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.