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同位素  2011 

Re/99Tcm(CO)3+黄酮复合物的合成及其与Aβ斑块的结合特性

, PP. 158-165

Keywords: 99Tcm,Aβ斑块,[Re/99Tcm(CO)3]+黄酮类衍生物

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Abstract:

为研制新型99Tcm(CO)3+标记的黄酮类Aβ显像剂,设计合成了同型Re/99Tcm(CO)3+黄酮类衍生物,用荧光法研究了Re(CO)3+黄酮类衍生物在体外与Aβ斑块的结合特性,并初步观察了其在昆明小鼠体内的生物分布。结果表明,Re(CO)3+黄酮类衍生物的亲和常数(Kd=5.43nmol/L)比放射性碘标记的黄酮类衍生物高。正常小鼠的动物分布结果表明,2min内脑初始摄取较高(0.46±0.23%ID/g),且清除较快(120min时为0.13±0.04%ID/g)。以上结果表明,99Tcm(CO)3+黄酮类衍生物有进一步研究的价值。

References

[1]  Hardy J, Selkoe DJ. The amyloid hypothesis of Alzheimer’s Disease: progress and problems on the road to therapeutics[J]. Sci, 2002, 297 (5 580): 353-356.
[2]  Hardy JA, Higgins GA. Alzheimer’s Disease: the amyloid cascade hypothesis[J]. Sci, 1992, 256(5 054): 184-185. 
[3]  Selkoe DJ. Imaging Alzheimer’s amyloid nat[J]. Biotechnol, 2000, 18 (7): 823824.
[4]  Selkoe DJ. Alzheimer’s Disease: genes, proteins, and therapy[J]. Physiol Rev, 2001, 81(2):741-766.
[5]  Mathis CA, Wang Y, Klunk WE. Imaging betaamyloid plaques and neurofibrillary tangles in the aging human brain[J]. Curr Pharm Des, 2004, 10 (13): 1 469-1 492.
[6]  Nordberg A. PET imaging of amyloid in Alzheimer’s Disease[J]. Lancet Neurol, 2004, 3 (9): 519-527.
[7]  Shoghi-Jadid K, Small GW, Agdeppa ED, et al. Localization of neurofibrillary tangles (NFTs) and betaamyloid plaques (APs) in the brains of living patients with Alzheimer’s Disease[J]. 2002, Am J Geriatr Psychiatry, 10 (1): 24-35.
[8]  Small GW, Kepe V, Ercoli LM, et al. PET of brain amyloid and tau in mild cognitive impairment[J]. N Engl J Med, 2006, 355(25): 2 652-2 663.
[9]  Klunk WE, Engler H, Nordberg A, et al. Imaging brain amyloid in Alzheimer’s Disease with pittsburgh compound-B[J]. Ann Neurol, 2004, 55 (3): 306-319.
[10]  Engler H, Forsberg A, Almkvist O, et al. Two-year follow-up of amyloid deposition in patients with Alzheimer’s Disease[J]. Brain, 2006, 129 (11): 2 856-2 866.
[11]  Verhoeff NPLG, Wilson AA, Takeshita S, et al. In-vivo imaging of Alzheimer’s Disease beta-amyloid with [11C]SB-13 PET[J]. Am J Geriatr Psychiatry, 2004, 12(6): 584-595.
[12]  Ono M, Wilson A, Nobrega J, et al. C11 labeled stilbene derivatives as Aβ aggregate-specific PET imaging agents for Alzheimer’s Disease[J]. Nucl Med Biol, 2003, 30 (6): 565-571.
[13]  Kudo Y, Okamura N, Furumoto S, et al. Styrylbenzoxazole derivatives for in vivo imaging of amyloid plaques in the brain[J]. J Nucl Med, 2007, 48 (4): 553-561.
[14]  [14 ] Jurisson SS, Berning D, Jia W, et al. Coordination compounds in nuclear medicine[J]. Chem Rev, 1993, 93(3): 1 137-1 156.
[15]  Zhuang ZP, Kung MP, Hou C, et al. Biphenyls labeled with technetium-99m for imaging β-amyloid plaques in the brain[J]. Nucl Med Biol, 2005, 32 (2): 171-184.
[16]  Ono M, Watanabe R, Kawashima H, et al. 18F-labeled flavones for in vivo imaging of beta-amyloid plaques in Alzheimer’s brains[J]. Bioorg Med Chem, 2009, 17(5): 2 069-2 076.
[17]  Ono M, Yoshida N, Ishibashi K, et al. Radioiodinated flavones for in vivo imaging of β-amyloid plaques in the brain[J]. J Med Chem, 2005, 48 (23): 7 253-7 260.
[18]  Alberto R, Schibli R, Egli A, et al. A novel Organometallic aqua complex of technetium for the labeling of biomolecules: synthesis of [99Tcm(OH2)3(CO)3]+ from [99TcmO4]- in aqueous solution and its reaction with a bifunctional ligand[J]. J Am Chem Soc, 1998, 120 (31): 7 987-7 988.
[19]  Klunk WE, Jacob RF, Preston MR. Quantifying amyloid β-Peptide (Aβ) aggregation using the congo redAβ (CR-Aβ) spectrophotometric assay[J]. Anal Chem, 1999, 266 (1): 66-76.
[20]  LeVine H, Thioflavine T. Interaction with synthetic Alzheimer’s Disease beta-amyloid peptides: detection of amyloid aggregation in solution[J]. Protein Sci, 1993, 2 (3): 404-410.
[21]  Ono M, Maya Y, Haratake M, et al. Synthesis and characterization of styrylchromone derivatives as betaamyloid imaging agents[J]. Bioorg Med Chem, 2007, 15 (1): 444-450.

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