Synthesis and Evaluation of Oleanolic Acid-Conjugated Lactoferrin for β-Amyloid Plaque Imaging

Bulletin of the Korean chemical society

Eun Kyoung Ryu¹  Naeun Choi¹  Chulhyun Lee¹  Jee-Hyun Cho¹  Sung-Min Kim¹  Il-ha Jeong¹  Kyo Chul Lee¹  Dongkyu Kim¹  Min Kyung Chae¹ 

关键词: Oleanolic acid;    Lactoferrin;    Alzheimer’s disease;    -Amyloid;    Radioligand;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

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.

【 授权许可】

Unknown