Paramagnetic water-soluble metallofullerenes having the highest relaxivity for MRI contrast agents
Paramagnetic water-soluble metallofullerenes having the highest relaxivity for MRI contrast agents
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DOI：
10.1021/bc000136m
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发表时间：
2001-07-01
影响因子：
4.7
通讯作者：
Shinohara, H
中科院分区：
文献类型：
--
作者：
Mikawa, M;Kato, H;Shinohara, H
合成了水溶性钆（Gd）内嵌金属富勒烯多羟基化合物（Gd@C-82（OH）（n），Gd-富勒烯醇），并对其顺磁性能进行了体内和体外评价，以作为下一代新型磁共振成像（MRI）造影剂。Gd-富勒烯醇的体外水质子弛豫率R-1（对1/T-1的影响）在1.0 T下显著高于（20倍）市售MRI造影剂Magnevist（钆-二亚乙基三胺五乙酸，Gd-DTPA），接近临床MRI的常见场。这种不寻常的高质子弛豫的Gd-富勒烯醇导致最高的信号增强在极低的Gd浓度在MRI研究。在以5 μ mol Gd/kg的剂量静脉内给予Gd-富勒烯醇后，在CDF 1小鼠的肺、肝、脾和肾的体内MRI中证实了强信号，该剂量是Gd-DTPA的典型临床剂量（100 μ mol Gd/kg）的1/20。
Water-soluble gadolinium (Gd) endohedral metallofullerenes have been synthesized as polyhydroxyl forms (Gd@C-82(OH)(n), Gd-fullerenols) and their paramagnetic properties were evaluated by in vivo as well as in vitro for the novel magnetic resonance imaging (MRI) contrast agents for next generation. The in vitro water proton relaxivity, R-1 (the effect on 1/T-1), of Gd-fullerenols is significantly higher (20-folds) than that of the commercial MRI contrast agent, Magnevist (gadolinium-diethylenetri-aminepentaacetic acid, Gd-DTPA) at 1.0 T close to the common field of clinical MRI. This unusually high proton relaxivity of Gd-fullerenols leads to the highest signal enhancement at extremely lower Gd concentration in MRI studies. The strong signal was confirmed in vivo MRI at lung, liver, spleen, and kidney of CDF1 mice after i.v. administration of Gd-fullerenols at a dose of 5 mu mol Gd/kg, which was 1/20 of the typical clinical dose (100 mu mol Gd/kg) of Gd-DTPA.