铼[^(188)Re]羰基化合物标记含RGD的环肽及其生物分布

Radiolabeling and biodistribution of RGD peptide with ^(188)Re-tricarbonyl complex

以fac-[188Re(CO)3(H2O)3]+为前体标记了含RGD的环形多肽,并对其在普通小鼠和荷S180肉瘤小鼠体内的生物分布作了初步研究。铼[188Re]羰基化合物标记含RGD环肽标记方法简单易行,75℃反应30min,标记率在90%以上。不会引起红细胞的溶血和凝聚现象,普通小鼠和荷S180肉瘤小鼠的生物分布实验表明,标记肽主要通过泌尿系统和肝胆代谢两个途径清除,1、4、24和48h肿瘤/肌肉比分别为:(4.4075±0.1139)、(5.1510±0.5375)、(4.4727±0.4895)和(4.8788±3.16)。

Three amino acids residues of Arg-Gly-Asp （RGD） are often the primary site of recognition by integrins which are responsible for tumor invasion and metastasis. In this research, one peptides containing RGD： HCRGD（D） FC were radiolabeled with ^188Re-wicarbonyl complex. High radiolabeling ratios （〉90%） were achieved under the reaction condition of 75℃, 30min. The radiolabeled peptide got high stability in PBS at room temperature for 4 hours. The hemolysis of red blood cells was not observed during incubation at 37℃ for 3 hours. Biodistribution studies were performed in normal male mice and S180-bearing mice, respectively. The radioactivities were rapidly eliminated by the hepatobiliary and urinary systems. Tumor/Muscle ratios were 4.4075±0. 1139, 5.1510±0.5375, 4.4727±0.4895 and 4.8788±3.16 at 1h, 4h, 24h and 48h after injection. The results showed that ^188Re-tricarbonyl peptide containing RGD was a potential agent for tumor treatment.