Zabel P L, Noujaim A A, Shysh A, Bray J
Eur J Nucl Med. 1983;8(6):250-4. doi: 10.1007/BF00522515.
The Thomsen-Friedenreich (T) antigen, beta-D-Gal-(1 leads to 3)-alpha-D-GalNAc, is exposed in reactive form on many human adenocarcinomata, but not on corresponding benign tissues. Peanut lectin (PNA) has a strong binding affinity for the T antigen and reportedly binds preferentially to certain malignant tissues. We investigated the potential of radiolabelled PNA as a tumour localising agent in an animal model system using a mouse lymphoma (RI) shown to bind fluorescein-labelled PNA in vitro. The radioiodinated lectin showed good tumour localization and rapid blood clearance. Clear images of tumours were obtained, in serial scintigraphic imaging, by 24 and 48 h. No blood background subtraction was necessary. Biodistribution studies revealed tumour to blood ratios in mice were 6:1 (at 24 h) and 17:1 (at 48 h), and tumour to muscle ratios were 34:1 (at 24 h) and 40:1 (at 48 h). Rapid in vivo breakdown of 125I-PNA led to some localization of free iodide in the kidneys, stomach, thyroid and salivary glands.
汤姆森 - 弗里登赖希(T)抗原,即β - D - 半乳糖 - (1→3) - α - D - N - 乙酰半乳糖胺,以反应性形式暴露于许多人类腺癌中,但在相应的良性组织中则不然。花生凝集素(PNA)对T抗原有很强的结合亲和力,据报道它优先与某些恶性组织结合。我们在一个动物模型系统中研究了放射性标记的PNA作为肿瘤定位剂的潜力,该系统使用了一种在体外显示能结合荧光素标记的PNA的小鼠淋巴瘤(RI)。放射性碘化凝集素显示出良好的肿瘤定位和快速的血液清除。在连续闪烁成像中,在24小时和48小时时获得了清晰的肿瘤图像。无需进行血液本底扣除。生物分布研究表明,小鼠体内肿瘤与血液的比率在24小时时为6:1,在48小时时为17:1,肿瘤与肌肉的比率在24小时时为34:1,在48小时时为40:1。125I - PNA在体内的快速分解导致游离碘在肾脏、胃、甲状腺和唾液腺中出现一定程度的定位。