| 卢 霞,王荣福.肿瘤血管靶向分子探针多肽RRL（g2）的作用研究[J].肿瘤学杂志,2013,19(12):925-929. |
| 肿瘤血管靶向分子探针多肽RRL（g2）的作用研究 |
| Technetium-99m-Arg-Arg-Leu(g2): A Modified Peptide Probe Targeted to Neovascularization in Molecular Tumor Imaging |
| 投稿时间：2013-11-12 |
| DOI：10.11735/j.issn.1671-170X.2013.12.B004 |
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| 中文关键词: RRL(g2) 肿瘤血管分子显像 放射性核素标记 99mTc |
| 英文关键词:RRL (g2) tumor angiogenesis molecular imaging radionuclide labeling 99mTc |
| 基金项目:首都卫生发展科研专项基金(2011-6032-03) |
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| 中文摘要: |
| 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。 |
| 英文摘要: |
| Abstract:［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. |
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