A gallium(III) Schiff base-curcumin complex that binds to amyloid-beta plaques

作者：Lange Jaclyn L; Hayne David J; Roselt Peter; McLean Catriona A; White Jonathan M; Donnelly Paul S

来源：Journal of Inorganic Biochemistry, 2016, 162: 274-279.

DOI：10.1016/j.jinorgbio.2016.02.029

• Gallium(III) complexes
• Gallium radiopharmaceuticals
• Alzheimer's disease
• Diagnostic imaging
• Positron-emission tomography
• Amyloid-beta

Gallium-68 is a positron-emitting isotope that can be used in positron-emission tomography imaging agents. Alzheimer's disease is associated with the formation of plaques in the brain primarily comprised of aggregates of a 42 amino acid protein called amyloid-beta. With the goal of synthesising charge neutral, low molecular weight, lipophilic gallium complexes with the potential to cross the blood brain barrier and bind to A beta plaques we have used an ancillary tetradentate N2O2 Schiff base ligand and the beta-diketone curcumin as a bidentate ligand to give a six-coordinate Ga3+ complex. The tetradentate Schiff base ligand adopts the cis-beta configuration with deprotonated curcumin acting as a bidentate ligand. The complex binds to amyloid-beta plaques in human brain tissue and it is possible that extension of this chemistry to positron-emitting gallium-68 could provide useful imaging agents for Alzheimer's disease.

• 出版日期2016-9