combined with a dual‐target bioactive screening assay for anti‐inflammatory and antispasmodic activities to characterize the chemical structure of various bioactive compounds of CS rapidly. Seven potential NF‐κB inhibitors were identified, including laudanosoline‐1‐O‐xylopyranose, 6‐O‐methyl‐laudanosoline‐1‐O‐glucopyranoside, menisperine, sinomenine, laurifoline, magnoflorine and norsinoacutin. Furthermore, IL‐6 and IL‐8 assays confirmed the anti‐inflammatory effects of these potential NF‐κB inhibitors, in which laudanosoline‐1‐O‐d ‐xylopyranose and menisperine were revealed as novel NF‐κB inhibitors. Among the seven identified alkaloids, three potential β₂‐adrenergic receptor agonists, including sinomenine, magnoflorine and laurifoline, were characterized using a luciferase reporter system to measure for the activity of β₂‐adrenergic receptor agonists. Finally, sinomenine, magnoflorine and laurifoline were identified not only as potential NF‐κB inhibitors but also as potential β₂‐adrenegic receptor agonists, which is the first time this has been reported. Molecular dynamic simulation and docking results suggest that the three dual‐bioactive constituents could not only inhibit Pseudomonas aeruginosa PAK strain‐induced inflammatory responses via a negative regulation of the Braf protein that participates in MAPK signaling pathway but also activate the β₂‐adrenegic receptor. These results suggest that CS extract has dual signaling activities with potential clinical application as a novel drug for asthma.     

3-O-Sulfation of Heparan Sulfate Enhances Tau Interaction and Cellular Uptake

Prion-like transcellular spreading of tau in Alzheimer's Disease (AD) is mediated by tau binding to cell surface heparan sulfate (HS). However, the structural determinants for tau–HS interaction are not well understood. Microarray and SPR assays of structurally defined HS oligosaccharides show that a rare 3-O-sulfation (3-O-S) of HS significantly enhances tau binding. In Hs3st1^−/− (HS 3-O-sulfotransferase-1 knockout) cells, reduced 3-O-S levels of HS diminished both cell surface binding and internalization of tau. In a cell culture, the addition of a 3-O-S HS 12-mer reduced both tau cell surface binding and cellular uptake. NMR titrations mapped 3-O-S binding sites to the microtubule binding repeat 2 (R2) and proline-rich region 2 (PRR2) of tau. Tau is only the seventh protein currently known to recognize HS 3-O-sulfation. Our work demonstrates that this rare 3-O-sulfation enhances tau–HS binding and likely the transcellular spread of tau, providing a novel target for disease-modifying treatment of AD and other tauopathies.     

Correlations between microstructure of α‐row nuclei and polymorphism of shear‐induced iPP/carbon fiber cylindrite

Herein, we reported the formation mechanism of hybrid crystalline (cylindrite) in isotactic polypropylene (iPP)/carbon fiber (CF) via pulling a CF within the iPP melt. The α‐row nuclei layer closely attached to the surface of CF acts as a self‐nucleation site, rather than a heterogeneous nucleation one, to grow cylindrites. As a result, the polymorphic feature of iPP/CF cylindrite is significantly influenced by the microstructure of α‐row nuclei. With decreasing crystallization temperature (T_c), the polymorphic cylindrite changes from pure α‐form to mixed α‐/β‐form and to β‐rich form. The main characteristics of this change include: (a) the outlines of α‐row nuclei layer correspond to wave‐like, saw‐like, and straight lines; (b) the orientation level of iPP molecules in the α‐row nuclei layer become higher; (c) the α‐lamellae rearrange from loose to compact; and (d) the distance between the growth sites of β‐sectors and the surface of CF is evidently longer than in the case of α‐sectors. Moreover, this study provides a guideline for developing the interfacial enhanced iPP/CF composites through manipulation of polymorphic structure in cylindrites. © 2019 Wiley Periodicals, Inc. J. Polym. Sci., Part B: Polym. Phys. 2019 , 57, 368–377     

Screening potential antagonists of epidermal growth factor receptor from Marsdenia tenacissima via cell membrane chromatography model assisted by HPLC–ESI–IT–TOF–MS

Marsdenia tenacissima, or Tongguanteng in Chinese, is a traditional Chinese herb and has a broad application in clinical practice for its pharmacological effects of treating asthma, pneumonia, tonsillitis, pharyngitis tumors, etc. However, few studies have reported the screening of the active components of this medicine for tumor therapy. In this work, a two‐dimensional analytical system was developed to screen antagonists of epidermal growth factor receptor (EGFR) from M. tenacissima. A fraction was retained on the EGFR cell membrane chromatography (CMC) column, separated and identified as tenacissoside G (TG), tenacissoside H (TH) and tenacissoside I (TI) by two‐dimensional HPLC–IT–TOF–MS. Molecular docking and 3‐(4,5‐dimethyl‐2‐thiazolyl)‐2,5‐diphenyl‐2‐H‐tetrazolium bromide (MTT) assay were carried out to assess the activity of TS (including TG, TH and TI). Molecular docking results showed that the binding mode of TS on EGFR is similar to that of gefitinib. The MTT assay demonstrated that gefitinib and TS (especially TI) could inhibit the growth of EGFR highly expressed cell lines in a dose‐dependent manner in the range of 5–50 μmol/L. In conclusion, the two‐dimensional EGFR/CMC–HPLC–IT–TOF–MS system could be a useful approach in drug discovery from traditional Chinese medicines for searching for potential antitumor candidates.     

Chiral aminocyclopentene-based cycloaddition strategies to bicyclic [3.3.0] rings

Two cycloaddition methods were applied to chiral protected aminocyclopentenes 2 and 9 and provided novel bicyclic products 3 and 4 in good yields. The explanation for the observed stereochemistry was based on the sterically encumbered β-face forcing the cycloadditions to occur on the α-face of the cyclopentene ring. The stereochemistry of 4 was confirmed by X-ray of the fumarate salt 10 and showed the trans-relationship between the newly formed ring and the chiral –NHBoc group.     

High performance of N,P co-doped metal-free carbon catalyst derived from ionic liquid for oxygen reduction reaction

Journal of Solid State Electrochemistry - One-pot strategy to fabricate N, P co-doping carbon was developed based on the functional ionic liquid (IL) as the N, P, and C precursors. The IL featuring...     

Eigenspace-based minimum variance beamformer combined with Wiener postfilter for medical ultrasound imaging

In this paper, a new beamformer which combines the eigenspace-based minimum variance (ESBMV) beamformer with the Wiener postfilter is proposed for medical ultrasound imaging. The primary goal of this work is to further improve the medical ultrasound imaging quality on the basis of the ESBMV beamformer. In this method, we optimize the ESBMV weights with a Wiener postfilter. With the optimization of the Wiener postfilter, the output power of the new beamformer becomes closer to the actual signal power at the imaging point than the ESBMV beamformer. Different from the ordinary Wiener postfilter, the output signal and noise power needed in calculating the Wiener postfilter are estimated respectively by the orthogonal signal subspace and noise subspace constructed from the eigenstructure of the sample covariance matrix.We demonstrate the performance of the new beamformer when resolving point scatterers and cyst phantom using both simulated data and experimental data and compare it with the delay-and-sum (DAS), the minimum variance (MV) and the ESBMV beamformer. We use the full width at half maximum (FWHM) and the peak-side-lobe level (PSL) to quantify the performance of imaging resolution and the contrast ratio (CR) to quantify the performance of imaging contrast. The FWHM of the new beamformer is only 15%, 50% and 50% of those of the DAS, MV and ESBMV beamformer, while the PSL is 127.2 dB, 115 dB and 60 dB lower. What is more, an improvement of 239.8%, 232.5% and 32.9% in CR using simulated data and an improvement of 814%, 1410.7% and 86.7% in CR using experimental data are achieved compared to the DAS, MV and ESBMV beamformer respectively. In addition, the effect of the sound speed error is investigated by artificially overestimating the speed used in calculating the propagation delay and the results show that the new beamformer provides better robustness against the sound speed errors. Therefore, the proposed beamformer offers a better performance than the DAS, MV and ESBMV beamformer, showing its potential in medical ultrasound imaging.     

Polymerizable Molecular Silsesquioxane Cage Armored Hybrid Microcapsules with In Situ Shell Functionalization

We prepared core–shell polymer–silsesquioxane hybrid microcapsules from cage‐like methacryloxypropyl silsesquioxanes (CMSQs) and styrene (St). The presence of CMSQ can moderately reduce the interfacial tension between St and water and help to emulsify the monomer prior to polymerization. Dynamic light scattering (DLS) and TEM analysis demonstrated that uniform core–shell latex particles were achieved. The polymer latex particles were subsequently transformed into well‐defined hollow nanospheres by removing the polystyrene (PS) core with 1:1 ethanol/cyclohexane. High‐resolution TEM and nitrogen adsorption–desorption analysis showed that the final nanospheres possessed hollow cavities and had porous shells; the pore size was approximately 2–3 nm. The nanospheres exhibited large surface areas (up to 486 m² g^?1) and preferential adsorption, and they demonstrated the highest reported methylene blue adsorption capacity (95.1 mg g^?1). Moreover, the uniform distribution of the methacryloyl moiety on the hollow nanospheres endowed them with more potential properties. These results could provide a new benchmark for preparing hollow microspheres by a facile one‐step template‐free method for various applications.