Title:Bis-iodine-labeled Curcumin as a Potential CT Imaging Agent for
β-amyloid Plaques in the Brain
Volume: 22
Issue: 7
Author(s): Yaqian Dai, Liduo Peng, Xiaoyan Tian, Xingwang Wu, Yuanhong Xu*, Taoshan Jiang*Jinping Qiao*
Affiliation:
- Department of Clinical Laboratory, The First Affiliated Hospital of Anhui Medical University, Hefei, 230000,
Anhui, China
- School of Life Sciences, Anhui Agricultural University, Hefei, 230000, Anhui, China
- Department of Clinical Laboratory, The First Affiliated Hospital of Anhui Medical University, Hefei, 230000,
Anhui, China
Keywords:
Alzheimer's disease, β-amyloid, curcumin, molecular imaging, Probe, BICUR.
Abstract:
Background: Alzheimer's disease (AD) is one of the most common causes of dementia,
affecting many old people.
Objectives: By designing and synthesizing intracerebral imaging probes, we tried to provide a new
solution for the early diagnosis of AD.
Methods: We designed and synthesized bis-iodine-labeled curcumin, and verified its performance
through in vivo and in vitro experiments.
Results: In this study, bis-iodine-labeled curcumin (7, BICUR) was synthesized. In the in vitro mass
spectrum binding assay, Kd values of BICUR with Aβ1-40 and Aβ1-42 aggregates were 46.29 nM and
64.29 nM, respectively. Aβ plaques in AD brain adjacent sections were positively stained by BICUR,
which was similar to some other curcumin derivatives. The Log P value of BICUR was 1.45. In the
biodistribution experiment, BICUR showed the highest initial brain uptake (5.87% compared to the blood
concentration) two minutes after the tail vein injection and rapid clearance from the mouse brain. In the
acute toxicity experiment, BICUR showed low toxicity, and the LD50 was >100 mg/kg. Moreover,
BICUR showed a high stability in vitro (86.68% unchanged BICUR after incubation for 120min in
mouse brain homogenate). Besides, BICUR produced an enhanced CT imaging effect that could be
sensitively detected in vitro, but it also showed an obvious differentiation from surrounding tissues after
intracerebral injection.
Conclusion: All results suggested that BICUR could probably act as a targeted CT imaging agent for
Aβ plaques in the brain.