摘要
针对临床上广泛应用的磁共振成像造影剂二乙三胺五乙酸钆(Gd-DTPA)是一种离子型造影剂,由于其成像时间短、渗透压较高,没有组织或器官选择性(靶向性),尤其对早期肿瘤的成像检测效果较差的问题,利用卟啉对肿瘤的特异亲和性,将5-(4-氨基苯基)-10,15,20-三吡啶基卟啉与二乙三胺五乙酸双酸酐(DTPAA)进行化学反应,合成了一种小分子配体(DTPA-2APTMPyP),再与金属钆离子Gd(Ⅲ)配合,从而制备了小分子磁共振成像造影剂(Gd-DTPA-2APTMPyP).并对所合成的配体及其配合物进行了红外光谱、紫外光谱与核磁共振等结构表征,证明产品为目标产物.同时初步测定了配合物的体外弛豫率与细胞毒性.实验表明,与临床应用的小分子造影剂二乙三胺五乙酸钆(Gd-DTPA)相比,这种小分子造影剂具有较高的弛豫率与略高的体外细胞毒性.
Gd-DTPA was the contrast agent widely used in clinical MRI for contrast enhancement. However, the short imaging time and the nonspecific distribution in vivo limit its utility in focal lesion detection and diagnosis. 5-（4-Aminophenyl）-lO, 15, 20-tripyridineporphyrin （APTMPyP） was chosen as a tumor-targeting group. A ligand containing porphyrin groups was then synthesized by the incorporation of APTMPyP into diethylenetriaminepentaaeetie dianhydride （DTPAA）. This ligand obtained was further reacted with gadolinium chloride to make corresponding tumor-targeting gadolinium complex Gd-DTPA-2APTMPyP. The ligand and gadolinium complex were characterized by infrared spectrum, Fourier Transform Infrared Spectrometer （FT-IR）, Ultraviolet spectrometry （UV）, etc and their properties in vitro were also evaluated. G＆DTPA-2APTMPyP possesses obviously higher relaxation effectiveness and slightly higher cytotoxicity to Hela cells than those of Gd-DTPA. Therefore Gd-DTPA-2APTMPyP can be used as a potential contrast agent in targeted MRI to tumors.
出处
《武汉工程大学学报》
CAS
2013年第2期1-5,10,共6页
Journal of Wuhan Institute of Technology
基金
国家自然科学基金面上项目(51173140)
武汉市科技攻关计划项目(2013年批文待发)
武汉工程大学第三届研究生创新基金(CX201139)
关键词
磁共振成像
造影剂
GD-DTPA
卟啉
magentic resonance imaging（MRI）
contrast agent relaxivity Gd-DTPA porphyrin
