Zhang Xiang,Zheng Lei,Xie Laiping,Luo Chaoxue,Li Qianwei,Huang Dingde.Biodistribution and imaging of 188Re-labeled peptides derived from VEGF125-136 in A549 tumor bearing nude mice[J].J Amry Med Univ (J Third Mil Med Univ),2014,36(01):15-19.
Zhang Xiang,Zheng Lei,Xie Laiping,Luo Chaoxue,Li Qianwei,Huang Dingde.Biodistribution and imaging of 188Re-labeled peptides derived from VEGF125-136 in A549 tumor bearing nude mice[J].J Amry Med Univ (J Third Mil Med Univ),2014,36(01):15-19.DOI:
Objective To determine the biodistribution and imaging of VEGF
125-136
-derived peptides (QKRKRKKSRKKH
RKRKRKKSRYIVLS) with
188
Re-labeling in A549 tumor bearing nude mice. Methods Ethylene dicysteine (EC) was used as the bifunctional chelating agent
and the labeling rates were measured by paper chromatography
and stabilities of the
188
Re-peptides were tested in saline and human serum. Biodistribution was studied by injecting labeled peptides through caudal vein of A549 tumor bearing nude mic
e
and the target/non-target radioactivity ratio (T/NT ratio) was measured and calculated. Single photon emission computed tomography (SPECT) was used for the planar imaging of tumor. Results Under the best labeling condition
the 2
188
Re-EC-peptides showed high labeling efficiency of (85.34±2.05)% and (90.9±3.45)% respectively
and good stabilities in saline and human serum. Adding rhenium ammonium acid after the reaction significantly increased the stabilities of the labeled peptides. Biodistribution and SPECT planar imaging showed that high radioactivity concentration was accumulated in the A549 tumor site of the mice. Their T/NT ratios were 5.87±1.30 and 5.46±0.87 respective at 6 h
which were significantly higher than that of VEGF
125-136
(1.75±0.72). Conclusion
188
Re-EC-peptides show high labeling efficiency and high accumulation in A549 tumor tissue
and may be used as tumor-targeting imaging probes and therapy drugs.