A Tripodal Ruthenium鈥揋adolinium Metallostar as a Potential 伪v尾3 Integrin Specific Bimodal Imaging Contrast Agent

详细信息    查看全文

• 作者：Peter Verwilst ; Svetlana V. Eliseeva ; Luce Vander Elst ; Carmen Burtea ; Sophie Laurent ; St茅phane Petoud ; Robert N. Muller ; Tatjana N. Parac-Vogt ; Wim M. De Borggraeve
• 刊名：Inorganic Chemistry
• 出版年：2012
• 出版时间：June 4, 2012
• 年：2012
• 卷：51
• 期：11
• 页码：6405-6411
• 全文大小：358K
• 年卷期：v.51,no.11(June 4, 2012)
• ISSN：1520-510X

文摘

Gd^III-containing metallostar contrast agents are gaining increased attention, because their architecture allows for a slower tumbling rate, which, in turn, results in larger relaxivities. So far, these metallostars find possible applications as blood pool contrast agents. In this work, the first example of a tissue-selective metallostar contrast agent is described. This RGD-peptide decorated Ru^II(Gd^III)₃metallostar is synthesized as an 伪_v尾₃-integrin specific contrast agent, with possible applications in the detection of atherosclerotic plaques and tumor angiogenesis. The contrast agent showed a relaxivity of 9.65 s^鈥? mM^鈥?, which represents an increase of 170%, compared to a low-molecular-weight analogue, because of a decreased tumbling rate (蟿_R = 470 ps). The presence of the MLCT band (absorption 375鈥?00 nm, emission 525鈥?50 nm) of the central Ru^II(Ph-Phen)₃-based complex grants the metallostar attractive luminescent properties. The ³MLCT emission is characterized by a quantum yield of 4.69% and a lifetime of 804 ns, which makes it an interesting candidate for time-gated luminescence imaging. The potential application as a selective MRI contrast agent for 伪_v尾₃-integrin expressing tissues is shown by an in vitro relaxometric analysis, as well as an in vitroT₁-weighted MR image.