圆二色光谱及其在药物研究方面的应用

对圆二色光谱技术在手性化合物分析中的应用进展进行综述,简单介绍了圆二色光谱的原理和特点,着重阐述了圆二色光谱在药物研究领域中的应用,初步探讨了HPLC-CD联用在该领域的应用.     

The Effects of Formulation on Imidacloprid Dissipation in Grapes and Vine Leaves and on Required Pre-Harvest Intervals under Lebanese Climatic Conditions

In this study, imidacloprid, a systemic insecticide, currently having a specified European Commission MRL value for vine leaves (2 mg kg⁻¹), was applied on a Lebanese vineyard under different commercial formulations: as a soluble liquid (SL) and water dispersible granules (WDG). In Lebanon, many commercial formulations of imidacloprid are subject to the same critical good agricultural practice (cGAP). It was, therefore, important to verify the variability in dissipation patterns according to matrix nature and formulation type. Random samplings of grapes and vine leaves were performed starting at 2 days until 18 days after treatment. Residue extractions were performed according to the QuEChERS method and the analytical determination using liquid chromatography coupled to tandem mass spectrometry (LC-MS-MS). The SL formulation yielded significantly higher initial deposit than the WDG formulation on grapes and vine leaves. The formulation type did not significantly affect the dissipation rates; the estimated half-lives in grapes and vine leaves were 0.5 days for all imidacloprid formulations. No pre-harvest intervals were necessary on grapes. PHIs of 3.7 days for the SL formulation and 2.8 days for the WDG formulation were estimated on vine leaves. The results showed that the type of formulation and the morphological and physiological characteristics of the matrix had an effect on the initial deposits, and thus residue levels, but not on the dissipation patterns.     

Vorticity-streamfunction formulation of unsteady incompressible flow past a cylinder: Sensitivity of the computed flow field to the location of the outflow boundary

The influence of the location of the outflow computational boundary on the unsteady incompressible flow past a circular cylinder at Reynolds number 100 is examined. The vorticity-streamfunction formulation of the Navier-Stokes equations is used in all computations. Two types of outflow boundary conditions are subjected to a series of tests in which the domain length is gradually reduced. The traction-free condition performs well in most cases and allows the outflow boundary to be located as close as 6.5 cylinder diameters from the body. The other boundary condition type is not as forgiving, but has the advantage of being simpler to implement and can still provide reasonably accurate solutions. It is also observed that both condition types can influence the flow field strongly and globally when the boundary is brought closer than 2.5 diameters from the body. In such cases the temporal periodicity of the solution is lost.     

脱氢枞胺及其衍生物的研究与应用进展

脱氢枞胺及其衍生物在手性拆分、金属离子浮选、表面活性、杀菌、医药、染料等领域有着重要的用途。本文对脱氢枞胺的制备、脱氢枞胺成盐衍生物以及脱氢枞胺成键衍生物的研究与应用进展进行了综述,并对脱氢枞胺及其衍生物的研究及应用前景进行了展望。     

A Novel Docetaxel-Biotin Chemical Conjugate for Prostate Cancer Treatment

A novel conjugate of docetaxel and biotin (designated as IDD-1010) was designed and chemically synthesized via an ester linkage at position 2’ carbon in docetaxel. The synthesized pure IDD-1010 exhibits a potent anti-cancer activity in in vitro and in vivo studies. At 10 nM, IDD-1010 has induced increased apoptosis and mitotic arrest of PC3-Luc prostate cancer cells, causing aneuploidy and cell death at higher concentrations. Toxicology studies indicate that the maximal tolerated dose (MTD) of IDD-1010 is 150 mg/kg in mice; equivalent to about 12.2 mg/kg of body weight, or to about an 850 mg dose for a patient weighing 70 kg. The MTD-treated mice exhibited weight gain similar to that of the control group, with no gross pathological signs at 14 days post-dosing. At a lower dose, IDD-1010 treatment did not lead to any significant weight loss in mice, although decreased the tumor volume stemming from injecting cancer cells into the dorsal loop of mouse prostate, and it was found to be more potent than Paclitaxel (reference drug). Similarly, IDD-1010 treatment significantly reduced tumor weight and thereby increased the percentage of mice survival as compared to reference drug-treated and control groups. To summarize, the described experiments using IDD-1010, as compared to the reference drug, strongly suggest a potential treatment utility with a wider therapeutic window for prostate cancer. Henceforth, clinical research on such a novel drug candidate would be greatly worthwhile.     

Meshless acoustic analysis using a weakly singular Burton-Miller boundary integral formulation

The Burton-Miller boundary integral formulation is solved by a complex variable boundary element-free method (CVBEFM) for the boundary-only meshless analysis of acoustic problems with arbitrary wavenumbers. To regularize both strongly singular and hypersingular integrals and to avoid the computation of the solid angle and its normal derivative, a weakly singular Burton-Miller formulation is derived by considering the normal derivative of the solid angle and adopting the singularity subtraction procedures. To facilitate the implementation of the CVBEFM and the approximation of gradients of the boundary variables, a stabilized complex variable moving least-square approximation is selected in the meshless discretization procedure. The results show the accuracy and efficiency of the present CVBEFM and reveal that the method can produce satisfactory results for all wavenumbers, even for extremely large wavenumbers such as k = 10 000.     

Inhibition of Metalloproteinase Activity by Chinese Formulations Used to Treat Inflammatory Diseases

Introduction Matrixmetalloproteinases(MMPs)areaclassof zinc requiringextracellularendopeptidasesthatcanto getherdegradeallcomponentsoftheextracellularma trixandbasementmembranes[1—3].Theyplayimpor tantrolesinconnectivetissueremodeling,occurringin normalb…     

水下对转螺旋桨流致辐射噪声机理与预报方法*

水下对转螺旋桨流致辐射噪声的预报对于水下目标的特征提取和分类识别具有重要意义。由桨叶的旋转引起的湍流场是水下对转螺旋桨流致辐射噪声的源场。分述了水下对转螺旋桨湍流边界层脉动、旋转干涉效应和空化效应引发的水动力噪声机制和研究进展,比较了目前工程应用中的3种对转螺旋桨流致辐射噪声预报方法的特点。在分析对转螺旋桨流致辐射噪声数值预报难点的基础上,综述了对转螺旋桨流致辐射噪声计算方法的研究进展,指出间接数值模拟方法是工程中进行对转螺旋桨流致辐射噪声预报的有效方法。     

Electrochemical Behaviour and Rapid Determination of L‐Dopa at Electrochemically Pretreated Screen Printed Carbon Electrode

A simple and rapid voltammetric method based on a disposable electrochemically pretreated screen‐printed carbon electrode is proposed for the determination of L ‐dopa. Under optimum differential pulse voltammetry conditions a limit of detection of 3.6×10^?7 M for L ‐dopa was obtained. The method was successfully applied to the determination of L ‐dopa in a commercial pharmaceutical formulation.     

Development of a competitive ELISA for the quantification of F5 conjugate in HER2-targeted STEALTH immunoliposome doxorubicin in plasma samples

HER2 (human epidermal growth factor receptor 2, erbB2, or neu) is overexpressed by a large number of tumor types and has been identified as an important target for cancer therapy. F5 is a single-chain human antibody fragment that recognizes HER2 receptor and is covalently conjugated to PEGylated lipid to form F5 conjugate (F5CG) in the product HER2 targeted STEALTH immunoliposome doxorubicin. Here we described the method development of a competitive enzyme-linked immunosorbent assay (ELISA) for the determination of total concentration of F5 conjugate in plasma samples. The method involved the biotinylation of F5CG, detergent treatment of plasma sample to solubilize F5CG into monomeric form, and competitive ELISA for solubilized F5CG competitively binding to anti-F5CG antibody with biotinylated F5CG for the determination of total F5CG in plasma. The detection range of this method was from 0.2 ng/mL to 125 ng/mL for F5CG in plasma. The lower limit of quantification (LLOQ) was 0.2 ng/mL. This method was established and used for the measurement of F5CG concentration to provide information about F5CG circulation after the administration of immunoliposome in preclinical studies.