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学科主题: 公共卫生
题名:
(99m)Tc-labeled bombesin(7-14)NH(2) with favorable properties for SPECT imaging of colon cancer
作者: Shi, Jiyun2; Jia, Bing2; Liu, Zhaofei2; Yang, Zhi3; Yu, Zilin2; Chen, Kai4; Chen, Xiaoyuan4; Liu, Shuang1; Wang, Fan2
刊名: BIOCONJUGATE CHEMISTRY
发表日期: 2008-06-01
DOI: 10.1021/bc700471z
卷: 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
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/56484
Appears in Collections:北京大学医药卫生分析中心_期刊论文

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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

Recommended Citation:
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.
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