Organic Radical Contrast Agents Based on Polyacetylenes Containing 2,2,6,6-Tetramethylpiperidine 1-Oxyl (TEMPO): Targeted Magnetic Resonance (MR)/Optical Bimodal Imaging of Folate Receptor Expressing HeLa Tumors in Vitro and in Vivo(a)
机构：[1]Department of Medical Imaging Center, Nanfang Hospital, Southern Medical University, Guangzhou 510515, China[2]Department of Radiology, Guangdong Provincial Traditional Chinese Medical Hospital, Guangzhou 510120, China[3]School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, China[4]Department of Hematology, Nanfang Hospital, Southern Medical University, Guangzhou 510515, China
Nitroxides have great potential as magnetic resonance imaging (MRI) contrast agents for tumor detection. Polyacetylenes(PAs) containing 2,2,6,6-tetramethyl-piperidine oxyl (TEMPO) and poly(ethylene glycol) were synthesized via metathesis polymerization of the corresponding substituted acetylenes to be used for targeted bimodal MRI /optical imaging of tumors. The poly(ethylene glycol) in the polyacetylenes enables covalent conjugation of carboxyl fluorescein and folic acid (FA) with hydroxyl groups to develop targeted multifunctional organic radical contrast agents (ORCAs). In vitro studies confirm the excellent binding specificity and subsequent enhanced cellular internalization of the targeted ORCAs (PA-TEMPO-FI-FA) without cytotoxicity. In vivo T1-weighted MRI demonstrates the active tumor targeting ability of PA-TEMPO-FI-FA to generate specific contrast enhancement in mice bearing HeLa tumors. Moreover, longitudinal optical imaging displays high tumor accumulation after 1h post-injection of PA-TEMPO-FI-FA. These results indicate that multifunctional ORCAs may provide a tumor-targeted delivery platform for further molecular imaging guided cancer therapy.
基金：
National Natural Science Foundation of China [81071146, 81271642]; Research Fund for the Docoral Program of Higher Education of China [20114433110009]
第一作者机构：[1]Department of Medical Imaging Center, Nanfang Hospital, Southern Medical University, Guangzhou 510515, China[2]Department of Radiology, Guangdong Provincial Traditional Chinese Medical Hospital, Guangzhou 510120, China
通讯作者：
推荐引用方式(GB/T 7714)：
Huang Lixia,Yan Chenggong,Cui Danting,et al.Organic Radical Contrast Agents Based on Polyacetylenes Containing 2,2,6,6-Tetramethylpiperidine 1-Oxyl (TEMPO): Targeted Magnetic Resonance (MR)/Optical Bimodal Imaging of Folate Receptor Expressing HeLa Tumors in Vitro and in Vivo(a)[J].MACROMOLECULAR BIOSCIENCE.2015,15(6):788-798.doi:10.1002/mabi.201400403.
APA：
Huang, Lixia,Yan, Chenggong,Cui, Danting,Yan, Yichen,Liu, Xiang...&Liu, Ruiyuan.(2015).Organic Radical Contrast Agents Based on Polyacetylenes Containing 2,2,6,6-Tetramethylpiperidine 1-Oxyl (TEMPO): Targeted Magnetic Resonance (MR)/Optical Bimodal Imaging of Folate Receptor Expressing HeLa Tumors in Vitro and in Vivo(a).MACROMOLECULAR BIOSCIENCE,15,(6)
MLA：
Huang, Lixia,et al."Organic Radical Contrast Agents Based on Polyacetylenes Containing 2,2,6,6-Tetramethylpiperidine 1-Oxyl (TEMPO): Targeted Magnetic Resonance (MR)/Optical Bimodal Imaging of Folate Receptor Expressing HeLa Tumors in Vitro and in Vivo(a)".MACROMOLECULAR BIOSCIENCE 15..6(2015):788-798
