Hosono M, Hosono M N, Haberberger T, Zamora P O, Guhlke S, Bender H, Knapp F F, Biersack H J
Department of Radiology, Saitama Medical Center, Saitama Medical School, Kawagoe.
Jpn J Cancer Res. 1996 Sep;87(9):995-1000. doi: 10.1111/j.1349-7006.1996.tb02131.x.
We examined the potential of radiolabeled somatostatin analogs, 125I-Tyr-3-octreotide (125I-octreotide), (111)In-DTPA(diethylenetriaminepentaacetatic acid)-D-Phe-1-octreotide (111In-octreotide), and 188Re-octreotide for targeting small-cell lung cancer (SCLC) in a mouse model. Tyr-3-octreotide was labeled with 125I by the chloramine T method, and (111)In-octreotide was obtained as a kit, while 188Re was eluted from a 188W/188Re generator, and octreotide was directly labeled with 188Re by reducing disulfide bonds. The 125I-, 111In-, and 188Re-octreotides were injected i.v. into athymic mice bearing NCI-H69 tumors, and the biodistributions were determined at 15 min, and 2, 4, 8, and 24 h. Tumor uptakes were 0.5+/-0.2, 0.3+/-0.1, 0.3+/-0.1 %ID/g, and tumor-to-blood ratios were 1.8, 11.9, 1.2 at 8 h for 125I-, 111In-, and 188Re-octreotides, respectively. Accumulations of 111In-octreotide in normal tissues were lower than those of 125I- and 188Re-octreotides. 188Re-octreotide can be used to localize SCLC lesions as efficiently as radioiodinated octreotide. However, 111In-octreotide was the most suitable agent to obtain high tumor-to-normal tissue contrast for localizing SCLC.
我们在小鼠模型中研究了放射性标记的生长抑素类似物125I-Tyr-3-奥曲肽（125I-奥曲肽）、（111）In-DTPA（二乙三胺五乙酸）-D-Phe-1-奥曲肽（111In-奥曲肽）和188Re-奥曲肽靶向小细胞肺癌（SCLC）的潜力。Tyr-3-奥曲肽通过氯胺T法用125I标记，（111）In-奥曲肽作为试剂盒获得，而188Re从188W/188Re发生器中洗脱，奥曲肽通过还原二硫键直接用188Re标记。将125I-、111In-和188Re-奥曲肽静脉注射到携带NCI-H69肿瘤的无胸腺小鼠体内，并在15分钟以及2、4、8和24小时测定生物分布。125I-、111In-和188Re-奥曲肽在8小时时的肿瘤摄取分别为0.5±0.2、0.3±0.1、0.3±0.1 %ID/g，肿瘤与血液的比率分别为1.8、11.9、1.2。111In-奥曲肽在正常组织中的蓄积低于125I-和188Re-奥曲肽。188Re-奥曲肽定位SCLC病变的效率与放射性碘化奥曲肽相同。然而，111In-奥曲肽是获得高肿瘤与正常组织对比度以定位SCLC的最合适试剂。
