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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 33, Number 11
BKCSDE 33(11)
November 20, 2012 

Synthesis and Evaluation of Oleanolic Acid-Conjugated Lactoferrin for β-Amyloid Plaque Imaging
Sung-Min Kim, Dongkyu Kim, Min Kyung Chae, Il-ha Jeong, Jee-Hyun Cho, Naeun Choi, Kyo Chul Lee, Chulhyun Lee*, Eun Kyoung Ryu*
Oleanolic acid, Lactoferrin, Alzheimer’s disease, β-Amyloid, Radioligand
β-Amyloid accumulation in the brain is a pathological hallmark of Alzheimer’s disease (AD). Since early detection of β-amyloid may facilitate more successful and timely therapeutic interventions, many investigators have focused on developing AD diagnostic reagents that can penetrate the blood-brain barrier (BBB). Oleanolic acid (OA) is a substance found in a variety of plants that has been reported to prevent the progression of AD in mice. In this study, we synthesized and evaluated a new radioligand in which OA was conjugated to lactoferrin (Lf, an iron-binding glycoprotein that crosses the BBB) for the diagnosis of AD. In an in vitro study in which OA-Lf was incubated with β-amyloid (1-42) aggregates for 24 h, we found that OA-Lf effectively inhibited β- amyloid aggregation and fibril formation. In vivo studies demonstrated that 123I-OA-Lf brain uptake was higher than123I-Lf uptake. Therefore, radiolabeled OA-Lf may have diagnostic potential for β-amyloid imaging.
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