Polydisulfide Based Biodegradable Macromolecular Magnetic Resonance Imaging Contrast Agents.

Polydisulfide Based Biodegradable Macromolecular Magnetic Resonance Imaging Contrast Agents.
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DOI:
10.1002/ijch.201000016
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发表时间:
2010-08
影响因子:
3.2
通讯作者:
Wu, Xueming
Wu, Xueming
中科院分区:
化学3区
文献类型:
--
作者:
Lu, Zheng-Rong;Wu, Xueming

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大分子Gd(III)配合物在对比增强磁共振成像(MRI)中优于小分子Gd(III)配合物,因为它们延长血液循环和优先肿瘤蓄积。然而,大分子造影剂尚未被批准用于临床应用,因为与它们缓慢的身体排泄相关的安全性问题。聚二硫化物Gd(III)配合物已被设计和开发为可生物降解的大分子MRI造影剂,以通过促进Gd(III)配合物从体内的清除来减轻担忧。这些试剂最初表现为大分子试剂,并导致脉管系统和肿瘤组织中的上级对比增强。然后,它们可以在体内容易地降解成小分子螯合物,这些小分子螯合物可以在MRI检查后通过肾过滤从体内快速排出。各种聚二硫化物Gd(III)配合物已被制备为可生物降解的大分子MRI造影剂。这些造影剂在动物模型中的血管和肿瘤组织中产生了强烈的对比增强,与小分子造影剂相比,具有最小的长期组织蓄积。聚二硫化物Gd(III)配合物作为安全有效的生物可降解大分子MRI造影剂用于心血管和癌症成像具有进一步临床开发的前景。综述了聚二硫化物Gd(III)配合物的化学和性质。
Macromolecular Gd(III) complexes are advantageous over small molecular Gd(III) complexes in contrast enhanced magnetic resonance imaging (MRI) because of their prolonged blood circulation and preferential tumor accumulation. However, macromolecular contrast agents have not been approved for clinical applications because of the safety concerns related to their slow body excretion. Polydisulfide Gd(III) complexes have been designed and developed as biodegradable macromolecular MRI contrast agents to alleviate the concerns by facilitating the clearance of Gd(III) complexes from the body. These agents initially behave as macromolecular agents and result in superior contrast enhancement in the vasculature and tumor tissues. They can then be readily degraded in vivo into small molecular chelates that can rapidly excrete from the body via renal filtration after the MRI examinations. Various polydisulfide Gd(III) complexes have been prepared as biodegradable macromolecular MRI contrast agents. These agents have resulted in strong contrast enhancement in the vasculature and tumor tissue in animal models with minimal long-term tissue accumulation comparable to small molecular contrast agents. Polydisulfide Gd(III) complexes are promising for further clinical development as safe and effective biodegradable macromolecular MRI contrast agents for cardiovascular and cancer imaging. The review summarizes the chemistry and properties of polydisulfide Gd(III) complexes.
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