Concurrent detection of cabozantinib as an anticancer agent and its major metabolites in human serum using fluorescence-coupled micellar liquid chromatography

A novel, highly sensitive, simple, and rapid strategy was designed and developed for simultaneous determination of cabozantinib (CBZ) as an anticancer agent and its main metabolites including monohydroxy sulfate (EXEL-1646), N-oxide (EXEL-5162(, amide cleavage product (EXEL-5366), and 6-desmethyl amide cleavage product sulfate) EXEL-1644). Measurements were done through a micellar liquid chromatography (MLC) method coupled with fluorescence detection. The high-performance liquid chromatography (HPLC) was performed using a Kinetex C18 100 Å column as well as acetonitrile, cetyltrimethylammonium bromide (CTAB; 0.2 mol.L^?1), and tris buffer (pH 8.5) solutions as the mobile phase at a 40:50:10 (v/v) ratio. The method’s linearity (20 to 700 ng.mL^?1), limit of detection (LOD; 2.11 to 3.69 ng.mL^?1), limit of quantification (LOQ; 20 to 30 ng.mL^?1), intra- and inter-day precisions (RSD < 4.00%), selectivity, recovery, and robustness were fully evaluated. According to the obtained results, the developed method can be used for simple and rapid (~35 min) quantification of CBZ as an anticancer drug and its major metabolites in human serum samples with high sensitivity and low cost.     

Elucidating the Binding Mode between Heparin and Inflammatory Cytokines by Molecular Modeling

Heparan sulfate (HS) interacts with a broad spectrum of inflammatory cytokines, thereby modulating their biological activities. It is believed that there is a structural-functional correlation between each protein and sugar sequences in the HS polysaccharides, however, the information in this regard is limited. In this study, we compared the binding of four inflammatory cytokines (CCL8, IL-1beta, IL-2 and IL-6) to immobilized heparin by an SPR analysis. To define the molecular base of the binding, we used a heparin pentasaccharide as representative structure to dock into the 3D-molecular structure of the cytokines. The results show a discrepancy in K_D values obtained by SPR analysis and theoretical calculation, pointing to the importance to apply more than one method when describing affinity between proteins and HS. By cluster analysis of the complex formed between the pentasaccharide and cytokines, we have identified several groups in heparin forming strong hydrogen bonds with all four cytokines, which is a significant finding. This molecular and conformational information should be valuable for rational design of HS/heparin-mimetics to interfere cytokine-HS interactions.     

Phase‐Junction Electrocatalysts towards Enhanced Hydrogen Evolution Reaction in Alkaline Media

To ensure sustainable hydrogen production by water electrolysis, robust, earth‐abundant, and high‐efficient electrocatalysts are required. Constructing a hybrid system could lead to further improvement in electrocatalytic activity. Interface engineering in composite catalysts is thus critical to determine the performance, and the phase‐junction interface should improve the catalytic activity. Here, we show that nickel diphosphide phase junction (c‐NiP₂/m‐NiP₂) is an effective electrocatalyst for hydrogen production in alkaline media. The overpotential (at 10 mA cm^?2) for NiP₂‐650 (c/m) in alkaline media could be significantly reduced by 26 % and 96 % compared with c‐NiP₂ and m‐NiP₂, respectively. The enhancement of catalytic activity should be attributed to the strong water dissociation ability and the rearrangement of electrons around the phase junction, which markedly improved the Volmer step and benefited the reduction process of adsorbed protons.     

Encapsulation of Phosphomolybdate Within Metal–Organic Frameworks with Dual Enzyme-like Activities for Colorimetric Detection of H2O2 and Ascorbic acid

Developing artificial enzyme mimetics for the detection of small biomolecules are a current research interest because natural enzymes bear some serious disadvantages, such as their catalytic activity can be easily inhibited and they can be digested by proteases. Herein, a heteropoly acids (HPA) encapsulating metal–organic framework (MOF) with metal-carbene structure, [Cu₁₀(H₃trz)₄(Htrz)₄][PMo₁₂VO₄₁] (PMA-MOF) as bifunctional enzyme-mimetic catalyst for colorimetric detection of hydrogen peroxide (H₂O₂) and ascorbic acid (AA) was designed and synthesized. Thanks to the good stability and the synergistic effect of PMA and MOF, PMA-MOF exhibits the lower limit of detection (0.222 μM towards H₂O₂ and 0.0046 μM to AA), and the smaller Km value (0.0138 mM for H₂O₂ and 0.136 mM for o-phenylenediamine) compared to most reported MOF- and HPA-based enzyme-mimetic catalyst, to the best our knowledge.

     

Thermal behaviors and kinetic analysis of two natural kaolinite samples selected from Qingshuihe region in Inner Mongolia in China

Journal of Thermal Analysis and Calorimetry - The thermal characteristic behaviors of two kaolinite samples selected from Qingshuihe region in Inner Mongolia in China were studied through...     

Two New Aristolochic Acid Analogues from the Roots of Aristolochia contorta with Significant Cytotoxic Activity

Twelve compounds, including two new aristolochic acid analogues with a formyloxy moiety (9–10) and 10 known aristolochic acid derivates (1–8 and 11–12), were obtained from the roots of Aristolochia contorta. Their structures were elucidated using extensive spectroscopic methods. Their cytotoxic activity in human proximal tubular cells HK-2 was evaluated by the MTT method, which has been widely used to assess cell viability. Among these molecules, compounds 3 and 9 were found to be more cytotoxic. Furthermore, molecular modeling was used to evaluate, for the first time, the interactions of compounds 3 and 9 with the target protein organic anionic transporter 1 (OAT1) that plays a key role in mediating aristolochic acid nephropathy. Structure–activity relationships are briefly discussed.     

The Effects of CO2 Additional on Flame Characteristics in the CH4/N2/O2 Counterflow Diffusion Flame

The effects (chemical, thermal, transport, and radiative) of CO₂ added to the fuel side and oxidizer side on the flame temperature and the position of the flame front in a one-dimensional laminar counterflow diffusion flame of methane/N₂/O₂ were studied. Overall CO₂ resulted in a decrease in flame temperature whether on the fuel side or on the oxidizer side, with the negative effect being more obvious on the latter side. The prominent effects of CO₂ on the flame temperature were derived from its thermal properties on the fuel side and its radiative properties on the oxidizer side. The results also highlighted the differences in the four effects of CO₂ on the position of the flame front on different sides. In addition, an analysis of OH and H radicals and the heat release rate of the main reactions illustrated how CO₂ affects the flame temperature.     

Formation and Structures of the μ4-Oxygen-Bridged High-Nuclearity Lead(II) Clusters from a Lead Propane-2-thiolate Complex

Journal of Cluster Science - Interaction of [Pb(SiPr)2]n with 1.5 equiv. of AgNO3 in DMF under aerobic conditions at room temperature gave a cationic lead-centered thiolate cluster...     

A Novel Method for the Detection of Trace Gases Based on Photo-Acoustic Spectroscopy

We study quartz tuning fork (QTF) characteristics using a 532 nm semiconductor laser with a power of 39 mW and calculate QTF vibrations caused by thermal noise and disturbance of the air using the equipartition theorem; the vibration value is about 1.152 Pm. The signal-to-noise ratio and QTF resonance amplitude acquired experimentally are 104.56 and 214.75 Pm, respectively. In addition, we develop a new photo-acoustic spectroscopic system for detection of trace acetylene using a CW diode laser source with distributed feedback operating near 1,532 nm, measure the absorption spectrum of acetylene employing this system, and show that the method elaborated is more sensitive than photoelectric detectors that provides new directions for research in photo-acoustic spectroscopy.