共查询到19条相似文献,搜索用时 78 毫秒
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通过二乙三胺五乙酸的双N-羟基琥珀酰亚胺活性酯与含氨基的乳糖或D-半乳糖衍生物反应,合成了8种含有D-半乳糖基的二乙三胺五乙酸非离子型配体,并进一步合成了其钆(Ⅲ)配合物,配体及配合物的结构经IR,^1HNMR与元素分析表征,对配合物的体外驰豫性能和小鼠急性毒性作了初步研究,家兔在磁共振成像实验表明这种上类造影剂具有肝靶向的特性。 相似文献
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通过在DTPA配体上修饰N-羧甲基壳聚糖(NCMCS)增加配体的分子量,构建配合物Gd-(DTPA-NCMCS)。测定了Gd-(DTPA-NCMCS)及对照组Gd-DTPA与Gd-(DTPA-CS)不同浓度的弛豫时间T1,拟合了配合物的纵向弛豫率r1,结果表明Gd-(DTPA-NCMCS)纵向弛豫能力明显强于Gd-DTPA,也高于配合物Gd-(DTPA-CS),浓度梯度的体外加权成像图清晰地观察到配合物Gd-(DTPA-NCMCS)比Gd-DTPA、Gd-(DTPA-CS)对应水溶液的信号更强。MTT法测定了Gd-(DTPA-NCMCS)的IC50值为568μmol·L-1,表现出良好的生物相容性。Gd-(DTPA-NCMCS)可作为潜在的磁共振造影剂。 相似文献
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文通过在DTPA配体上修饰N-羧甲基壳聚糖(NCMCS)增加配体的分子量,构建配合物Gd-(DTPA-NCMCS).测定了Gd-(DTPA-NCMCS)及对照组Gd-DTPA与Gd-(DTPA-CS)不同浓度的弛豫时间T1,拟合了配合物的纵向弛豫率r1,结果表明Gd-(DTPA-NCMCS)纵向弛豫能力明显强于Gd-DTPA,也高于配合物Gd-(DTPA-CS),浓度梯度的体外加权成像图清晰地观察到配合物Gd-(DTPA-NCMCS)比Gd-DTPA、Gd-(DTPA-CS)对应水溶液的信号更强。MTT法测定了Gd-(DTPA-NCMCS)的IC50值为568 μmol·L-1,表现出良好的生物相容性。Gd-(DTPA-NCMCS)可作为潜在的磁共振造影剂。 相似文献
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由二乙三胺五乙胺(DTPA)双酸酐和乙二胺四乙酸(EDTA)双酸酐与维生素B6族化全物吡哆醇(PN)或其衍生物合成了一系列新型的多胺多羧酸双吡哆醇酯衍生物及其钆、锰、铁等顺磁性金属螯合物,研究了其中钆和锰螯合物在体外水溶液中对水质子的给向弛豫性能,结果表明,所有配体和配合物均有很好的水溶性,且对光和空气稳定,螯合物的驰豫率(T1)与可与其母体螯全物相媲美,如钆-二乙三胺五乙酸二吡哆醇酯(GdDTP 相似文献
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Platas-Iglesias C Mato-Iglesias M Djanashvili K Muller RN Elst LV Peters JA de Blas A Rodríguez-Blas T 《Chemistry (Weinheim an der Bergstrasse, Germany)》2004,10(14):3579-3590
A new pyridine-containing ligand, N,N'-bis(6-carboxy-2-pyridylmethyl)ethylenediamine-N,N'-diacetic acid (H(4)L), has been designed for the complexation of lanthanide ions. (1)H and (13)C NMR studies in D(2)O solutions show octadentate binding of the ligand to the Ln(III) ions through the nitrogen atoms of two amine groups, the oxygen atoms of four carboxylates, and the two nitrogen atoms of the pyridine rings. Luminescence measurements demonstrate that both Eu(III) and Tb(III) complexes are nine-coordinate, whereby a water molecule completes the Ln(III) coordination sphere. Ligand L can sensitize both the Eu(III) and Tb(III) luminescence; however, the quantum yields of the Eu(III)- and Tb(III)-centered luminescence remain modest. This is explained in terms of energy differences between the singlet and triplet states on the one hand, and between the 0-phonon transition of the triplet state and the excited metal ion states on the other. The anionic [Ln(L)(H2O)]- complexes (Ln=La, Pr, and Gd) were also characterized by theoretical calculations both in vacuo and in aqueous solution (PCM model) at the HF level by means of the 3-21G* basis set for the ligand atoms and a 46+4 f(n) effective core potential for the lanthanides. The structures obtained from these theoretical calculations are in very good agreement with the experimental solution structures, as demonstrated by paramagnetic NMR measurements (lanthanide-induced shifts and relaxation-rate enhancements). Data sets obtained from variable-temperature (17)O NMR at 7.05 T and variable-temperature (1)H nuclear magnetic relaxation dispersion (NMRD) on the Gd(III) complex were fitted simultaneously to give insight into the parameters that govern the water (1)H relaxivity. The water exchange rate (k(298)(ex)=5.0 x 10(6) s(-1)) is slightly faster than in [Gd(dota)(H2O)]- (DOTA=1,4,7,10-tetrakis(carboxymethyl)-1,4,7,10-tetraazacyclododecane). Fast rotation limits the relaxivity under the usual MRI conditions. 相似文献
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A new class of paramagnetic macromolecular magnetic resonance imaging contrast agents has been developed. Eight new polyamide ligands were synthesized by copolymerization of ethylenediaminetetraacetic acid dianhydride or diethylenetriaminepentaacetic acid dianhydride and diamine monomers. Their gadolinium(III), manganese(II) and iron(III) complexes were also synthesized. All polyamide ligands and metal complexes were characterized by 1H nuclear magnetic resonance, infrared spectra and elemental analyses. Relaxivity studies showed that the polyamide paramagnetic metal complexes had obviously higher relaxation effectiveness as compared to corresponding simple monomeric paramagnetic metal complexes. 相似文献
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Battistini E Gianolio E Gref R Couvreur P Fuzerova S Othman M Aime S Badet B Durand P 《Chemistry (Weinheim an der Bergstrasse, Germany)》2008,14(15):4551-4561
Nanosized contrast agents have great potential in magnetic resonance molecular imaging applications for clinical diagnosis. This study proposes new nanoparticles spontaneously formed under mild conditions and composed of a noncovalent adduct between a gadolinium complex, a polymer of beta-cyclodextrin (pbetaCD: MW 1.5 x 10(6) g mol(-1)) and a dextran grafted with alkyl chains (MD). The formation of this supramolecular nanoassembly is based upon a "lock-and-key" recognition process in which the hydrophobic alkyl chains of MD and the adamantyl moieties of macrocyclic Gd(III) chelates are included in the cavities of pbetaCD. The large number of betaCDs contained in the pbetaCD resulted in the formation of 200 nm diameter nanoparticles, each entrapping 1.8 x 10(5) molecules of a low-molecular-weight Gd complex. This system, which exhibits a great relaxivity enhancement (48.4 mM(-1) s(-1), at 20 MHz and 37 degrees C) compared to the Gd(III) chelate itself (5.2 mM(-1) s(-1)), appears to be a promising strategy for the in vivo targeted delivery of Gd(III) complexes. The mechanisms of particle formation, conjugation strategies, and relaxometric characterizations in the field of contrast-enhanced magnetic resonance imaging are discussed. 相似文献
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《Magnetic resonance in chemistry : MRC》2003,41(8):585-588
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. 相似文献
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Hanaoka K Kikuchi K Terai T Komatsu T Nagano T 《Chemistry (Weinheim an der Bergstrasse, Germany)》2008,14(3):987-995
Magnetic resonance imaging (MRI) permits noninvasive three-dimensional imaging of opaque organisms. Gadolinium (Gd(3+)) complexes have become important imaging tools as MRI contrast agents for MRI studies, though most of them are nonspecific and report solely on anatomy. Recently, MRI contrast agents have been reported whose ability to relax water protons is triggered or greatly enhanced by recognition of a particular biomolecule. This new class of MRI contrast agents could open up the possibility of reporting on the physiological state or metabolic activity deep within living specimens. One possible strategy for this purpose is to utilize the increase in the longitudinal water proton r(1) relaxivity that occurs upon slowing the molecular rotation of a small paramagnetic complex, a phenomenon which is known as receptor-induced magnetization enhancement (RIME), by either binding to a macromolecule or polymerization of the agent itself. Here we describe the design and synthesis of a novel beta-galactosidase-activated MRI contrast agent, the Gd(3+) complex [Gd-5], by using the RIME approach. beta-Galactosidase is commonly used as a marker gene to monitor gene expression. This newly synthesized compound exhibited a 57% increase in the r(1) relaxivity in phosphate-buffered saline (PBS) with 4.5% w/v human serum albumin (HSA) in the presence of beta-galactosidase. Detailed investigations revealed that RIME is the dominant factor in this increase of the observed r(1) relaxivity, based on analysis of Gd(3+) complexes [Gd-5] and [Gd-8], which is generated from [Gd-5] by the activity of beta-galactosidase, and spectroscopic analysis of their corresponding Tb(3+) complexes, [Tb-5] and [Tb-8]. 相似文献
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将具有良好生物膜穿透性的异烟肼(INH)和Gd-DO3A偶联,合成了小分子MRI造影剂Gd-DO3A-INH;利用脉冲电转染技术标记间充质干细胞,有效提高了进入细胞的Gd-DO3A-INH浓度,并诱导部分游离态Gd-DO3A-INH在细胞质中自组装成纳米粒子。细胞样品的TEM观察到细胞内形成了Gd-DO3A-INH纳米粒子;细胞传代实验和体外MRI揭示了2种不同状态的Gd-DO3A-INH对细胞水质子弛豫速率的影响机制,以及细胞传代过程中细胞内2种不同状态Gd-DO3A-INH的浓度涨落引起的MRI造影效果的变化机制。 相似文献