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用自行研制的[~(131)I-Tyr~3]octreotide 进行载胰腺癌裸鼠的肿瘤受休显像。以固相-液相结合法化学合成 oc-treotide,经 HPLC 纯化和鉴定后用氯胺 T 法进行~(131)I 标记。标记物以 Sephadex G-10纯化,经尾静脉注入载胰腺癌裸鼠体内,分别在1、2、3、4、5和6小时进行肿瘤显像,划出感兴趣区(ROI),测其 T/B 值。3天后再重新注射标记物,并于3小时观察体内分布,计算各组织 T/NT 比值。结果:化学合成的纯品 octreotide 经 HPLC、氨基酸分析、快原子轰击质谱鉴定,保留时间、氨基酸组成及分子量(1135)均与文献值相符。注射后1小时肿瘤中即有明显放射性浓聚,2小时可清晰显示肿瘤,T/B 值达5.31。3小时肿瘤与肌肉的 T/NT 比值为3.43。故自行研制的[~(131)I-Tyr~3]octreotide 可用于生长抑素受体阳性肿瘤的显像。
Tumor resection imaging was performed in pancreatic cancer-bearing nude mice with self-developed [~ (131) I-Tyr ~ 3] octreotide. The oc-treotide was chemically synthesized by solid phase-liquid phase method. After purified by HPLC and identified by ~ (131) I chloramines T method. The markers were purified by Sephadex G-10 and injected into the tail vein of pancreatic cancer-bearing nude mice. Tumor imaging was performed at 1, 2, 3, 4, 5, and 6 hours respectively. ROI T / B value. Three days later, the markers were re-injected and observed in vivo for 3 hours to calculate the T / NT ratio of each tissue. Results: The pure synthesized octreotide was identified by HPLC, amino acid analysis and mass spectrometry with fast atom bombardment. The retention time, amino acid composition and molecular weight (1135) were consistent with those of the literature. One hour after injection, there was obvious radioactive accumulation in the tumor, and the tumor was clearly visible in two hours. The T / NT ratio of tumor to muscle was 5.31 at T / B of 5.31.3 hours. Therefore, self-developed [~ (131) I-Tyr ~ 3] octreotide can be used for the imaging of somatostatin receptor-positive tumors.