Pharmacokinetic Study of ZS-1, a Targeted Peptide to NCI-H1299, in Rats Following Intravenous Administration

To investigate the pharmacokinetics of ZS-1 following intravenous injection in rats, ZS-1 was administered at doses of 20, 30 and 45 mg kg^?1, respectively. Blood samples were collected at 0.5, 3, 8, 12, 15, 20, 30, 40 and 45 min. ZS-1 in rat plasma was measured by LC. The limit of detection (LOD) was 0.02 μg mL^?1. The relative standard deviation (RSD) of intra- and inter-day precisions were <10%, and the accuracy of intra- and inter-day were >94%. The mean extraction recovery of ZS-1 was 86.1%. After intravenous injection at doses of 20, 30 and 45 mg kg^?1, the concentration–time curves of ZS-1 fitted well to one compartment model. Area under the concentration–time curves (AUC) increased with dose. Clearance rates (CL) and elimination half-lives (T _1/2) had no significant difference between different dose groups (P > 0.05). ZS-1 was stable in plasma after at 25 °C for 2, 4, 6 h, after three freeze–thaw cycles, after ?20 °C for a month, and after ?80 °C for 3 months. The accuracy of ZS-1 was between 96.8 and 106.9%. The results indicated there was no significant degradation. These data indicated that the method for analysis of ZS-1 was reliable and the pharmacokinetic data could guide dosing regimens to be tested in future clinical pharmacokinetic study.     

Development of a Biomimetic Enzyme‐linked Immunosorbent Assay Method for the Determination of Methimazole in Urine Sample

A fast and direct competitive biomimetic enzyme‐linked immunosorbent assay (BELISA) method was developed for the determination of methimazole (MMZ) in urine sample based on a molecularly imprinted film as an artificial antibody. This is the first example to monitor methimazole with a direct competitive biomimetic enzyme‐linked immunosorbent assay (BELISA) method. The imprinted film was directly synthesized on the well surface of MaxiSorp polystyrene 96‐well plate and characterized. The results showed that it exhibited an antibody‐like binding ability, rapid adsorption speed, high stability, which was particularly advantageous and suitable for BELISA development. The BELISA method established in this paper had a higher selectivity for MMZ than for the structurally related compounds and the IC₅₀ (calculated as the concentration giving 50% inhibition of color development) and the detection limit values under optimized experimental conditions were 70 ± 4 μg L^‐1 and 0.9 ± 0.04 μg L^‐1, respectively. The method was applied to the determination of MMZ in spiked urine sample with excellent recoveries ranging from 90% to 95%, and the imprinted film was able to be reused for 20 times without loss of sensitivity. The results obtained by BELISA correlated well with that obtained by the high performance liquid chromatography (HPLC) method.     

Simultaneous Determination of Four Sudan Dyes in Egg Yolks by Molecularly Imprinted SPE Coupled with LC-UV Detection

A highly selective molecularly imprinted solid-phase extraction (MISPE) combined with liquid chromatography-ultraviolet detection was developed for the simultaneous isolation and determination of four Sudan dyes (I, II, III and IV) in egg-yolk products. The imprinted microspheres synthesized by suspension polymerization using phenylamine?Cnaphthol as mimic template show high selectivity and affinity to the four kinds of Sudan dyes and were successfully applied as selective sorbents of solid-phase extraction for the simultaneous determination of the four Sudans from egg-yolk samples. Good linearity was obtained in a range of 0.062?C10 ??g g^?1 and the average recoveries of the four Sudans at three spiked levels ranged from 94.1 to 102.5% with the relative standard deviations less than 5.8%. The developed extraction protocol eliminated the effect of template leakage on quantitative analysis and could be applied for the determination of Sudans in complicated food samples.     

Micellar nucleation differential microemulsion polymerization

Polymer nanoparticles within the range of 2–5 nm with a solid content of more than 13 wt.% and a narrow molecular weight polydispersity (Mw/Mn ∼ 1.1) were for the first time prepared using a micellar nucleation differential microemulsion polymerization system emulsified by sodium dodecyl sulfate (SDS), with SDS/monomer (methyl methacrylate) and SDS/H₂O weight ratios of up to 1:16 and 1:100, respectively. It was found that for benzoyl peroxide (BPO), micellar nucleation is more favorable for the synthesis of smaller polymer nanoparticles than ammonium persulfate (APS) which gives rise to homogeneous nucleation and 2,2′-azobisisobutyronitrile (AIBN) which involves partially heterogeneous nucleation. In the polymerization process, there exists a critical stability concentration (CSC) of SDS, above which the size of the nanoparticles is to be minimized and stabilized. With an increase in the monomer addition rate, the polymerization system changes from a microemulsion system to an emulsion system. A mechanism was proposed to describe the micellar nucleation process of differential microemulsion polymerization. This study may contribute to the development of fine polymer nanoparticles for drug delivery systems.     

Layer-by-layer self-assembly polytungstogermanate multilayer films and their photocatalytic properties under sunlight irradiation

Seven different types of thio- and/or amine-modified cellulose resin materials were synthesized and their mercury (II) ion adsorption properties determined. All seven resins showed good mercury (II) adsorption capability in the more neutral pH regions. However, the o-benzenedithiol- and o-aminothiophenol-modified cellulosic resins were found to be very effective in removing mercury (II) ions from strongly acidic media. For example, 93.5-100% mercury (II) ion recoveries from very acid aqueous solutions (nitric acid concentration ranged from 0.1 to 2.0 mol/L) were obtained using the o-benzenedithiol-modified resin while recoveries ranged from ca. 50% to 60% for the o-aminothiophenol-modified resin. An adsorption capacity of 23 mg (as Hg atoms) per gram of resin was observed for the o-benzenedithiol-modified cellulose in the presence of 1.0 mol/L nitric acid. This same resin shows very good selectivity for mercury (II) as only ruthenium (II) also somewhat adsorbed onto it out of 14 other metal ions studied (Ag(+), Al(3+), As(3+), Co(2+), Cd(2+), Cr(3+), Cu(2+), Fe(3+), Mn(2+), Ni(2+), Pt(2+), Pb(2+), Ru(2+), and Zn(2+)).     

Multimetallic synergic sedation of a labile sodium atrane: synthesis and characterization of a tetranuclear sodium atrane cation complex

A series of sodium and aluminum atrane complexes of Na(3)L(THF)(5) (1), [AlLMe][Na(4)L(THF)(6)] (2), AlL(THF) (3), AlNaLMe(THF)(2) (4), and AlNaLOBn(THF)(2) (5), wherein L = tris(2-oxy-4,6-di-tert-butyl-benzyl)amine, were synthesized and characterized by NMR, X-ray crystallography, and elemental analysis. The trinuclear sodium atrane complex of Na(3)L(THF)(5) (1) is labile at room temperature; however, the tetranuclear sodium atrane cation in complex 2 can be stabilized by a multimetallic synergetic effect due to a firm interaction ring of -[Na-O-benzene](3)-. Complex 2 is also the first example of a sodatrane and alumatrane ion-paired complex in which both the cationic and anionic moieties contain an atrane ligand.     

Donor/acceptor complex of triphenylene and trinitrotoluene on Au(111): a scanning tunneling microscopy study

The co-adsorption of trinitrotoluene (TNT), a typical π-electron acceptor, and triphenylene (TP), a typical π-electron donor, on a Au(111) surface was investigated by in situ Electrochemical Scanning Tunneling Microscopy (ECSTM). DFT calculations proved that parallelly stacked and well-overlapped TP and TNT molecules can form Donor-Acceptor dyads through intermolecular π-π charge transfer, which agree well with the experimental results in the present work.     

Copper-mediated methylthiolation of aryl halides with DMSO

A copper-mediated methylthiolation of aryl halides with the widely available DMSO is described. The procedure tolerates a series of functional groups such as methoxy, nitro, chloro, fluoro, trifluoromethyl, formyl and methoxycarbonyl groups. Thus, it represents a simple and facile methylthiolation procedure.     

Nearly monodispersed core-shell structural Fe3O4@DFUR-LDH submicro particles for magnetically controlled drug delivery and release

Nearly monodispersed magnetic Fe(3)O(4)@DFUR-LDH submicro particles containing the anticancer agent DFUR were prepared via a coprecipitation-calcination-reconstruction strategy of LDH materials over the surface of Fe(3)O(4) particles, and present well-defined core-shell structure, strong magnetization and obvious magnetically controlled drug delivery and release properties.     

Enantioselective intramolecular Rauhut-Currier reaction catalyzed by chiral phosphinothiourea

Chiral organophosphine-catalyzed enantioselective Rauhut-Currier reaction has been disclosed for the first time. With L-valine-derived phosphinothiourea, the intramolecular Rauhut-Currier reaction of bis(enones) was achieved in good yields (up to 99%) with excellent enantioselectivities (up to 99.4% ee).