Pinkment: a synthetic platform for the development of fluorescent probes for diagnostic and theranostic applications

Reaction-based fluorescent-probes have proven successful for the visualisation of biological species in various cellular processes. Unfortunately, in order to tailor the design of a fluorescent probe to a specific application (i.e. organelle targeting, material and theranostic applications) often requires extensive synthetic efforts and the synthetic screening of a range of fluorophores to match the required synthetic needs. In this work, we have identified Pinkment-OH as a unique “plug-and-play” synthetic platform that can be used to develop a range of ONOO⁻ responsive fluorescent probes for a variety of applications. These include theranostic-based applications and potential material-based/bioconjugation applications. The as prepared probes displayed an excellent sensitivity and selectivity for ONOO⁻ over other ROS. In vitro studies using HeLa cells and RAW 264.7 macrophages demonstrated their ability to detect exogenously and endogenously produced ONOO⁻. Evaluation in an LPS-induced inflammation mouse model illustrated the ability to monitor ONOO⁻ production in acute inflammation. Lastly, theranostic-based probes enabled the simultaneous evaluation of indomethacin-based therapeutic effects combined with the visualisation of an inflammation biomarker in RAW 264.7 cells.

Pinkment, a resorufin based ONOO⁻ selective and sensitive ‘plug and play’ fluorescence-based platform for in vitro and in vivo use, enables facile functionalisation for various imaging and theranostic applications.     

Studies on the properties of ionic liquid EMIInCl4

This paper reports that an ionic liquid (IL) has been prepared by directly mixing InCl₃ and 1-methyl-3-ethylimidazolium chloride (EMIC) with molar ratio 1/1 under dry argon atmosphere. The densities, and surface tension of the pure IL were determined at temperature range of 293.15 to 343.15 ± 0.1 K. The volumetric properties and the properties of surface for ionic liquid based on group III were discussed by Glasser's theory and Yang's interstice model.     

Studies on the thermodynamics of solvent extraction of indium (III) with HDEHMTPCA

The equilibrium molalities In³⁺ in {In₂(SO₄)₃ + Na₂SO₄ + HDEHMTPCA + n-C₈H₁₈ + water} were measured at ionic strength from (0.1 to 2.0) mol · kg⁻¹ containing Na₂SO₄ as supporting electrolyte in aqueous phase and at constant molality extractant at temperatures from (278.15 to 303.15) K in organic phase. The standard extraction constants K⁰ at various temperatures were obtained by methods of extrapolation and polynomial approximation. Thermodynamic quantities for the extraction process were calculated.     

磷钼酸四氢三铵的制备及其交换性能

磷钼酸四氢三铵的制备及其交换性能臧二乐，梁树权（北京农业大学应用化学系北京１０００９４）（中国院学院化学研究所北京）关键词磷钼酸四氢三铵，制备，离子交换性能通式为Ｍ＿ｎＸＹ＿（１２）Ｏ＿（４０）·ｐＨ＿２Ｏ（其中Ｍ为一价阳离子；Ｘ为Ｐ、Ａｓ、Ｓｉ、Ｇ...     

Zero Current Potentiometry for Measuring the Interface Potential at the Electrode/Solution Interface. Theoretical and Experimental Study

A novel electrochemical approach has been proposed to measure the interface potential at the electrode/solution interface based on reconstructing the three‐electrode system of a potentiostat. In this work, the method was investigated both theoretically and experimentally. Mathematical expressions, describing current? potential characteristics, were derived. Zero current potential E_zcp was defined as the potential at which the current is zero based on linear sweep voltammetry, and was determined from the I? E curve to measure the interface potential. The experimental results obtained with the couples Fe(CN)₆^3?/Fe(CN)₆^4? and Co(NH₃)₆³⁺/Co(NH₃)₆²⁺ as examples agreed well with the theory. The proposed approach exhibits an excellent performance for measuring the interface potential due to the advantages of rapidity, high stability and accuracy.     

Synthesis of Hexamine Ligands by Using Trityl as an N-Blocking Group

The amino-groups of diethylenetriamine were regioselectively protected by trityl groups and then reacted with dihalogenated alkylane to give the terminal N-blocked hexamine derivatives, from which a series of hexamine ligands (5 _a-f) were obtained by removing the trityl groups with 5.0 M HCl solution. Alternatively, the hexamine ligands could be also prepared via amidation and reduction reactions. The synthetic routes described here are mild, efficient and easy to handle.     

Metabolite identification of the antimalarial piperaquine in vivo using liquid chromatography–high‐resolution mass spectrometry in combination with multiple data‐mining tools in tandem

Artemisinin‐based combination therapy is widely used for the treatment of uncomplicated Plasmodium falciparum malaria, and piperaquine (PQ) is one of important partner drugs. The pharmacokinetics of PQ is characterized by a low clearance and a large volume of distribution; however, metabolism of PQ has not been thoroughly investigated. In this work, the metabolite profiling of PQ in human and rat was studied using liquid chromatography tandem high‐resolution LTQ‐Orbitrap mass spectrometry (HRMS). The biological samples were pretreated by solid‐phase extraction. Data processes were carried out using multiple data‐mining techniques in tandem, i.e., isotope pattern filter followed by mass defect filter. A total of six metabolites (M1–M6) were identified for PQ in human (plasma and urine) and rat (plasma, urine and bile). Three reported metabolites were also found in this study, which included N‐oxidation (M1, M2) and carboxylic products (M3). The subsequent N‐oxidation of M3 resulted in a new metabolite M4 detected in urine and bile samples. A new metabolic pathway N‐dealkylation was found for PQ in human and rat, leading to two new metabolites (M5 and M6). This study demonstrated that LC‐HRMSⁿ in combination with multiple data‐mining techniques in tandem can be a valuable analytical strategy for rapid metabolite profiling of drugs. Copyright © 2016 John Wiley & Sons, Ltd.     

Preparation of Fluorine-Containing Polyacrylate Emulsion by a UV-initiated Polymerization

A fluorine-containing polyacrylate emulsion was synthesized by a UV-initiated emulsion polymerization from methyl methacrylate (MMA) and hexafluorobutly methacrylate (HFMA) in the presence of 2-hydroxy-4-(2-hydroxyethoxy)-2-methyl-propiophenone (Irgacure 2959) as a hydrophilic photoinitiator at room temperature. The latex and films were characterized by Fourier transformed infrared (FT-IR) spectrometry, nuclear magnetic resonance (¹H-NMR, ¹⁹F-NMR) spectrometry, transmission electron microscopy (TEM), recycling gel permeation chromatography (GPC), dynamic light scattering (DLS), and contact angle (CA) analysis, respectively. The effects of photoinitiator and emulsifier concentration on the polymerization were discussed. Compared to the corresponding thermal polymerization, UV-initiated polymerization of the MMA/HFMA emulsion could be accomplished at a much higher speed. The polymerization conversion in UV-initiated polymerization reached 95% within 10 min at an emulsifier concentration of 0.6 wt%, photoinitiator concentration of 0.4 wt%, and monomer concentration of 10 wt%.