Alstolactines A–C,novel monoterpenoid indole alkaloids from Alstonia scholaris

Three novel ring-fused monoterpenoid indole alkaloids, alstolactines A–C (1–3), were isolated from the long-term stored leaves of Alstonia scholaris. Their structures were identified on the basis of extensive spectroscopic data and X-ray diffractions. Moreover, the absolute configurations of these related structures were indicated by the crystal X-ray diffractions (Mo Kα) of 1a, a chlorinated derivative of 1.     

Electrophile-driven copper-catalyzed one-pot synthesis of 3-halogen quinoline derivatives

A convenient and regioselective one-pot synthesis of 3-chloride or 3-bromide quinoline derivatives was achieved through a Grignard addition reaction by alkynyl Grignard regent to o-trifluoroacetyl aniline and a Cu(II)-catalyzed cyclization–halogenation tandem reaction with aqueous HCl or HBr as electrophilic reagent.     

Study of Interactions and Association Thermodynamics Between Sudan Red and Sodium Dodecyl Sulfate in Microemulsions

The absorption spectrum of Sudan red III (SR) in oil solutions and a series of O/W microemulsion with surfactant sodium dodecyl sulfate (SDS) has been determined by the UV-Vis spectrophotometer. We found that an association interaction existed between the stain SR and anionic surfactant SDS in water/mixed oil/SDS microemulsions. By measuring the absorbance of Sudan red in a series of microemulsions which has different R values and using the appropriate association models to analyze the experimental data, we obtain the association constants of SR and SDS, and the values of thermodynamics functions of associationΔ_r G _m has also been calculated from the association constants.     

The synthesis of a new cardiac sympathetic nerve imaging agent N-[11C]CH3-dopamine and biodistribution study

In this study, we synthesized and characterized N-[¹¹C]methyl-dopamine ([¹¹C]MDA) for cardiac sympathetic nerve imaging. [¹¹C]MDA was synthesized by direct N-methylation of dopamine with [¹¹C]methyl iodide and purified by semi-preparation reverse high pressure liquid chromatography (HPLC). The total synthesis time was 45 min including HPLC purification. The radiochemical yields of [¹¹C]MDA was 20 ± 3 %, without decay correction. The radiochemical purity was >98 % and the specific activity was about 50 GBq/mmol. The biological properties of [¹¹C]MDA were evaluated by biodistribution study in normal mice. PET imaging was performed in healthy Chinese mini-swines. Biodistribution study showed that [¹¹C]MDA had high myocardium uptake. PET/CT imaging showed [¹¹C]MDA had clear and symmetrical myocardium uptake, which was blocked obviously by injecting imipramine hydrochloride. [¹¹C]MDA would be a promising candidate of radiotracer for cardiac sympathetic nervous system imaging.     

Environmental gamma background measurements in China Jinping Underground Laboratory

To determine the environmental gamma background levels which affects rare events experiments, we measured in situ gamma spectrum at four locations in the China Jinping Underground Laboratory. The integral background count rates (40–2,700 keV) varied from 3.76 to 74.1 cps. The average count rate of the measurements inside the CJPL was 73.4 cps. The spectrometer was calibrated with a ¹⁵²Eu point source and Monte Carlo simulation to obtain the activity conversion factors for the rock and the air, respectively. The rocks that surrounded the CJPL was characterized by very low activity concentrations of ²³⁸U (3.69–4.21 Bq kg^?1), ²³²Th (0.52–0.64 Bq kg^?1) and ⁴⁰K (4.28 Bq kg^?1).     

Design and preliminary assessment of 99mTc-labeled ultrasmall superparamagnetic iron oxide-conjugated bevacizumab for single photon emission computed tomography/magnetic resonance imaging of hepatocellular carcinoma

Hepatocellular carcinoma (HCC) has a very high incidence and mortality. Early diagnosis and timely treatments are therefore required to improve the quality of life and survival rate of HCC patients. Here, we developed a vascular endothelial growth factor (VEGF)-based multimodality imaging agent for single photon emission computed tomography (SPECT), computed tomography (CT) and magnetic resonance imaging (MRI) and used it to assess HCC mice and explore the combinative value of CT/MRI-based morphological imaging and SPECT functional imaging. HCC targeting with ¹²⁵I-labeled bevacizumab monoclonal antibody (mAb) was examined using SPECT/CT in HepG2 tumor-bearing mice after intravenous mAb injection. Based on this, an integrated, bimodal, VEGF-targeted, ultrasmall superparamagnetic iron oxide (USPIO)-conjugated ^99mTc-labeled bevacizumab mAb was synthesized to increase tumor penetration and accumulations. The in vivo pharmacokinetics and HepG2 tumor targeting were explored through in vivo planar imaging and SPECT/CT using a mouse model of HepG2 liver cancer. The specificity of the radiolabeled nanoparticles for HepG2 HCC was verified using in vitro immunohistochemistry and Prussian blue staining. With diethylenetriamine pentaacetic acid as a bifunctional chelating agent, USPIO-bevacizumab achieved a ^99mTc labeling efficiency of >90 %. The in vivo imaging results also exhibited the targeting of USPIO on HepG2 HCC. The specificity of these results was confirmed using in vitro immunohistochemistry and Prussian blue staining. Our preliminary findings showed the potential of USPIO as an imaging agent for the SPECT/MRI of HepG2 HCC.     

The sequestration of U(VI) on functional β-cyclodextrin-attapulgite nanorods

Eight elastomeric composites (NRU, GR1–GR4, NRBG08–NRBG24) containing mixtures of different proportions of heavy metal additives (Bi, W, Gd and Sb) have been synthesized and examined as protective shields. The NRU sample was a pure rubber matrix and served as a reference sample for heavy metal modified composites. Experimental procedure used for evaluation of the composite shields and their attenuation properties was based on the utilization of HPGe spectrometry and analysis of X-ray fluorescence radiation intensity of the heavy metal additives in the following energy ranges for: Sb (20–35 keV), Gd (35–55 keV), W (55–70 keV) and Bi (70–90 keV). The main contributor to the induced X-ray fluorescence radiation within the shield is Bi additive and the intensity of the X-ray radiation generated within the energy range of 70–90 keV strongly depends on its concentration. It was found that decreasing concentration of the Bi fraction from 0.35 (GR samples) to 0.15 (NRBG samples) results in significant lowering Bi X-ray fluorescence radiation within the 70–90 keV energy range. Secondary effect of decreasing Bi concentration was efficient diminishing excitation processes for lower Z heavy metal additives (W, Gd and Sb, GR vs. NRBG samples). As the final quality parameter of the shielding properties for the examined elastomers, dose reduction factor (DRF) coefficients were calculated for each shield. It was found, that the best shielding properties are observed for composites with lower Bi concentration (0.15 vs. 0.35 Bi mass fraction) with only slight further improvement of their parameters (DRF) with increasing of Gd concentration (Gd mass fraction 0.08, 0.16 and 0.24). The most efficient dose reduction composite was found to be NRBG24 elastomer with DRF value 0.47 (53 % dose reduction) for ca. 2 mm and 0.44 g/cm² layer thickness.     

Li改性MnO_2及LiMn_2O_4催化NH_3-SCR反应性能研究

采用高温固相反应法、Pechini合成方法和柠檬酸配位法,制备了系列锂锰复合氧化物LiMn2O4催化剂,应用于NH3-SCR反应,并与固相反应法合成的MnO2进行了比较。采用N2吸附-脱附、扫描电镜、X射线衍射、H2程序升温还原、NH3程序升温脱附、NO程序升温脱附和X射线光电子能谱对LiMn2O4催化剂进行表征。结果表明,引入Li有利于提高锰基催化剂的SCR活性和抗硫性。Pechini法制备LiMn2O4的NO转化率可在130~260℃达到90%以上;固相反应法制备LiMn2O4的NO转化率大于90%的温度为90~310℃;MnO2的温度窗口则仅为140~280℃。与MnO2相比,引入Li可形成LiMn2O4结构,因此,催化剂中更多的锰离子保持在相对较低的价态Mn3+,并调整表面活性氧含量;同时,Li的存在调变了LiMn2O4表面的酸位,从而减少高温下MnO2表面容易发生的NH3非选择性氧化,改善其催化NH3-SCR反应的温度窗口,也增强了抗硫性。     

新型双环新烟碱类似物的合成及其生物活性

设计合成了六个新型双环新烟碱类似物,通过1H NMR,13C NMR,高分辨质谱和单晶结构对目标化合物的结构进行了表征.初步的生物活性测试表明:在500 mg?L-1浓度下,目标化合物6a,6c~6f对豆蚜(Aphis craccivora)具有很好的杀虫活性.通过分子对接比较并解释了目标化合物6a和吡虫啉的活性和作用模式的差异,其结果表明目标化合物6a的吡啶环和受体残基色氨酸147的芳香环侧链具有?-?堆积作用,与吡虫啉的作用方式存在一定差异.     

Construction of a portable sample preparation device with a magnetic poly(methacrylic acid‐co‐ethylene dimethacrylate) monolith as the extraction medium and its application in the enrichment of UV filters in water samples

A portable sample preparation device with a magnetic polymer monolith as the extraction medium was constructed. The monolith was synthesized by polymerizing methacrylic acid and ethylene dimethacrylate around a cylindrical magnet. In this way, the monolith with a magnetic core could be readily attached to the extraction device by magnetism. The constructed device was evaluated for the enrichment of UV filters in water samples, followed by high‐performance liquid chromatographic analysis. The extraction efficiency for the targets was satisfactory with no matrix interference. Good linearities were obtained for the UV filters with the correlation coefficients >0.9986. The limits of detection and quantification for the UV filters were 0.3–0.8 and 1.0–2.4 ng/mL, respectively. The recoveries of the UV filters from the spiked water samples at the concentration of 100 ng/mL were 95.3–101.7%, with relative standard deviations <10%. Accordingly, the proposed portable device was demonstrated to be suitable for on‐site simultaneous sampling, purification, and preconcentration within a single step.