北京大学医学部机构知识库
Advanced  
IR@PKUHSC  > 北京大学临床肿瘤学院  > 乳腺癌预防治疗中心  > 期刊论文
学科主题: 临床医学
题名:
Synthesis and in vitro/in vivo evaluation of Tc-99m-labeled folate conjugates for folate receptor imaging
作者: 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
发表日期: 2011-05-01
DOI: 10.1016/j.nucmedbio.2010.11.007
卷: 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
所属项目编号: 20701004
项目资助者: National Natural Science Foundation of China
WOS记录号: WOS:000290601300013
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/61178
Appears in Collections:北京大学临床肿瘤学院_乳腺癌预防治疗中心_期刊论文

Files in This Item:

There are no files associated with this item.


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

Recommended Citation:
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.
Service
Recommend this item
Sava as my favorate item
Show this item's statistics
Export Endnote File
Google Scholar
Similar articles in Google Scholar
[Lu, Jie]'s Articles
[Pang, Yan]'s Articles
[Xie, Fang]'s Articles
CSDL cross search
Similar articles in CSDL Cross Search
[Lu, Jie]‘s Articles
[Pang, Yan]‘s Articles
[Xie, Fang]‘s Articles
Related Copyright Policies
Null
Social Bookmarking
Add to CiteULike Add to Connotea Add to Del.icio.us Add to Digg Add to Reddit

Items in IR are protected by copyright, with all rights reserved, unless otherwise indicated.

 

 

Valid XHTML 1.0!
Copyright © 2007-2017  北京大学医学部 - Feedback
Powered by CSpace