1] Kurume University School of Medicine, Kurume, Japan. [2].
1] [2].
Nat Med. 2014 Feb;20(2):215-9. doi: 10.1038/nm.3437. Epub 2014 Jan 12.
Progressive inflammation in atherosclerotic plaques is associated with increasing risk of plaque rupture. Molecular imaging of activated macrophages with 2-deoxy-2-[(18)F]fluoro-D-glucose ([(18)F]FDG) has been proposed for identification of patients at higher risk for acute vascular events. Because mannose is an isomer of glucose that is taken up by macrophages through glucose transporters and because mannose receptors are expressed on a subset of the macrophage population in high-risk plaques, we applied (18)F-labeled mannose (2-deoxy-2-[(18)F]fluoro-D-mannose, [(18)F]FDM) for targeting of plaque inflammation. Here, we describe comparable uptake of [(18)F]FDM and [(18)F]FDG in atherosclerotic lesions in a rabbit model; [(18)F]FDM uptake was proportional to the plaque macrophage population. Our FDM competition studies in cultured cells with 2-deoxy-2-[(14)C]carbon-D-glucose ([(14)C]2DG) support at least 35% higher [(18)F]FDM uptake by macrophages in cell experiments. We also demonstrate that FDM restricts binding of anti-mannose receptor antibody to macrophages by approximately 35% and that mannose receptor targeting may provide an additional avenue for imaging of plaque inflammation.
动脉粥样硬化斑块中的进行性炎症与斑块破裂风险的增加有关。用 2-脱氧-2-[(18)F]氟-D-葡萄糖 ([(18)F]FDG) 对活化的巨噬细胞进行分子成像,已被提议用于识别急性血管事件风险较高的患者。因为甘露糖是葡萄糖的异构体,通过葡萄糖转运蛋白被巨噬细胞摄取,并且甘露糖受体在高危斑块中的巨噬细胞亚群上表达,我们应用 (18)F 标记的甘露糖 (2-脱氧-2-[(18)F]氟-D-甘露糖,[(18)F]FDM) 来靶向斑块炎症。在这里,我们描述了 [(18)F]FDM 和 [(18)F]FDG 在兔模型中的动脉粥样硬化病变中具有可比的摄取;[(18)F]FDM 的摄取与斑块内的巨噬细胞群体成正比。我们在培养细胞中的 FDM 竞争研究用 2-脱氧-2-[(14)C]碳-D-葡萄糖 ([(14)C]2DG) 支持在细胞实验中,巨噬细胞对 [(18)F]FDM 的摄取至少高 35%。我们还证明 FDM 限制了抗甘露糖受体抗体与巨噬细胞的结合约 35%,并且甘露糖受体靶向可能为斑块炎症的成像提供另一种途径。