TY - JOUR
T1 - A fluorinated azine as a versatile scaffold for the development of Cu(II)-specific multi-functional imaging probes
AU - Ye, Weijian
AU - Xie, Mengting
AU - Wei, Junjie
AU - Li, Guocong
AU - Tang, Yongjin
AU - Hou, Lu
AU - Wang, Lu
AU - Yu, Huijuan
AU - Lee, Chi Sing
AU - Xu, Hao
N1 - Funding Information:
The authors gratefully acknowledge the support of K.C. Wong Education Foundation (China) , and the Project of Innovative Team for the Guangdong Universities ( 2018KCXTD001 , China). This work was financially supported by Postdoctoral Fund of the First Affiliated Hospital, Jinan University (No. 809028 ), Hong Kong Baptist University ( RC-SGT2/18-19/SCI/005 and RC-ICRS-18-19-01A ), the National Natural Science Foundation of China (Nos. 81871383 and 82071974 ), Guangdong Basic and Applied Basic Research Foundation ( 2020A1515011192 , China) and the Fundamental Research Funds for the Central Universities ( 21619104 ). We thank Jianzhou Li from Ge healthcare for the assistant on radio labeling and supplying Fig. S13.
Publisher Copyright:
© 2021 Elsevier B.V.
PY - 2021/9/15
Y1 - 2021/9/15
N2 - Copper is vital to many physiological activities, and its dyshomeostasis is related to cancers as well as neurodegenerative diseases. Copper targeting probes with single imaging modality have been extensively reported and employed in specific aspects. Herein, we delineate the development of Cu(II)-specific multi-functional imaging probes based on a fluorinated azine FN. The azine selectively binds to a Cu2+ ion, forming a 1:1 FN-Cu2+ complex, and induces a substantial fluorescence quenching, which can be resumed upon addition of H2S (Na2S as the source of H2S). The binding of the paramagnetic Cu2+ ions also leads to the relaxation enhancement of the 19F nuclei in the FN-Cu2+ complex and improve the signal-to-noise ratio of the phantom images. The 18F-radiolabeled analogue, [18F]FN, is synthesized for the first time and used in PET/CT imaging on cynomolgus for a preliminary study of pharmacokinetics.
AB - Copper is vital to many physiological activities, and its dyshomeostasis is related to cancers as well as neurodegenerative diseases. Copper targeting probes with single imaging modality have been extensively reported and employed in specific aspects. Herein, we delineate the development of Cu(II)-specific multi-functional imaging probes based on a fluorinated azine FN. The azine selectively binds to a Cu2+ ion, forming a 1:1 FN-Cu2+ complex, and induces a substantial fluorescence quenching, which can be resumed upon addition of H2S (Na2S as the source of H2S). The binding of the paramagnetic Cu2+ ions also leads to the relaxation enhancement of the 19F nuclei in the FN-Cu2+ complex and improve the signal-to-noise ratio of the phantom images. The 18F-radiolabeled analogue, [18F]FN, is synthesized for the first time and used in PET/CT imaging on cynomolgus for a preliminary study of pharmacokinetics.
KW - F magnetic resonance
KW - Azine
KW - Copper ion
KW - Fluorescent probe
KW - Positron emission tomography
UR - http://www.scopus.com/inward/record.url?scp=85105751559&partnerID=8YFLogxK
U2 - 10.1016/j.snb.2021.130106
DO - 10.1016/j.snb.2021.130106
M3 - Journal article
AN - SCOPUS:85105751559
SN - 0925-4005
VL - 343
JO - Sensors and Actuators B: Chemical
JF - Sensors and Actuators B: Chemical
M1 - 130106
ER -
