新型肺癌分子探针^18F-氟丙酰-Lladtthhrpwt的合成及其小动物PET显像

目的制备^18F-氟丙酰．Lladtthhrpwt（18F-FP-ZS-6），并观察其在荷人肺腺癌NCI-H1299裸鼠体内分布。方法利用噬菌体随机展示肽库筛选实验得到多肽Lladtthhrpwt（zs-6），基于氟多功能化学合成模块PET．MF-2V-IT-I合成常用辅助基团18F-2-氟丙酸对硝基苯酯（NFP），再与多肽zs-6反应得到18F．FP-ZS-6。将纯化后的18F-FP-ZS-6通过尾静脉注入荷人肺腺癌NCI-H1299裸鼠体内，进行microPET显像。结果成功制备18F-FP-ZS-6。其衰减校正后总产率为（5-2）％（n=3），放化纯〉95％。Micr0PET显示18F-FP-ZS-6在荷瘤裸鼠肿瘤与腹部呈高摄取，在注射后5、15、25、35、45、55、65、75和85min时，肿瘤摄取值分别为0．329、0．350、0．405、0．433、0．420、0．415、0．402、0．403、0．390％ID／g；在注射后35min达最高，随后缓慢减少。结论成功制备18F-FP-ZS-6，其在荷人肺腺癌裸鼠肿瘤中有-定聚集．有可能作为人肺腺癌显像剂。

Synthesis of 18F-FP-Lladtthhrpwt as a new probe for the detection of lung cancer by microPET

Objective To prepare 18 F-2-fluoropropionyl （ FP ） -Lladtthhrpwt （ ts F-FP-ZS-6） by a multifunetional l18F radiolabeling module and investigate its in vivo distribution in human lung cancer cell （NCI-H1299）-bearing nude mice by mieroPET. Methods Using a phage display peptide library to screen and identify Lladtthhrpwt （ZS-6） which has an affinity for human lung cancer. PET-MF-2V-IT-I synthesizer was used for the synthesis and purification of I18F-FP-ZS-6. MicroPET studies were carried out in NCI- H1299-bearing nude mice after injection of I18F-FP-ZS-6. Results 4-nitrophenyl 2-[ 18F]fluoropropionate （l18F-NFP） was prepared by ＂ one-pot＂ radiochemical procedure. The radiochemical yield of l18F-FP-ZS-6 was （5＋2）% （n=3, decay-corrected） from t18F and the radiochemical purity was more than 95%. Micro- PET studies showed that the uptake of 18F-FP-ZS-6 was high in the tumor and stomach of NCI-H1299-bear ing nude mice model. The tumor uptake of I18F-FP-ZS-6 was 0.329, 0.350, 0.405, 0.433, 0.420, 0.415, 0. 402, 0.403, 0.390 %ID/g at 5, 15, 25, 35, 45, 55, 65, 75, 85 min post-injection, respectively. The tumor uptake peak was at 35 min post-injection and then 18F-FP-ZS-6 was cleared slowly. Conclusions 18F- FP-ZS-6 could be successfully prepared. It might be a ootential tracer for imazinz human lun cancer.