摘要
探讨了放射性碘标记血管活性肠肽（VIP）实现肿瘤VIP受体显像的可能性。应用氯胺-T法标记、SephadexG－50柱层析分离纯化制备125I－VIP，硅胶TLC与体外竞争结合实验检测标记VIP的稳定性与生物活性；研究125I－VIP在荷SGC7901裸鼠体内分布。结果显示：125I标记率为73．8％；标记VIP的比活度为18．2PBq／mol；放化纯为98％，-80℃贮存48天后为96．3％；VIP以剂量依赖方式抑制125I-VIP与SGC7901细胞结合；各时相肿瘤放射性均高于肌肉（P＜0.05—0.01），高峰摄取时间为30min（3．58±0．48％ID／g），T／N峰比值（3.05）出现于60min；肺放射性高于血液（P＜0．05），肠道放射性始终处于低水平；体内放射性主要经肾脏排泄。本研究表明放射性核素标记VIP可望成为一有效的肿瘤VIP受体显像剂。
To study the possibility of radioactive labelled vasoactive intestinal peptiede (VIP) for tumor VIP receptor imaging. 125I-VIP was prepared by chloramine-T method, and purified by sephadex G-50 column chromatography. The bioactivity and stability of 125I-VIP were measured by silica 60 F254 TLC and competition test to SGC7901 cell in vitro. The biodistribution of 125I-VIP was studied in the nude mice bearing tumor. The results showed that labelled rate of 125I was 73.8%, the specific activity was 18.2PBq/mol, the radiochemical purity(RCP) was over 98% and remained 96.3% after 48 days stored at m80oC. The specific binding of 125I-VIP to the SGC7901 cell was inhibited by VIP in dose dependence in the competition experiment. The radioactivity of tumor was higher than that of muscles in all phases (P<0.05-0.01),the peak activity of tumor occured at 30min (3.58 ± 0.48ID%/g) and the peak ratio of T/N occured at 60min after the injection. The activity of lungs was obviously higher than that of blood, the intestine was always in low level. Most of the activity in the body was mainly eliminated from kidney. The present study demonstrated that the radioactive labelled VIP is a promosing agent for tumor VIP receptor scintigraphy.
出处
《核技术》
CAS
CSCD
北大核心
1998年第11期641-644,共4页
Nuclear Techniques
基金
国家自然科学基金
关键词
血管活性肠肽
药物分布
肿瘤
受体分析
碘标记
VIP,Pharmacological distribution, Tumor, Gastric tumor, Animal,Receptor analysis
