<sup>131</sup>Ⅰ-Tyr-octreotide的标记方法学及其生物学分布的研究

苏燕; 王峰; 王自正; 孟庆乐; 张乐乐; 蒋娥

¹³¹Ⅰ-Tyr-octreotide的标记方法学及其生物学分布的研究

苏燕 , 王峰 , 王自正 , 孟庆乐 , 张乐乐 , 蒋娥

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¹³¹Ⅰ-Tyr-octreotide的标记方法学及其生物学分布的研究

210006 南京, 南京医科大学附属南京第一医院核医学科
基金项目:
江苏省社会发展科技项目(BS2004507)

南京市重大基金资助项目(ZKX0214)
中图分类号: R817.9

abeling mothod and biodistribution of ¹³¹Ⅰ-Tyr-octreotide

Department of Nuclear Medicine, Nanjing First Hospital of Nanjing Medical University, Nanjing 210006 China
CLC number: R817.9

摘要: 目的探讨¹³¹Ⅰ采用氯胺-T氧化还原法标记生长抑素类似物Tyr-octreotide的可行性和标记物的稳定性,并研究其在正常小鼠体内的生物学分布和非小细胞肺癌荷瘤鼠SPECT显像.方法采用氯胺-T法制备¹³¹Ⅰ-Tryr-octreotide,并测定标记物的放化纯、胶体含量及正常小鼠体内的生物学分布,不同时间点眼球取血后处死,测定血液及各主要脏器的放射性,计算%ID/g.对非小细胞肺癌荷瘤鼠模型进行¹³¹Ⅰ-Tyr-octreotide显像研究.结果采用氯胺-T法¹³¹Ⅰ标记Tyr-octreotide的最佳条件:磷酸缓冲液(0.2 mol/L)0.15 ml,Tyr-octreotide(lg/L)10μl,Na¹³¹Ⅰ(3.7MBq)0.1 ml,氯胺.T(30 g/L)4μl,迅速混匀反应2.5 min,之后加入Na₂S₂O₅(30g/L)5μI终止反应,放化纯可达97%,6 h后放化纯可达83%,胶体含量为1.02%.小鼠体内分布实验表明,肾脏和肝脏对¹³¹Ⅰ-Tyr-octreotide的摄取最高,胃肠消化器官次之,其他脏器摄取较少;对肿瘤组织具有较好的亲和力.结论 ¹³¹Ⅰ-Tyr-octreotide采用氯胺-T法标记具有标记率高、方法简便和迅速、体外稳定性较好、无需进一步纯化等优点.在小鼠体内主要经肝、肾系统代谢,血液清除快,有望成为以生长抑素介导的生物靶向诊断和治疗非小细胞肺癌的分子药物.
- 奥曲肽 /
- 碘放射性同位素 /
- 同位素标记 /
- 癌,非小细胞肺 /
- 生物学分布
Abstract: Objective To evaluate the feasibility and stability of chloramine-T labeling of somatostatin analog Tyr-oetreotide, observe its biodistribution in mice.Methods ¹³¹Ⅰ-Tyr-octreotide was prepare for chloramine-T method and the radiochemical purity and colloid content were measured and the biodistribution was studied. ¹³¹Ⅰ-Tyr-octreotide was injected via tail vein and measure the radioaction of differents organs at differtent time.Results The best condition of ¹³¹Ⅰ-Tyr-octreotide labeling was:(0.2 mol/L) 0.15 ml H₃PO₄ buffer, Tyr-octreotide (1 g/L) 10 μl, Na¹³¹Ⅰ(3.7 MBq)0.1 ml, chloramine-T (30g/L)4μl, Na₂S₂O₅ (30g/L)5μl, reaction time is 2.5 min. The instant radiochemical purity was (97%), and the radiochemical purity of (83%) was remaind after 6h, colloid content is 1.02%. The biodistribution showed high uptake of the tracer in kidney and liver, the stomach intestine was also high, other organs show low uptake.Conclusions Tyr-octreotide was easy to be labeled by chloramine-T. It has achieved high radio-labelling ratio and is a convenient and fast methods. It was quickly cleared from blood and has a high target. ¹³¹Ⅰ-Tyr-octreotide may be a promising agent mediated by somatostatin for diagnos and treatment of cancer.
- Oetreotide /
- Iodine radioisotopes /
- Isotopelabeling /
- Carcinoma,non-small cell lung /
- Biodistribution
本作品遵循Signature-Non-Commercial Use 4.0 International (CC BY-NC 4.0)协议

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¹³¹Ⅰ-Tyr-octreotide的标记方法学及其生物学分布的研究

210006 南京, 南京医科大学附属南京第一医院核医学科

收稿日期: 2007-06-29

基金项目: 江苏省社会发展科技项目(BS2004507)南京市重大基金资助项目(ZKX0214)

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摘要: 目的探讨¹³¹Ⅰ采用氯胺-T氧化还原法标记生长抑素类似物Tyr-octreotide的可行性和标记物的稳定性,并研究其在正常小鼠体内的生物学分布和非小细胞肺癌荷瘤鼠SPECT显像.方法采用氯胺-T法制备¹³¹Ⅰ-Tryr-octreotide,并测定标记物的放化纯、胶体含量及正常小鼠体内的生物学分布,不同时间点眼球取血后处死,测定血液及各主要脏器的放射性,计算%ID/g.对非小细胞肺癌荷瘤鼠模型进行¹³¹Ⅰ-Tyr-octreotide显像研究.结果采用氯胺-T法¹³¹Ⅰ标记Tyr-octreotide的最佳条件:磷酸缓冲液(0.2 mol/L)0.15 ml,Tyr-octreotide(lg/L)10μl,Na¹³¹Ⅰ(3.7MBq)0.1 ml,氯胺.T(30 g/L)4μl,迅速混匀反应2.5 min,之后加入Na₂S₂O₅(30g/L)5μI终止反应,放化纯可达97%,6 h后放化纯可达83%,胶体含量为1.02%.小鼠体内分布实验表明,肾脏和肝脏对¹³¹Ⅰ-Tyr-octreotide的摄取最高,胃肠消化器官次之,其他脏器摄取较少;对肿瘤组织具有较好的亲和力.结论 ¹³¹Ⅰ-Tyr-octreotide采用氯胺-T法标记具有标记率高、方法简便和迅速、体外稳定性较好、无需进一步纯化等优点.在小鼠体内主要经肝、肾系统代谢,血液清除快,有望成为以生长抑素介导的生物靶向诊断和治疗非小细胞肺癌的分子药物.