学科主题临床医学
Synthesis and in vitro/in vivo evaluation of Tc-99m-labeled folate conjugates for folate receptor imaging
Lu, Jie1; Pang, Yan1; Xie, Fang1; Guo, Hongjuan1; Li, Yan1,2,3; Yang, Zhi2,3; Wang, Xuebin1
关键词Technetium-99m Folate receptor Folate conjugate KB tumor Biodistribution
刊名NUCLEAR MEDICINE AND BIOLOGY
2011-05-01
DOI10.1016/j.nucmedbio.2010.11.007
38期:4页:557-565
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Radiology, Nuclear Medicine & Medical Imaging
研究领域[WOS]Radiology, Nuclear Medicine & Medical Imaging
关键词[WOS]PRECLINICAL EVALUATION ; BIOLOGICAL EVALUATION ; BINDING-PROTEIN ; OVARIAN-CANCER ; CELL-LINES ; IN-VIVO ; ACID ; BIODISTRIBUTION ; TISSUES ; STABILITY
英文摘要

Introduction: Folate receptor (FR) is a potential molecular target for radionuclide imaging since it is overexpressed in many human epithelial tumor cells. In this study, a novel folate conjugate was synthesized and labeled with Tc-99m using different coligands. In vitro and in vivo evaluations of these complexes have been done to explore the effect of coligands on the stable, affinity and pharmacokinetic properties.

Methods: A novel folate conjugate, HYNIC-NHHN-FA, was synthesized and characterized. This conjugate was radiolabeled with Tc-99m using tricine, tricine /diphenylphosphinobenzene-3-sulfonic acid sodium (TPPMS) and tricine /trisodium triphenylphosphine-3,3′,3 ′′-trisulfonate (TPPTS) as coligands, respectively. The complexes were purified by high-pressure liquid chromatography (HPLC). In vitro and in vivo evaluations were performed with FR-positive KB cells, normal Kunming mice and athymic nude mice bearing KB tumors.

Results: Labeling with Tc-99m using different coligands resulted in three complexes, Tc-99m (HYNIC-NHHN-FA)(tricine), 5, Tc-99m (HYNIC-NHHN-FA)(tricine/TPPMS), 6 and Tc-99m (HYNIC-NHHN-FA)(tricine/TPPTS), 7. Complex 5 showed at least two isomers and was unstable after being purified by HPLC. Complexes 6 and 7 displayed high stability and similar affinity to FR in vitro. Biodistribution results in athymic nude mice bearing KB tumor showed that complex 7 had a high uptake in FR-positive tumor (9.79=/-1.66%ID/g at 4 h postinjection), and the results of blockade studies confirmed the specific accumulation of the radiotracer in vivo. However, complex 6 showed a low tumor uptake due to its fast excretion via the gastrointestinal tract.

Conclusion: The modification of the coligands can significantly alter the pharmacokinetic properties of the corresponding Tc-99m-HYNIC complexes. Tc-99m (HYNIC-NHHN-FA)(tricine/TPPTS), 7 could be a promising radiotracer for FR imaging. (C) 2011 Elsevier Inc. All rights reserved.

语种英语
WOS记录号WOS:000290601300013
项目编号20701004
资助机构National Natural Science Foundation of China
引用统计
被引频次:25[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/400002259/61178
专题北京大学临床肿瘤学院_乳腺癌预防治疗中心
北京大学临床肿瘤学院_核医学科
作者单位1.Beijing Normal Univ, Coll Chem, Minist Educ, Key Lab Radiopharmaceut, Beijing 100875, Peoples R China
2.Minist Educ, Key Lab Carcinogenesis & Translat Res, Beijing 100142, Peoples R China
3.Peking Univ, Breast Ctr, Sch Oncol, Beijing Canc Hosp & Inst, Beijing 100142, Peoples R China
推荐引用方式
GB/T 7714
Lu, Jie,Pang, Yan,Xie, Fang,et al. Synthesis and in vitro/in vivo evaluation of Tc-99m-labeled folate conjugates for folate receptor imaging[J]. NUCLEAR MEDICINE AND BIOLOGY,2011,38(4):557-565.
APA Lu, Jie.,Pang, Yan.,Xie, Fang.,Guo, Hongjuan.,Li, Yan.,...&Wang, Xuebin.(2011).Synthesis and in vitro/in vivo evaluation of Tc-99m-labeled folate conjugates for folate receptor imaging.NUCLEAR MEDICINE AND BIOLOGY,38(4),557-565.
MLA Lu, Jie,et al."Synthesis and in vitro/in vivo evaluation of Tc-99m-labeled folate conjugates for folate receptor imaging".NUCLEAR MEDICINE AND BIOLOGY 38.4(2011):557-565.
条目包含的文件
条目无相关文件。
个性服务
推荐该条目
保存到收藏夹
查看访问统计
导出为Endnote文件
谷歌学术
谷歌学术中相似的文章
[Lu, Jie]的文章
[Pang, Yan]的文章
[Xie, Fang]的文章
百度学术
百度学术中相似的文章
[Lu, Jie]的文章
[Pang, Yan]的文章
[Xie, Fang]的文章
必应学术
必应学术中相似的文章
[Lu, Jie]的文章
[Pang, Yan]的文章
[Xie, Fang]的文章
相关权益政策
暂无数据
收藏/分享
所有评论 (0)
暂无评论
 

除非特别说明,本系统中所有内容都受版权保护,并保留所有权利。