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Coupling Reaction of Oligo p-Phenylene Ethynylene and Peptide Antagonist RM26 Labeling with 131I

JIAN Yuan1,2;ZHOU Zhi-jun2;ZHUO Lian-gang2;ZHAO Peng2;LIAO Wei2;WANG Guan-quan2;LIU Ning1   

  1. 1.Institute of Nuclear Science and Technology, Key Laboratory of Radiation Physics and Technology (Sichuan University), Ministry of Education, Sichuan University, Chengdu 610064, China;2.Institute of Nuclear Physics and Chemistry, China Academy of Engineering Physics, Mianyang 621900, China
  • Online:2016-08-20 Published:2016-08-10

寡聚对苯乙炔与多肽拮抗剂RM26的偶联及131I标记研究

蹇源1,2;周志军2;卓连刚2;赵鹏2;廖伟2;王关全2;刘宁1   

  1. 1.四川大学 原子核科学技术研究所 辐射物理及技术教育部国家重点实验室,四川 成都610064;2.中国工程物理研究院,四川 绵阳621900

Abstract:

Investigations reveale that oligo p-phenylene ethynylene (OPE) molecule can insert into cell membrane, which leads to its cellular internization capacility. Antagonists have high cancer cell affinity, high uptake in cancer cells and fast clearance in normal tissue, these capabilities have attracted much research interest in radiopharmaceutical development. Combining the strong cell-penetrating ability and high affinity of Gastrin-releasing peptide which is overexpressed in the PC-3 cells, the thesis designed and synthesized unsymmetric OPE(NH2) molecule. Then the OPE(NH2) molecule was followed by the coupling reaction with RM26 peptide to obtain the OPE-RM26, and (Tyr)3-RM26 was also got for controling study. After that, the (Tyr)3-RM26 and OPE-RM26 were radiolabeled with I-131 to give high radiolabeling yields that could up to 95%. The radiolabeling compound was stable after 24 h storage at room temperature. These labeled compounds are ready for animal in-vivo experiment. It is expected that OPE-RM26-131I has multi-properties with targeting membrane crossing fire of radioactive elements. The molecule may fast travel to the target tissue and bind to GRP receptor and internalized into cancer cells. The casade process will give rise to its cancer cell toxicity due to longer retention and more killing effect of ray’s irradiation to cancer cells. In this way, OPE-RM26-131I can achieve better anti-cancer ability.

Key words: oligo p-phenylene ethynylene, peptide antagonist, coupling reaction, I-131labeling

摘要:

结合寡聚对苯乙炔(oligo p-phenylene ethynylene, OPE)较强细胞膜穿透能力和多肽拮抗剂RM26对PC-3癌细胞的高亲和性,设计合成OPE-RM26偶联物。采用Iodogen涂管法对偶联物进行131I标记,得到标记率为95%的放射性标记物131I-OPE-RM26,室温下放置24 h后其放化纯度仍大于90%,具有良好的体外稳定性。研究结果为制备具有靶点识别、膜穿透性、射线杀伤的多功能放射性药物提供参考。

关键词: 寡聚对苯乙炔, 多肽拮抗剂, 偶联反应, 131I标记