高等学校化学学报 ›› 2013, Vol. 34 ›› Issue (9): 2139.doi: 10.7503/cjcu20130368

• 有机化学 • 上一篇    下一篇

CD20靶向Cy7-Rituximab分子探针的制备及在小鼠活体荧光成像中的应用

林新峰1, 朱华1, 洪业2, 杨志1   

  1. 1. 北京大学肿瘤医院暨北京市肿瘤防治研究所核医学科, 恶性肿瘤发病机制及转化研究教育部重点实验室, 北京100142;
    2. 中国原子能科学研究院, 北京 102413
  • 收稿日期:2013-04-23 出版日期:2013-09-10 发布日期:2013-08-30
  • 作者简介:杨志,男,博士,副教授,副研究员,主要从事核医学、放射性药物及纳米技术的研究.E-mail:pekyz@163.com
  • 基金资助:

    国家自然科学基金(批准号:81071198,81172082);北京市自然科学基金(批准号:7132040);北京大学肿瘤医院院内基金(批准号:2013自主12)资助.

Synthesis and Evaluation of Cy7-Rituximab Targeting CD20 Antigen for in vivo Animal Fluorescence Imaging

LIN Xin-Feng1, ZHU Hua1, HONG Ye2, YANG Zhi1   

  1. 1. Key Laboratory of Carcinogenesis and Translational Research, Ministry of Education, Department of Nuclear Medicine, Peking University Cancer Hospital & Institute, Beijing 100142, China;
    2. China Institute of Atomic Energy, Beijing 102413, China
  • Received:2013-04-23 Online:2013-09-10 Published:2013-08-30

摘要:

以B淋巴细胞表面CD20抗原靶向的单克隆抗体Rituximab为载体, 通过共价键偶联荧光基团菁染料Cy7, 获得了新型荧光分子探针Cy7-Rituximab. 利用全光谱紫外-可见分光光度仪、SDS-聚丙烯酰胺凝胶电泳和基质辅助激光解析电离飞行时间质谱等对该探针结构进行表征, 并通过激光共聚焦显微镜观察了其在弥漫大B细胞淋巴瘤(DLBCL)细胞中的摄取情况. 选用BALB/C裸鼠为模型, 尾静脉注射 Cy7-Rituximab, 通过活体荧光成像系统观察了其在小鼠体内的分布情况. 研究结果表明, 修饰后的Cy7-Rituximab保持了原有抗体的免疫活性. 活体荧光成像结果表明, 在CD20高表达的脾脏部位监测到该分子探针的特异性浓集.

关键词: 光学影像探针, 活体成像, CD20抗原, 利妥昔单抗

Abstract:

A new fluorescence molecular imaging probe Cy7-Rituximab was synthesized through the connection of fluorescence Cy7 dye and protein Rituximab. The probe was fully characterized by fluorescence spectrophotometer, SDS-PAGE and confocal microscopy. The uptake of Cy7-Rituximab probe in DLBCL cells was observed by laser scanning confocal microscope. Cy7-Rituximab probe of 0.4 mL(0.6 mg/mL) was injected to BALB/C nude mice through tail vein. The biodistribution of the novel probe Cy7-Rituximab was eventually observed, especially its specific concentration in spleen.

Key words: Optical imaging probe, Living imaging, CD20 antigen, Rituximab

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