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Contrast Media & Molecular Imaging
Volume 2018, Article ID 5362329, 9 pages
https://doi.org/10.1155/2018/5362329
Research Article

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

Key Laboratory of Nuclear Medicine of Ministry of Health and Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China

Correspondence should be addressed to Ling Qiu; gro.mnisj@gniluiq and Jianguo Lin; gro.mnisj@ougnaijnil

Received 19 September 2017; Accepted 17 January 2018; Published 5 March 2018

Academic Editor: Yuebing Wang

Copyright © 2018 Hongbo Huang et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Abstract

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.