ACS Medicinal Chemistry Letters
Letter
myocardium with PET.16 However, FDG uptake is influenced
by confounding factors such as individual differences and
myocardial inflammation of infarcted region, which often leads
to false negatives and positives.17 The use of radiolabeled
necrosis-avid probes may provide depiction of infarcted
myocardium to guide clinical decision-making. Compared
with [18F]FDG, necrosis-avid tracers have the following
advantages. First, they were designed with high avidity and
specificity; second, they were not affected by individual
differences and inflammation. Furthermore, imaging necrosis
can avoid functional impairment of salvageable myocardium
caused by the absorption of tracers. Moreover, it may allow
evaluation of patient follow-up and outcome assessment of
revascularization therapies. To the best of our knowledge, this
is the first attempt to label anthraquinone derivatives with 18F
and explore their targetability to necrotic tissues and imaging
necrotic myocardium in vivo by PET. Furthermore, the
possible mechanisms of [18F]FA3OP for necrotic myocardium
were discussed. [19F]FA3OP may bind DNA to achieve
targetability to necrotic myocardium by intercalation in vitro.
In summary, [18F]FA3OP is a promising agent for fast imaging
of necrotic myocardium.
ABBREVIATIONS
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MI/R, myocardial infarction and reperfusion; NAAs, necrosis
avid agents; Hyp, hypericin; SPECT, single photon emission
computed tomography; PET, positron emission tomography;
PEG, polyethylene glyeol; RP-HPLC, reversed-phase high
performance liquid chromatography; Ct-DNA, calf thymus
DNA; EB, ethidium bromide; 18F-FDG, fluorine-18 deoxy-
glucose
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ASSOCIATED CONTENT
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* Supporting Information
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AUTHOR INFORMATION
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Corresponding Authors
ORCID
Author Contributions
A.-Y.J., Q.-M.J., Y.-C.N., J.Z., Z.Y., and Z.-Q.Y. have designed
the studies. A.-Y.J., C.S., L.B., and X.-H.D. have done the
biological experiments. A.-Y.J., Q.-M.J., D.-J.Z., and H.Z. have
performed the chemistry work. All the aforementioned authors
and Z.-P.S. have participated in preparing, editing, and
approving the content of the manuscript.
Funding
This work was partially supported by the National Natural
Science Foundation of China (No. 81501536, 81473120), A
Project Funded by the Priority Academic Program Develop-
ment of Jiangsu Higher Education Institutions, and A Project of
Medical and Health Technology Development Program in
Shandong Province (No.2013WS0354).
Notes
The authors declare no competing financial interest.
ACKNOWLEDGMENTS
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We thank Mrs Shaoli Song for her generous help.
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ACS Med. Chem. Lett. XXXX, XXX, XXX−XXX