碘－123-IBOX製備與生物特性研究

Preparation and Biological Characterization of 123Ⅰ-IBOX

張剛瑋(Kang-Wei Chang) ； 李世瑛(Shih-Ying Lee) ； 張家榮(Chia-Jung Chang) ； 黃立宗(Li-Chung Hwang) ； 高弘俊(Hung-Chun Gao) ； 陳家杰(Chia-Chieh Chen)

《核子醫學雜誌》 21卷1期 (2008/03) Pp. 15-20

https://doi.org/10.6332/ANMS.2101.003

摘要

腦中乙型類澱粉質(β-amyloid Aβ)沈積是阿玆海默氏症最明顯的臨床徵兆。針對Aβ正子放射型電腦斷層攝影(PET)與單光子電腦斷層攝影(SPECT)的核醫藥物開發已有許多文獻報導，本研究以碘－123標幟thioflavin T衍生物IBOX，並以Tg2576基因轉殖鼠及同品系對照鼠進行生物實驗。體外試驗發現Tg2576工基因轉殖鼠在海馬迴與前皮質層的碘－123-IBOX攝取分別爲1.67與1.83倍高於對照鼠。microSPECT造影發現Tg2576基因轉殖鼠腦部碘－123-IBOX與周遭組織攝取比值爲2.14，明顯高於對照鼠的1.70。體表外試驗顯示Tg2576基因轉殖鼠在海馬迥與前皮質層的碘－123-IBOX結合分別爲1.07與1.05倍高於對照鼠。研究結果顯示碘－123-IBOX可以作爲偵測阿玆海默氏症腦Aβ沈積的核醫藥物。

關鍵字

阿玆海默氏症 ； 乙型類澱粉質 ； 單光子電腦斷層攝影

並列摘要

Accumulation of β-amyloid (Aβ) plaques in the brain is a characteristic neuropathological event to Alzheimer's disease (AD). There are several radioactive ligands developed for in vivo imaging of Aβ plaques by PET or SPECT. Radioligand 123I-IBOX, 2-(4-dimethylaminophenyl)-6-iodobenzoxazole, a thioflavin T derivative, has been developed by Kung et al to image Aβ plaques in the brain. In this work, 123I-IBOX was prepared as an imaging probe for biological studies in Tg2576 transgenic and control mice. In vitro assay revealed 123I-IBOX uptakes in hippocampus and frontal cortex of Tg2576 mice were 1.67 and 1.83 fold, respectively, higher than those of control. MicroSPECT images showed the uptake ratio of the brain to the reference region in Tg2576 mice (2.14) was higher than that in control mice (1.70). The results of ex vivo assay demonstrated that 123I-IBOX bindings in hippocampus and frontal cortex of Tg2576 mice were 1.07 and 1.05 fold, respectively, higher than those of control. We concluded 123I-IBOX is potential for tracing Aβ plaques in brains of Alzheimer's disease patients.

並列關鍵字

Alzheimer's disease ； β-amyloid ； microSPECT