Centro de Investigaciones Nucleares, Facultad de Ciencias, Universidad de República, Mataojo 2055, 11400 Montevideo, Uruguay.
Bioorg Med Chem Lett. 2011 Sep 15;21(18):5598-601. doi: 10.1016/j.bmcl.2011.06.079. Epub 2011 Jun 30.
Study of fluorophore and technetium labeling of poly(amido)-amine (PAMAM) generation 4 (G4) dendrimer and its evaluation as potential molecular imaging agent in both normal and melanoma-bearing mice, are described. Dendrimers were first conjugated with FITC (fluorescein isothiocyanate). Dendrimer-FITC was then incubated with the intermediate (99m)Tc(CO)(3)(H(2)O)(3) and purified by gel filtration. Biodistribution and scintigraphy images were performed administrating (99m)Tc(CO)(3)-dendrimer-FITC to normal mice (NM) or melanoma-bearing mice (MBM). Cryostat tissue sections from MBM mice were analyzed by confocal microscopy. Radiolabeling yield of dendrimer was approx. 90%. The (99m)Tc(CO)(3)-dendrimer-FITC complex was stable for at least 24h. Biodistribution studies in NM showed blood clearance with hepatic and renal depuration. MBM showed a similar pattern of biodistribution with high tumor uptake that allowed tumor imaging. Confocal microscopy analysis showed cytoplasmic distribution of (99m)Tc(CO)(3)-dendrimer-FITC.
研究了荧光素和锝标记的聚（酰胺-胺）（PAMAM）四代（G4）树枝状大分子及其作为正常和荷黑色素瘤小鼠潜在分子成像剂的评价。首先将树枝状大分子与 FITC（异硫氰酸荧光素）缀合。然后将树枝状大分子-FITC 与中间产物 [(99m)Tc(CO)(3)(H(2)O)(3)]+孵育，并通过凝胶过滤进行纯化。通过向正常小鼠（NM）或荷黑色素瘤小鼠（MBM）给药 [（99m）Tc（CO）（3）-树枝状大分子-FITC] 进行生物分布和闪烁成像研究。对 MBM 小鼠的冰冻组织切片进行共聚焦显微镜分析。树枝状大分子的放射性标记产率约为 90%。（99m）Tc（CO）（3）-树枝状大分子-FITC 复合物至少稳定 24 小时。NM 中的生物分布研究表明血液清除伴有肝和肾清除。MBM 表现出与高肿瘤摄取相似的生物分布模式，允许进行肿瘤成像。共聚焦显微镜分析显示（99m）Tc（CO）（3）-树枝状大分子-FITC 的细胞质分布。
