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(99m)Tc-labeled bombesin(7-14)NH(2) with favorable properties for SPECT imaging of colon cancer
Shi, Jiyun2; Jia, Bing2; Liu, Zhaofei2; Yang, Zhi3; Yu, Zilin2; Chen, Kai4; Chen, Xiaoyuan4; Liu, Shuang1; Wang, Fan2
刊名BIOCONJUGATE CHEMISTRY
2008-06-01
DOI10.1021/bc700471z
19期:6页:1170-1178
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Biochemical Research Methods ; Biochemistry & Molecular Biology ; Chemistry, Multidisciplinary ; Chemistry, Organic
研究领域[WOS]Biochemistry & Molecular Biology ; Chemistry
关键词[WOS]GASTRIN-RELEASING-PEPTIDE ; CYCLIC RGDFK DIMER ; IN-VIVO EVALUATION ; RECEPTOR ANTAGONIST USEFUL ; BOMBESIN-LIKE PEPTIDES ; PROSTATE-CANCER ; VITRO/IN VIVO ; RADIOCHEMICAL INVESTIGATIONS ; BREAST-CANCER ; MOUSE MODEL
英文摘要

In this report, we present the synthesis and evaluation of the (99m)Tc-labeled beta-Ala-BN(7-14)NH(2) (ABN = beta-Ala-Gln-Trp-Ala-Val-Gly-flis-Leu-Met-NH2) as a new radiotracer for tumor imaging in the BALB/c nude mice bearing HT-29 human colon cancer xenografts. The gastrin releasing peptide receptor binding affinity of ABN and HYNIC-ABN (6-hydrazinonicotinamide) was assessed via a competitive displacement of (125)I-[Tyr4]BBN bound to the PC-3 human prostate carcinoma cells. The IC(50) Values were calculated to be 24 +/- 2 nM and 38 +/- 1 nM for ABN and HYNIC-ABN, respectively. HYNIC is the bifunctional coupling agent for (99m)Tc-labeling, while tricine and TPPTS (trisodium triphenylphosphine-3,3′,3 ′′-trisulfonate) are used as coligands to prepare the ternary ligand complex [(99m)Tc(HYNIC-ABN)(tricine)(TPPTS)I in very high yield and high specific activity. Because of its high hydrophilicity (log P = -2.39 +/- 0.06), [(99m)Tc(HYNlC-ABN)(tricine)(TPPS)] was excreted mainly through the renal route with little radioactivity accumulation in the liver, lungs, stomach, and gastrointestinal tract., The tumor uptake at 30 min postinjection (p.i.) was 1.59 +/- 0.23%ID/9 with a steady tumor washout over the 4 h study period. As a result, it had the best T/B ratios in the blood (2.37 +/- 0.68), liver (1.69 +/- 0.41), and muscle (11.17 +/- 3.32) at I h p.i. Most of the injected radioactivity was found in the urine sample at I h p.i., and there was no intact [99mTc(HYNIC-ABN)(tricine)(TPPFS)] detectable in the urine, kidney, and liver samples. Its metabolic instability may contribute to its rapid clearance from the liver, lungs, and stomach. Despite the steady radioactivity washout, the tumors could be clearly visualized in planar images of the BALB/c nude mice bearing the HT-29 human colon xenografts at 1 and 4 h p.i. The favorable excretion kinetics from the liver, lungs,. stomach, and gastrointestinal tract makes [(99m)Tc(HYNIC-ABN)(tricine)(TPPTS)] a promising SPECT radiotracer for imaging colon cancer.

语种英语
WOS记录号WOS:000256950700010
引用统计
被引频次:42[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/56484
专题北京大学医药卫生分析中心
北京大学基础医学院
北京大学临床肿瘤学院_核医学科
作者单位1.Purdue Univ, Sch Hlth Sci, W Lafayette, IN 47907 USA
2.Peking Univ, Med Isotopes Res Ctr, Beijing 100083, Peoples R China
3.Peking Univ, Oncol Sch, Dept Nucl Med, Beijing 100036, Peoples R China
4.Stanford Univ, Sch Med, Dept Radiol, Mol Imaging Program Stanford, Stanford, CA 94305 USA
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GB/T 7714
Shi, Jiyun,Jia, Bing,Liu, Zhaofei,et al. (99m)Tc-labeled bombesin(7-14)NH(2) with favorable properties for SPECT imaging of colon cancer[J]. BIOCONJUGATE CHEMISTRY,2008,19(6):1170-1178.
APA Shi, Jiyun.,Jia, Bing.,Liu, Zhaofei.,Yang, Zhi.,Yu, Zilin.,...&Wang, Fan.(2008).(99m)Tc-labeled bombesin(7-14)NH(2) with favorable properties for SPECT imaging of colon cancer.BIOCONJUGATE CHEMISTRY,19(6),1170-1178.
MLA Shi, Jiyun,et al."(99m)Tc-labeled bombesin(7-14)NH(2) with favorable properties for SPECT imaging of colon cancer".BIOCONJUGATE CHEMISTRY 19.6(2008):1170-1178.
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