Title : Luminescent Ru(II) Phenanthroline Complexes as a Probe for Real-Time Imaging of Abeta Self-Aggregation and Therapeutic Applications in Alzheimer's Disease - Silva_2016_J.Med.Chem_59_9215 |
Author(s) : Silva DE , Cali MP , Pazin WM , Carlos-Lima E , Salles Trevisan MT , Venancio T , Arcisio-Miranda M , Ito AS , Carlos RM |
Ref : Journal of Medicinal Chemistry , 59 :9215 , 2016 |
Abstract :
The complexes cis-[Ru(phen)(2)(Apy)(2)](2+), Apy = 4-aminopyridine and 3,4-aminopyridine, are stable in aqueous solution with strong visible absorption. They present emission in the visible region with long lifetime that accumulates in the cytoplasm of Neuro2A cell line without appreciable cytotoxicity. The complexes also serve as mixed-type reversible inhibitors of human AChE and BuChE with high active site contact. cis-[Ru(phen)(2)(3,4Apy)(2)](2+) competes efficiently with DMPO by the OH() radical. Luminescence using fluorescence lifetime imaging (FLIM) enables real-time imaging of the conformational changes of the self-aggregation of Abeta with incubation of complexes (0-24 h) in phosphate buffer at micromolar concentrations. By this technique, we identified protofibrills in the self-assembly of Abeta(1-40) and globular structures in the short fragment Abeta(15-21) in aqueous solution. |
PubMedSearch : Silva_2016_J.Med.Chem_59_9215 |
PubMedID: 27668683 |
Silva DE, Cali MP, Pazin WM, Carlos-Lima E, Salles Trevisan MT, Venancio T, Arcisio-Miranda M, Ito AS, Carlos RM (2016)
Luminescent Ru(II) Phenanthroline Complexes as a Probe for Real-Time Imaging of Abeta Self-Aggregation and Therapeutic Applications in Alzheimer's Disease
Journal of Medicinal Chemistry
59 :9215
Silva DE, Cali MP, Pazin WM, Carlos-Lima E, Salles Trevisan MT, Venancio T, Arcisio-Miranda M, Ito AS, Carlos RM (2016)
Journal of Medicinal Chemistry
59 :9215