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CC BY-NC-ND 4.0 · SynOpen 2022; 06(02): 80-85
DOI: 10.1055/a-1818-8330
paper

Radiosynthesis and Tumor MicroPET/CT Imaging of 18F-Fluoro­ethoxylerianin, an 18F-Labeled Erianin Analogue

Hui Nie‡
a   Department of Pharmaceutical Engineering, School of Chemical and Environmental Engineering, Shanghai Institute of Technology, Shanghai 201418, P. R. of China
b   Shanghai Engineering Research Center of Green Fluoropharmaceutical Technology, Shanghai 201418, P. R. of China
,
Nian Wang‡
c   Department of Nuclear Medicine, Fudan University Shanghai Cancer Center, 270 Dong’An Road, Shanghai 200032, P. R. of China
d   The Education Ministry Key Lab of Resource Chemistry and Shanghai Key Laboratory of Rare Earth Functional Materials, Shanghai Normal University, 100 Guilin Road, Shanghai, 200234, P. R. of China
,
Jinwen Huang  ∗
a   Department of Pharmaceutical Engineering, School of Chemical and Environmental Engineering, Shanghai Institute of Technology, Shanghai 201418, P. R. of China
b   Shanghai Engineering Research Center of Green Fluoropharmaceutical Technology, Shanghai 201418, P. R. of China
,
Zhuang Ni
a   Department of Pharmaceutical Engineering, School of Chemical and Environmental Engineering, Shanghai Institute of Technology, Shanghai 201418, P. R. of China
b   Shanghai Engineering Research Center of Green Fluoropharmaceutical Technology, Shanghai 201418, P. R. of China
,
Kangyan Xue
a   Department of Pharmaceutical Engineering, School of Chemical and Environmental Engineering, Shanghai Institute of Technology, Shanghai 201418, P. R. of China
b   Shanghai Engineering Research Center of Green Fluoropharmaceutical Technology, Shanghai 201418, P. R. of China
,
Lixing Song
a   Department of Pharmaceutical Engineering, School of Chemical and Environmental Engineering, Shanghai Institute of Technology, Shanghai 201418, P. R. of China
b   Shanghai Engineering Research Center of Green Fluoropharmaceutical Technology, Shanghai 201418, P. R. of China
,
Mingwei Wang∗
c   Department of Nuclear Medicine, Fudan University Shanghai Cancer Center, 270 Dong’An Road, Shanghai 200032, P. R. of China
,
Fanhong Wu∗
a   Department of Pharmaceutical Engineering, School of Chemical and Environmental Engineering, Shanghai Institute of Technology, Shanghai 201418, P. R. of China
b   Shanghai Engineering Research Center of Green Fluoropharmaceutical Technology, Shanghai 201418, P. R. of China
› Author AffiliationsThis research was supported by the National Natural Science Foundation of China (grant numbers 21172148, 216721521, 21771041).
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Abstract

Erianin is an active constituent of Dendrobium candidum. In this work, 18F-fluoroethoxylerianin ([18F]FEE), a 18F-Labeled erianin analogue, was designed and synthesized to evaluate the properties of erianin and related analogues by in vivo PET imaging. The initial product was separated and purified by liquid-phase separation module Explora LC and simple homemade solid-phase extraction, and high purity [18F]FEE was finally obtained. The radiochemical purity of [18F]FEE was determined by Radio-TLC and Radio-HPLC. [18F]FEE showed good stability in normal saline and serum, and could be quickly eliminated from mice. Cell experiments, biological distribution, and small-animal PET/CT further showed that [18F]FEE had a high uptake rate in HepG2 tumor cells, and showed good imaging ability in a HepG2 tumor model. The results of this study indicate that the synthesized 18F-labeled erianin analogue is an effective new probe for positron emission tomography (PET) imaging of HepG2 hepatocellular carcinoma, which provides an intuitive and reliable theoretical basis for the development of erianin as an anticancer drug.

Keywords

fluorine-18 - radiosynthesis - microPET/CT - tumors - erianin

Supporting Information

    Supporting information for this article is available online at https://doi.org/10.1055/a-1818-8330. Included are 1H, 13C and 19F NMR spectra, HPLC elution conditions and traces.
  • Supporting Information


Publication History

Received: 12 March 2022

Accepted after revision: 05 April 2022

Accepted Manuscript online:
06 April 2022

Article published online:
25 April 2022

© 2022. The Author(s). This is an open access article published by Thieme under the terms of the Creative Commons Attribution-NonDerivative-NonCommercial-License, permitting copying and reproduction so long as the original work is given appropriate credit. Contents may not be used for commercial purposes or adapted, remixed, transformed or built upon. (https://creativecommons.org/licenses/by-nc-nd/4.0/)

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