含卟啉的钆配合物作为一种肿瘤靶向磁共振成像（MRI）造影剂
Porphyrin-containing Gadolinium Complex as a Tumor-targeting Magnetic Resonance Imaging (MRI) Contrast Agent.
作者信息
Ouyang Yao-Hua, Xu Wei, Zhou Cheng-Kai, Liu Fan, Li Bin, Yan Guo-Ping, Yang Lian, Chen Si, Jiang Can
机构信息
School of Materials Science and Engineering, Wuhan Institute of Technology, 693 Xiongchu Road, Wuhan 430074, Hubei Province, China.
Center for Magnetic Resonance Imaging of Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430022, Hubei Province, China.
出版信息
Curr Drug Deliv. 2018;15(7):972-978. doi: 10.2174/1567201815666180409111005.
OBJECTIVE
Gadolinium diethylenetriaminepentaacetic di[5-(4'-amidophenyl)-10,15,20- tris(4'-sulfonatophenyl) porphyrin trisodium salt] (Gd-DTPA-2APTSPP) was synthesized by the reaction of diethylenetriaminepentaacetic dianhydride with 5-(4'-aminophenyl)-10,15,20-tris(4'-sulfonatophenyl) porphyrin and subsequently chelation with gadolium chloride.
METHODS
This gadolinium complex was characterized and its properties in vitro and in vivo were also evaluated. Compared with Gd-DTPA, Gd-DTPA-2APTSPP possessed high relaxivity r1, low cytotoxicity to HeLa cells and high enhanced signal intensities of the VX2 carcinoma in rabbits for a prolonged time.
CONCLUSION
Moreover, Gd-DTPA-2APTSPP can distinguish the VX2 carcinoma from the reactive hyperplasia incited by inflammation and normal tissues in rabbits. Therefore, Gd-DTPA-2APTSPP can be taken up selectively by tumors and show the potential as a tumor-targeting MRI contrast agent.
目的
通过二乙烯三胺五乙酸二酐与5-(4'-氨基苯基)-10,15,20-三(4'-磺酸钠苯基)卟啉反应，随后与氯化钆螯合，合成钆二乙烯三胺五乙酸二5-(4'-氨基苯基)-10,15,20-三(4'-磺酸钠苯基)卟啉三钠盐。
方法
对该钆配合物进行表征，并评估其体外和体内性质。与钆喷酸葡胺(Gd-DTPA)相比，Gd-DTPA-2APTSPP具有高纵向弛豫率r1、对人宫颈癌HeLa细胞低细胞毒性以及对兔VX2癌长时间的高增强信号强度。
结论
此外，Gd-DTPA-2APTSPP能区分兔VX2癌与炎症激发的反应性增生及正常组织。因此，Gd-DTPA-2APTSPP可被肿瘤选择性摄取，显示出作为肿瘤靶向磁共振成像(MRI)造影剂的潜力。
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