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[目的]对131I标记的新型环RGD肽二聚体[c(RGD)2]在荷B16和U87两种小鼠肿瘤模型中的生物分布和显像进行研究,以探讨其应用于肿瘤血管生成显像和治疗的可能性。[方法]采用ChT法对c(RGD)2进行131I标记,标记产物经Sephadex G10分离纯化;建立荷黑色素瘤(B16)和荷人神经胶质瘤(U87)的动物模型,进行体内生物分布和显像研究,分析131Ic(RGD)2在不同肿瘤中的摄取差异。[结果]131I对c(RGD)2的标记率为(76.35±2.33)%,经Sephadex G10分离纯化后放射化学纯度达(95.20±3.25)%;静脉注射24h后,131I-c(RGD)2在B16和U87肿瘤中的摄取率分别为(0.18±0.02)ID%/g和(0.30±0.03)ID%/g,两者具有显著统计学差异(P<0.001);肿瘤与肌肉(T/M)摄取比值分别为4.42±1.70与4.29±1.32,肿瘤与血液(T/B)摄取比值分别为2.27±0.45与5.00±0.63。荷B16肿瘤小鼠全身显像在静脉注射24h后可见肿瘤影像,但肿瘤与周围组织对比度较低;而荷U87肿瘤裸鼠全身显像静脉注射3h后即可见清晰的肿瘤影像,随时间延长,肿瘤与周围组织对比度增高。[结论]131I标记的新型环RGD肽二聚体在肿瘤组织中有较高的摄取率,但在不同肿瘤中的摄取有较大的差异,其在U87肿瘤中摄取率更高,对U87肿瘤显像清晰,有可能应用于肿瘤血管生成显像和治疗效果预测。
[Objective] To study the biodistribution and imaging of 131I-labeled novel RGD peptide dimer [c (RGD) 2] in tumor models of B16 and U87-bearing mice to investigate its application in tumor angiogenesis Possibility of imaging and treatment. [Method] 131I-labeled c (RGD) 2 was obtained by ChT method and the product was isolated and purified by Sephadex G10. Animal models of human melanoma (B16) and human glioma (U87) were established. Imaging studies analyzed 131Ic (RGD) 2 uptake in different tumors. [Results] The labeling rate of 131I to c (RGD) 2 was (76.35 ± 2.33)%, and the radiochemical purity was (95.20 ± 3.25)% after purification by Sephadex G10. The uptake rates in B16 and U87 tumors were (0.18 ± 0.02)% ID (ID) / g and (0.30 ± 0.03) ID% / g respectively, with significant difference between the two groups (P <0.001) M uptake were 4.42 ± 1.70 and 4.29 ± 1.32, respectively. The uptake ratios of tumor to blood (T / B) were 2.27 ± 0.45 and 5.00 ± 0.63, respectively. B16 tumor-bearing mice with whole body imaging in 24 hours after intravenous injection of tumor images, but the tumor and surrounding tissue contrast is low; and Dutch nurse U87 tumor nude mice after 3h intravenous injection of clear tumor images can be seen over time, Tumor and surrounding tissue increased contrast. [Conclusion] The 131I-labeled RGD peptide dimer has higher uptake rate in tumor tissue, but the uptake in different tumors is quite different. Its uptake rate in U87 tumor is higher, and the uptake rate of U87 tumor Imaging is clear, it may be applied to tumor angiogenesis imaging and prediction of therapeutic effect.