摘要
目的 探讨放射性核素标记小分子环形多肽RGD 4CY实现肿瘤αvβ3 受体显像的可行性。方法 采用Iodogen法标记、SEP PAKC18柱分离纯化制备12 5I RGD 4CY。测定12 5I RGD 4CY在正常小鼠与荷人QBC93 9胆管癌裸鼠体内的放射性分布 ,计算肿瘤(T)与非肿瘤组织 (TN)放射性比值。进行12 5I RGD 4CY荷瘤动物全身放射自显影。结果 正常小鼠血液放射性清除和肝脏放射性下降迅速 ,肠道无明显增加 ,主要通过肾脏排泄 ,肌肉和肺的放射性 12 0min时分别仅为肝脏的 3 2 %与 44 % (P <0 0 5 )。荷瘤裸鼠各时相肿瘤的放射性均高于肌肉、肠道与肺 (P <0 0 5 ) ,2 40min时T/NT值分别为 2 6.0、8 7与 2 6.0。放射自显影示肿瘤放射性浓聚影最强 ,肺、颈部及其它软组织呈低水平分布。结论 放射性标记RGD 4CY可望成为一有效的肿瘤αvβ3
Objective To investigate the possibility of labeled RGD 4CY with radionuclide to perform tumor αvβ3 receptor scintigraphy. Methods 125 I RGD 4CY was labeled with the Iodogen method and subsequently separated with SEP PAKC18 column. The biodistribution of 125 I RGD 4CY was detected in the normal mice and nude mice bearing human QBC939 cholangiocarcinoma from 10 to 240 min and the autoradiography was performed in tumor bearing nude mice. Results The radioactivity in the blood and liver declined rapidly in the mice, but did not obviously increase in intestine mainly due to elimination through kidneys. The amount of radioactivity in lungs and muscles was only 32% and 44% respectively at 240 min( P <0.05). The radioactivity in tumor was higher than that in muscles, intestines and lungs at all phases in tumor bearing nude mice( P <0.05～0.01). The peak ratio of T/NT occurred at 240 min after injection and were 26.0, 8.7 and 26.0, respectively. Autoradiography showed that the activity of tumor was the highest and there was low level of radioactive distribution in lungs, neck and other soft tissues. Conclusion The radionuclide labeled RGD 4CY is a potential tracer for tumorαvβ3 receptor scintigraphy.
出处
《第三军医大学学报》
CAS
CSCD
北大核心
2002年第11期1340-1342,共3页
Journal of Third Military Medical University
