Novel radical‐responsive MRI contrast agent based on paramagnetic liposomes

A novel, radical responsive MRI contrast agent based on a gadolinium chelate conjugated to a liposome through a disulfide linker was synthesized, with the aim of pursuing the in vivo mapping of radicals. The liposome was prepared by incorporating a thiol‐activated phospholipid, which was subsequently reacted with a gadolinium chelate containing a free thiol group. The long reorientational motion of the supramolecular adduct endows the paramagnetic agent with a relaxivity significantly higher than that of the free complex. The disulfide bond represents a radical‐sensitive moiety and a large decrease in contrast efficacy (T₁ relaxivity) is shown upon its cleavage. A preliminary assessment of the system was made by means of in vitro gamma‐irradiation and thiol–disulfide bond exchange with dithiothreitol. Both methods showed a clear dose‐dependent decrease in T₁‐relaxivity. Copyright © 2003 John Wiley & Sons, Ltd.     

Three-dimensional aromaticity in deltahedral boranes and carboranes

Methods derived from topology and graph theory indicate that the deltahedral boranes B _n H _n ^2– and the corresponding carboranes C₂B_n–2H _n (6 n 12) may be regarded as three-dimensional delocalized aromatic systems in which surface bonding and core bonding correspond to -bonding and -bonding, respectively, in planar polygonal two-dimensional hydrocarbons CinnH _n ^(n–6)+ (n=5/7). The two extreme types of topologies which may be used to model core bonding in deltahedral boranes and carboranes are the deltahedral (D _n ) topology based on the skeleton of the underlying deltahedron and the complete (K _n ) topology based on the corresponding complete graph. Analyses of the Hoffmann-Lipscomb LCAO extended Hückel computations, the Armstrong—Perkins—Stewart self-consistent molecular orbital computations, and SCF MOab initio GAUSSIAN-82 computations on B₆H₆ ^2– indicate that the approximation of the atomic orbitals by the sum of the molecular orbitals, as is typical in modernab initio computations, leads to significantly weaker apparent core bonding approximated more closely by deltahedral (D _n ) topology than by complete (K _n ) topology.This work was presented at the Workshop The Modern Problems of Heteroorganic Chemistry sponsored by the A. N. Nesmeyanov Institute of Organoelement Compounds of the Russian Academy of Sciences (May 8–13, 1993).Translated fromIzvestiya Akademii Nauk. Seriya Khimicheskaya, No. 8, pp. 1353–1360, August, 1993.     

神光-Ⅱ装置三倍频实验中靶场单元技术的改进

 主要介绍为了满足神光-Ⅱ高功率激光装置三倍频光（351nm，3ω）的物理实验要求，靶场三倍频模拟光源和瞄准监视系统两个主要单元技术的改进，即三倍频模拟光源由基频光（1 053nm，3ω）通过腔外的KTP+BBO晶体倍频获得，再经八路分光系统和主激光耦合；瞄准监视系统由透射式光学系统改进为反射式光学系统，避免原系统存在较大的色差，提高瞄准精度。     

Cornelian Cherry (Cornus mas L.) Extracts Exert Cytotoxicity in Two Selected Melanoma Cell Lines—A Factorial Analysis of Time-Dependent Alterations in Values Obtained with SRB and MTT Assays

Despite the fact that phytochemicals of Cornaceae species have long been discussed as possible auxiliary agents in contemporary treatment, the insights on their properties remain relatively scarce. This study focuses on Cornus mas L. (Cornelian cherry), the extracts of which are reported to exert a pleiotropic effect shown in both in vivo and in vitro studies. This study aimed to explore the cytotoxic effect of extracts from fruits of red (Cornus mas L. ‘Podolski’) and yellow (Cornus mas L. ‘Yantarnyi’ and ‘Flava’) Cornelian cherries on two melanoma cell lines (A375 and MeWo). The extracts were characterized in the context of the concentration of bioactive compounds of antioxidative properties. Cytotoxicity was investigated with the use of the following two assays: SRB and MTT. An additional, alternative protocol for the SRB assay was used in this study so as to account for possible bias. Cytotoxicity was assessed as a difference in the whole time series of cell viability, instead of analyzing differences in raw values (often found in the literature). Both extracts from Cornus mas L. induced cytotoxicity in both A375 and MeWo cell lines, although the response of these cells was different. Moreover, based on this study, there is no evidence for claiming a different magnitude of cytotoxicity between these two extracts.     

动态场景中的背景恢复

为了解决存在运动对象的场景中的背景恢复问题，采用了一种自适应的背景模型。这种背景模型结合背景的构建与更新为一体，不需要预先存储图像序列、它根据后续差异图像中提供的更新的背景信息，借助于背景颜色程度函数，跟踪记录图像中各象素出现的各种颜色的背景颜色程度变化从而得到最新的背景图像。实验表明这种方法对于背景中对象的运动和运动对象的逗留具有很强的适应能力，能以较快的速度恢复最新的背景图像。     

基于小波变换的目标边缘搜索分割方法

为满足目标识别实时性、抗噪声的要求,提出了利用小波变换的图像边缘搜索分割方法.用反对称双正交小波算子对图像进行小波变换,对小波变换模极大值进行启发式搜索检测边缘,得到目标边缘的链码表示.该搜索方法能较好地克服噪声干扰,边缘丢失时能通过在模值分布图中搜索找回边缘,增强算法的鲁棒性.实验结果表明,在同样平台下,使用该方法检测边缘能减少一般小波多尺度分析的计算量,计算速度与使用Sobel算子的梯度方法相当,且具有更好的抗噪声能力.该方法边缘连接良好率高,特征提取方便,综合提高了图像处理算法效率.     

基于相位一致性的实时压缩跟踪方法

针对基于压缩感知的目标跟踪算法在跟踪过程中,光照剧烈变化引起跟踪不稳定或跟踪失败的问题,本文提出了一种基于相位一致性的改进跟踪方法.该方法利用相位一致性图像特征对光照变化不敏感的特点,首先对样本搜索区域内的图像进行相位一致性变换,然后再提取变换后相位一致性图像的特征,将其用于分类器中来确定目标位置.实验结果表明,该方法在目标受到光照剧烈变化影响的情况下具有很强的适应性,在目标大小为50pixel×55pixel时平均处理帧频可达22fps.与已有基于压缩感知跟踪算法相比,该算法在光照变化剧烈的情况下仍具有很好的鲁棒性,而且在目标尺度和纹理发生一定变化的情况下跟踪稳定.     

Indirect target detection method in FLIR image sequences

Due to the complexity of the scene, target detection in forward-looking infrared (FLIR) imagery is a challenging problem, especially for occluded target. The main contribution of this paper is to propose an indirect detection method for improving the recognition probability and effectiveness of target detection method in FLIR image sequences under complex conditions. The proposed method mainly includes four steps: preparation of forward-looking reference image of landmark, extraction of the real-time scene image, template matching and target location, in which some key technologies are proposed, such as perspective transformation used to solve projective problems, position prediction for improving real-time performance, and target location used for identifying the target’s position. Experimental results are shown to demonstrate the robustness and efficiency of proposed method in FLIR image sequences.     

Synthesis and characterization of an MRI Gd‐based probe designed to target the translocator protein

DPA‐713 is the lead compound of a recently reported pyrazolo[1,5‐a]pyrimidineacetamide series, targeting the translocator protein (TSPO 18 kDa), and as such, this structure, as well as closely related derivatives, have been already successfully used as positron emission tomography radioligands. On the basis of the pharmacological core of this ligands series, a new magnetic resonance imaging probe, coded DPA‐C₆‐(Gd)DOTAMA was designed and successfully synthesized in six steps and 13% overall yield from DPA‐713. The Gd‐DOTA monoamide cage (DOTA = 1,4,7,10‐tetraazacyclododecane‐1,4,7,10‐tetraacetic acid) represents the magnetic resonance imaging reporter, which is spaced from the phenylpyrazolo[1,5‐a]pyrimidineacetamide moiety (DPA‐713 motif) by a six carbon‐atom chain. DPA‐C₆‐(Gd)DOTAMA relaxometric characterization showed the typical behavior of a small‐sized molecule (relaxivity value: 6.02 mM^?1 s^?1 at 20 MHz). The good hydrophilicity of the metal chelate makes DPA‐C₆‐(Gd)DOTAMA soluble in water, affecting thus its biodistribution with respect to the parent lipophilic DPA‐713 molecule. For this reason, it was deemed of interest to load the probe to a large carrier in order to increase its residence lifetime in blood. Whereas DPA‐C₆‐(Gd)DOTAMA binds to serum albumin with a low affinity constant, it can be entrapped into liposomes (both in the membrane and in the inner aqueous cavity). The stability of the supramolecular adduct formed by the Gd‐complex and liposomes was assessed by a competition test with albumin. Copyright © 2013 John Wiley & Sons, Ltd.