铁基磁共振成像剂具有显著的分子和功能特征
Lorenzo Palagi1, Enza Di Gregorio1, Diana Costanzo1
1Department of Molecular Biotechnology and Health Sciences, University of Torino, Via Nizza 52, Torino 10126, Italy.
Journal of the American Chemical Society
|August 25, 2021
概括
一种新型的铁复合物Fe ((deferasirox) 2显示为加多 (Gd) 基MRI对比剂的安全替代品. 这种基于铁的药物表现出相似的疗效,并在24小时内从体内清除.
科学领域:
- 生物医学成像
- 材料科学
- 无机化学
背景情况:
- 基于加多 (Gd) 的MRI对照剂引发了安全问题.
- 由于铁在生物学上具有重要作用,因此正在探索含铁的物种作为潜在的替代品.
- 寻求具有高度稳定的Fe (III) 复合体,特别是具有六合协调连接体的复合体.
研究的目的:
- 评估特定的六合协调Fe (III) 复合物Fe (deferasirox) 2作为Gd基MRI对比剂的替代品的潜力.
- 研究Fe{deferasirox}的稳定性,放松性和体内性能2.
- 评估Fe ((deferasirox) 的安全性和清除情况2.
主要方法:
- 用deferasirox合成和表征Fe (III) 复合物.
- 热力学稳定性和人类血清白蛋白结合亲和度测量.
- 在各种磁场强度 (20-80 MHz) 的放松度测量.
- 在携带瘤的小鼠模型中进行体内MRI研究.
- 诱导合等离子体质谱 (ICP-MS) 用于生物分布和清除研究.
主要成果:
- Fe ((deferasirox) 2 具有卓越的热力学稳定性和高结合性与人血清白蛋白.
- 该复合体表现出良好的放松性,由第二球水分子和白蛋白附加物形成增强.
- 在生体磁共振成像 (MRI) 试验中,小鼠的对比能力与Gd ((DTPA) 相当.
- 在健康小鼠中,ICP-MS证实Fe ((deferasirox) 2) 在24小时内从血液中完全清除.
结论:
- Fe ((deferasirox) 2是一种高度稳定的Fe ((III) 复合物,具有对MRI对比度增强的有利特性.
- 它的可比体内性能和快速清除表明它是一个有前途的,可能更安全的Gd基药物替代品.
- 对Fe ((deferasirox) 2的进一步研究可能会导致改善MRI对比剂的毒性降低.
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