[1]苏燕,王峰,王自正,等.131Ⅰ-Tyr-octreotide的标记方法学及其生物学分布的研究[J].国际放射医学核医学杂志,2007,31(5):257-260.
　SU Yan,WANG Feng,WANG Zi-zheng,et al.abeling mothod and biodistribution of 131Ⅰ-Tyr-octreotide[J].International Journal of Radiation Medicine and Nuclear Medicine,2007,31(5):257-260.
点击复制

131Ⅰ-Tyr-octreotide的标记方法学及其生物学分布的研究(/HTML)
分享到：

《国际放射医学核医学杂志》[ISSN:1673-4114/CN:12-1381/R]

卷:
31
期数:
2007年第5期
页码:
257-260
栏目:
实验核医学
出版日期:
1900-01-01

文章信息/Info

Title:
abeling mothod and biodistribution of 131Ⅰ-Tyr-octreotide
作者:
苏燕;  王峰;  王自正;  孟庆乐;  张乐乐;  蒋娥
210006 南京, 南京医科大学附属南京第一医院核医学科
Author(s):
SU Yan;  WANG Feng;  WANG Zi-zheng;  MENG Qing-le;  ZHANG Le-le;  JIANG E
Department of Nuclear Medicine, Nanjing First Hospital of Nanjing Medical University, Nanjing 210006 China
关键词:
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
Keywords:
Oetreotide; Iodine radioisotopes; Isotopelabeling; Carcinoma; non-small cell lung; Biodistribution
分类号:
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.
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.

参考文献/References:

1 H udson E, Lester JF, Attanoos RL, et al. Successful treatment of bronchorrhea with octreotide in a patient with adenocarcinoma of the lung. J Pain Symptom Manage, 2006,32(3):200-202.
2 Verwijnen SM, Sillevis Smith PA, Hoeben RC, et al. Molecular imaging and treatment of malignant gliomas following adenoviral transfer of tile herpes sinlplex virus-thymidine kinase gene and the somatostatin receptor subtype 2 gene. Cancer Biother Radiopharm, 2004, 19(1):111-120.
3 Mussig K, Petersenn S, Wehrmann M, et al. Somatostatin receptor expression in a parathyroid hormone-related peptlde-secreting pancreatic neuroendocrine turnout causing severe hypercalcaemia. Eur J Gastroenterol Hepatol, 2007,19(8):719-723.
4 Bangard M, Behe M, Guhlke S, et al. Detection of somatostatin receptor-positive tumours using the 99mTc-tricine-HYNIC-D-Phe1-Thy3-octreotide:first results in patients and comparison with 111In-DTPA-D-Phel-octreotide. Eur J Nucl Med, 2000, 27(6):628-637.
5 Sehmitt A, Bernhardt P, Nilsson O, et ah Differences in biodistribution between 99mTc-depreotide, 111In-DTPA-octreotide, and 177Lu-DOTA-Tyr3-octreotate in a small cell lung cancer animal model. Cancer Biother Radiopharm, 2005, 20(2):231-236.
6 Bushnell D, Menda Y, Madsen M, et al. Effects of intravenous amino acid administration with Y-90 DOTA-Phe1-Tyr3-Octreotide (SMT487[OctreoTher] treatment. Cancer Biother Radiopharm, 2004, 19(1):35-41.

相似文献/References:

[1]梁雯丽,郑艳,李娜,等.Graves甲亢患者131I治疗后早期TRAb及TSAb变化的研究分析[J].国际放射医学核医学杂志,2016,40(1):13.[doi:10.3760/cma.j.issn.1673-4114.2016.01.003]
　Liang Wenli,Zheng Yan,Li Na,et al.Analysis of the changes in early TRAb and TSAb after 131I treatment for patients with Graves hyperthyroidism[J].International Journal of Radiation Medicine and Nuclear Medicine,2016,40(5):13.[doi:10.3760/cma.j.issn.1673-4114.2016.01.003]
[2]邓艳,张伟.125I-碘酞酸盐临床应用进展[J].国际放射医学核医学杂志,2016,40(3):225.[doi:10.3760/cma.j.issn.1673-4114.2016.03.012]
　Deng Yan,Zhang Wei.125I-iothalamate clinical applications[J].International Journal of Radiation Medicine and Nuclear Medicine,2016,40(5):225.[doi:10.3760/cma.j.issn.1673-4114.2016.03.012]
[3]田琦,蒋宁一,郑丽.265例精细个体化131I治疗Graves甲亢的疗效观察[J].国际放射医学核医学杂志,2016,40(4):259.[doi:10.3760/cma.j.issn.1673-4114.2016.04.004]
　Tian Qi,Jiang Ningyi,Zheng Li.Therapeutic effect of fine individual 131I treatment on Graves disease hyperthyroidism[J].International Journal of Radiation Medicine and Nuclear Medicine,2016,40(5):259.[doi:10.3760/cma.j.issn.1673-4114.2016.04.004]
[4]杨珂,唐波,于夕荣,等.甲状腺癌131i治疗病房的辐射屏蔽计算与评价[J].国际放射医学核医学杂志,2015,39(5):405.[doi:10. 3760 / cma. j. issn. 1673-4114. 2015. 05. 012]
　yang ke,tang bo,yu xirong,et al.shielding calculation and assessment in 131i therapy for thyroid cancer[J].International Journal of Radiation Medicine and Nuclear Medicine,2015,39(5):405.[doi:10. 3760 / cma. j. issn. 1673-4114. 2015. 05. 012]
[5]刘娇,程兵,常伟,等.非高危分化型甲状腺癌低剂量和高剂量131I清甲疗效的分析[J].国际放射医学核医学杂志,2016,40(6):419.[doi:10.3760/cma.j.issn.1673-4114.2016.06.004]
　Liu Jiao,Cheng Bing,Chang Wei,et al.Ablation efficacy in non-high-risk differentiated thyroid carcinoma patients with low-dose and high-dose 131I[J].International Journal of Radiation Medicine and Nuclear Medicine,2016,40(5):419.[doi:10.3760/cma.j.issn.1673-4114.2016.06.004]
[6]徐蓉生,梅艳,赵力威,等.B超引导下术中125I粒子植入治疗晚期胰腺癌的疗效评价[J].国际放射医学核医学杂志,2016,40(6):424.[doi:10.3760/cma.j.issn.1673-4114.2016.06.005]
　Xu Rongsheng,Mei Yan,Zhao Liwei,et al.Evaluation of 125I particle implantation in the treatment of patients with advanced pancreatic neoplasms using B ultrasound-guided surgery[J].International Journal of Radiation Medicine and Nuclear Medicine,2016,40(5):424.[doi:10.3760/cma.j.issn.1673-4114.2016.06.005]
[7]王越,晋建华,李思进,等.甲状腺24h摄碘率与131I治疗Graves甲亢疗效相关性研究[J].国际放射医学核医学杂志,2015,39(6):442.[doi:10.3760/cma.j.issn.1673-4114.2015.06.002]
　Wang Yue,Jin Jianhua,Li Sijin,et al.Correlation between thyroid 24 h of radioactive iodine uptake and clinical efficacy of 131I therapy for Graves’ hyperthyroidism[J].International Journal of Radiation Medicine and Nuclear Medicine,2015,39(5):442.[doi:10.3760/cma.j.issn.1673-4114.2015.06.002]
[8]郭坤,高蕊,于燕,等.表皮生长因子受体基因表达与甲状腺功能亢进症131I治疗预后的关系[J].国际放射医学核医学杂志,2015,39(1):4.[doi:10.3760/cma.j.issn.1673-4114.2015.01.003]
　Guo Kun,Gao Rui,Yu Yan,et al.The relationship between epidermal growth factor receptor mRNA expression and the efficacv of 131I treatment in hyperthyroidism patients[J].International Journal of Radiation Medicine and Nuclear Medicine,2015,39(5):4.[doi:10.3760/cma.j.issn.1673-4114.2015.01.003]
[9]赵腾,梁军,林岩松.131I治疗前刺激性Tg在分化型甲状腺癌风险评估及治疗决策中的意义[J].国际放射医学核医学杂志,2015,39(1):61.[doi:10.3760/cma.j.issn.1673-4114.2015.01.013]
　Zhao Teng,Liang Jun,Lin Yansong.The role of preablative stimulated thyroglobulin in guiding risk estimation and therapeutic decisions of differentiated thyroid carcinoma[J].International Journal of Radiation Medicine and Nuclear Medicine,2015,39(5):61.[doi:10.3760/cma.j.issn.1673-4114.2015.01.013]
[10]胡小春,蒋宁一,李敬彦,等.硒对经131I治疗Graves病患者血清甲状腺过氧化物酶抗体水平的影响[J].国际放射医学核医学杂志,2015,39(2):140.[doi:10.3760/cma.j.issn.1673-4114.2015.02.008]
　Hu Xiaochun,Jiang Ningyi,Li Jingyan,et al.Effect of additional selenium on the levels of serum thyroid peroxidase antibody in patients with Graves disease treated with 131I[J].International Journal of Radiation Medicine and Nuclear Medicine,2015,39(5):140.[doi:10.3760/cma.j.issn.1673-4114.2015.02.008]

备注/Memo

备注/Memo:
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)
通讯作者:王自正(E-mail:zzwang136@yahoo.com.con)
更新日期/Last Update: 1900-01-01