One-Step 18F-Labeling of Estradiol Derivative for PET Imaging of Breast Cancer

• Main Authors: Hongbo Huang, Ke Li, Gaochao Lv, Guiqing Liu, Xueyu Zhao, Qingzhu Liu, Shanshan Wang, Xi Li, Ling Qiu, Jianguo Lin
• Format: Article
• Language: English
• Published: Hindawi-Wiley 2018-01-01
• Series: Contrast Media & Molecular Imaging
• Online Access: http://dx.doi.org/10.1155/2018/5362329

Positron emission tomography (PET) imaging is a useful method to evaluate in situ estrogen receptor (ER) status for the early diagnosis of breast cancer and optimization of the appropriate treatment strategy. The 18F-labeled estradiol derivative has been successfully used to clinically assess the ER level of breast cancer. In order to simplify the radiosynthesis process, one-step 18F-19F isotope exchange reaction was employed for the 18F-fluorination of the tracer of [18F]AmBF3-TEG-ES. The radiotracer was obtained with the radiochemical yield (RCY) of ~61% and the radiochemical purity (RCP) of >98% within 40 min. Cell uptake and blocking assays indicated that the tracer could selectively accumulate in the ER-positive human breast cancer cell lines MCF-7 and T47D. In vivo PET imaging on the MCF-7 tumor-bearing mice showed relatively high tumor uptake (1.4~2.3 %D/g) and tumor/muscle uptake ratio (4~6). These results indicated that the tracer is a promising PET imaging agent for ER-positive breast cancers.