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[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。
[Objective] To design and synthesize the polypeptide RRL (g2) with smaller molecular structure and label it with radionuclide 99mTc to obtain a new type of optimized tumor angiogenesis probe. [Method] The synthetic peptide RRL (g2) and the control peptide fragment GGG (g2) were synthesized by chemical synthesis. The molecular weight and purity of the synthesized compounds were identified by high performance liquid chromatography (HPLC) and electrospray ionization mass spectrometry Further, the radionuclide 99mTc labeled RRL (g2) polypeptide probe and the control peptide were evaluated in vitro and in vivo. [Result] The purity of RRL (g2) and GGG (g2) synthesized by chemical synthesis method was more than 99%, and the labeling rate of radionuclide 99mTc was about 73%. The stability was good. At 30 minutes after intravenous injection of the molecular probe, 99mTc-RRL (g2) had a higher uptake rate in tumor tissue relative to the control peptide 99mTc-GGG (g2), and remained in the tumor tissue for a longer period of time. [Conclusion] Compared with 131I-tRRL, 99mTc-RRL (g2), a novel tumor angiogenic peptide probe, has more advantages in tumor neovascular molecular imaging applications such as increased tumor uptake and is more promising Novel tumor neo-molecular imaging peptide probes.