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肿瘤血管靶向分子探针多肽RRL(g2)的作用研究 被引量:6

Technetium-99m-Arg-Arg-Leu(g2):A Modified Peptide Probe Targeted to Neovascularization in Molecular Tumor Imaging
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摘要 [目的]设计合成分子结构更小的多肽RRL(g2),并用放射性核素99mTc标记,得到新型优化肿瘤新生血管分子探针。[方法]应用化学合成法合成多肽RRL(g2)及对照肽片段GGG(g2),应用高效液相色谱(HPLC)及电喷雾离子质谱(EMI-MS)对合成化合物的分子量及纯度进行鉴定,进而对放射性核素99mTc标记的RRL(g2)多肽探针及对照肽进行体内外生物学性质评价。[结果]应用化学合成法合成的RRL(g2)及GGG(g2)纯度达99%以上,放射性核素99mTc的标记率约73%,稳定性较好。静脉注射分子探针后30min,99mTc-RRL(g2)相对于对照肽99mTc-GGG(g2),在肿瘤组织中有较高的摄取率,而且在肿瘤组织中能滞留较长时间。[结论]新型肿瘤新生血管多肽探针99mTc-RRL(g2)相比于131I-tRRL,在肿瘤新生血管分子显像应用中拥有更大的优势,如肿瘤摄取率的增加,是更有前景的新型肿瘤新生分子显像多肽探针。 [Purpose] To develop smaller structure cyclic RRL(g2) and radiolabeled with 99mTc as a novel and optimized peptide probe on tumor angiogenesis molecular imaging.[Methods] Both RRL(g2) and control peptide GGG(g2) peptide chains were synthesized and characterized by HPLC and EMI-MS analysis.After synthesized and purified,the peptides were radiolabeled with 99mTc by a one-step method for physicochemical property assay and biodistribution experiments.[Results] The purity of peptide RRL(g2) and GGG(g2) were more than 99% after synthesized and purified.The radiolabeling of 99mTc-RRL(g2) has reached 73% and it is stable in vitro.99mTc-RRL(g2) had higher tumor uptake(30min after injection) and longer tumor retention than 99mTc-GGG(g2) in tumor models tested.[Conclusions] The 99mTc-RRL(g2) has more good characteristics such as higher tumor uptake radio and short halflife-time compared with 131I-tRRL.The information obtained here may guide the future development of RRL peptide-based tumor angiogenesis molecular imaging and internal radiotherapeutic agents targeting tumor neavascular.
作者 卢霞 王荣福
出处 《肿瘤学杂志》 CAS 2013年第12期925-929,共5页 Journal of Chinese Oncology
基金 首都卫生发展科研专项基金(2011-6032-03)
关键词 RRL(g2) 肿瘤血管分子显像 放射性核素标记 99mTc RRL(g2) tumor angiogenesis molecular imaging radionuclide labeling 99mTc
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