（99m）锝-乙撑双半胱氨酸-鸟嘌呤：合成、生物分布及动物肿瘤成像

(99m)Tc-EC-guanine: synthesis, biodistribution, and tumor imaging in animals.

作者信息

Yang David J, Ozaki Kaoru, Oh Chang-Sok, Azhdarinia Ali, Yang Thomas, Ito Megumi, Greenwell Allison, Bryant Jerry, Kohanim Saady, Wong Vincenzo K, Kim E Edmund

机构信息

Division of Diagnostic Imaging, The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, USA.

出版信息

Pharm Res. 2005 Sep;22(9):1471-9. doi: 10.1007/s11095-005-6157-8. Epub 2005 Aug 24.

DOI:10.1007/s11095-005-6157-8

PMID:16132359

Abstract

PURPOSE

DNA markers are useful in assessing cell proliferation. The purpose of this study was to synthesize (99m)Tc-ethylenedicysteine-guanine (EC-Guan) for evaluation of cell proliferation.

METHODS

Tumor cells were incubated with (99m)Tc-EC-Guan for cell cycle analysis. Prostate tumor cells that were overexpressing the HSV thymidine kinase gene, or various tumor cells were incubated with (99m)Tc-EC-Guan at 0.5-2 h. Thymidine incorporation assays were performed in lung cancer cells incubated with EC-Guan at 0.1-1 mg/well. Tissue distribution, autoradiography, and planar scintigraphy of (99m)Tc-EC-Guan and (99m)Tc-EC (control) were determined in tumor-bearing rodents at 0.5-4 h.

RESULTS

Cell culture assays indicated that EC-Guan was incorporated in DNA, and there was no significant uptake difference between HSVTK overexpressed and normal groups. Biodistribution and scintigraphic imaging studies of (99m)Tc-EC-Guan showed increased tumor/tissue count density ratios as a function of time.

CONCLUSIONS

Our results indicate that (99m)Tc-EC-Guan may be useful as a tumor proliferation imaging agent.

摘要

目的

DNA标记物在评估细胞增殖方面很有用。本研究的目的是合成99m锝-乙二巯基半胱氨酸-鸟嘌呤（EC-鸟嘌呤）用于评估细胞增殖。

方法

将肿瘤细胞与99m锝-EC-鸟嘌呤一起孵育用于细胞周期分析。将过表达单纯疱疹病毒胸苷激酶基因的前列腺肿瘤细胞或各种肿瘤细胞与99m锝-EC-鸟嘌呤在0.5至2小时内孵育。在以0.1至1毫克/孔的EC-鸟嘌呤孵育的肺癌细胞中进行胸苷掺入试验。在荷瘤啮齿动物中于0.5至4小时测定99m锝-EC-鸟嘌呤和99m锝-EC（对照）的组织分布、放射自显影和平面闪烁显像。