F-18 labeled vasoactive intestinal peptide analogue in the PET imaging of colon carcinoma in nude mice.
As large amount of vasoactive intestinal peptide (VIP) receptors are expressed in various tumors and VIP-related diseases, radiolabeled VIP provides a potential PET imaging agent for VIP receptor. However, structural modification of VIP is required before being radiolabeled and used for VIP receptor imaging due to its poor in vivo stability. As a VIP analogue, [R(8, 15, 21), L(17)]-VIP exhibited improved stability and receptor specificity in preliminary studies. In this study, F-18 labeled [R(8,15,21), L(17)]-VIP was produced with the radiochemical yield being as high as 33.6% ± 3% (decay-for-corrected, n = 5) achieved within 100 min, a specific activity of 255 GBq/ μmol, and a radiochemical purity as high as 99% as characterized by radioactive HPLC, TLC, and SDS-Page radioautography. A biodistribution study in normal mice also demonstrated fast elimination of F-18 labeled [R(8,15,21), L(17)]-VIP in the blood, liver, and gastrointestinal tracts. A further micro-PET imaging study in C26 colon carcinoma bearing mice confirmed the high tumor specificity, with the tumor/muscle radioactivity uptake ratio being as high as 3.03 at 60 min following injection, and no apparent radioactivity concentration in the intestinal tracts. In addition, blocking experiment and Western Blot test further confirmed its potential in PET imaging of VIP receptor-positive tumor.
Department of Nuclear Medicine, Zhongshan Hospital, Fudan University, Shanghai 200032, China ; Shanghai Institute of Medical Imaging, Shanghai 200032, China.
Dengfeng
D
Cheng
Shanghai Institute of Applied Physics, Chinese Academy of Sciences, Shanghai 201800, China.
Yuxia
Y
Liu
Shanghai Institute of Applied Physics, Chinese Academy of Sciences, Shanghai 201800, China.
Hua
H
Shen
Department of Nuclear Medicine, Zhongshan Hospital, Fudan University, Shanghai 200032, China ; Shanghai Institute of Medical Imaging, Shanghai 200032, China.
Lifang
L
Pang
Shanghai Institute of Applied Physics, Chinese Academy of Sciences, Shanghai 201800, China.
Duanzhi
D
Yin
Shanghai Institute of Applied Physics, Chinese Academy of Sciences, Shanghai 201800, China.
Yongxian
Y
Wang
Department of Respiratory Medicine, Zhongshan Hospital, Fudan University, Shanghai 200032, China.
Shanqun
S
Li
Department of Nuclear Medicine, Zhongshan Hospital, Fudan University, Shanghai 200032, China ; Shanghai Institute of Medical Imaging, Shanghai 200032, China.
Hongcheng
H
Shi
D000818:Animals; D002277:Carcinoma / Q000175:diagnosis* / Q000000981:diagnostic imaging / Q000473:pathology; D003110:Colonic Neoplasms / Q000175:diagnosis* / Q000000981:diagnostic imaging / Q000473:pathology; D003952:Diagnostic Imaging / Q000379:methods; D004958:Estradiol / Q000031:analogs & derivatives; D006801:Humans; D051379:Mice; D008819:Mice, Nude; D049268:Positron-Emission Tomography; D011859:Radiography; D014660:Vasoactive Intestinal Peptide
D014660:Vasoactive Intestinal Peptide; D004958:Estradiol; C043436:16-fluoroestradiol