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Deprecated: Implicit conversion from float 263.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 ACS+Chem+Neurosci 2013 ; 4 (6): 924-9 Nephropedia Template TP
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Biological Activity of sym-Triazines with Acetylcholine-like Substitutions as Multitarget Modulators of Alzheimer?s Disease #MMPMID23472585
Veloso AJ; Chow AM; Dhar D; Tang DF; Ganesh HV; Mikhaylichenko S; Brown IR; Kerman K
ACS Chem Neurosci 2013[Jun]; 4 (6): 924-9 PMID23472585show ga
The bioactivities of two novel compounds (TAE-1 and TAE-2) that contain a sym-triazine scaffold with acetylcholine-like substitutions are examined as promising candidate agents against Alzheimer?s disease. Inhibition of amyloid-? fibril formation in the presence of A?1?42, evaluated by Thioflavin T fluorescence, demonstrated comparable or improved activity to a previously reported pentapeptide-based fibrillogenesis inhibitor, iA?5p. Destabilization of A?1?42 assemblies by TAE-1 and TAE-2 was confirmed by scanning electron microscopy imaging. sym-Triazine inhibition of acetylcholinesterase (AChE) activity was observed in cytosol extracted from differentiated human SH-SY5Y neuronal cells and also using human erythrocyte AChE. The sym-triazine derivatives were well tolerated by these cells and promoted beneficial effects on human neurons, upregulating expression of synaptophysin, a synaptic marker protein, and MAP2, a neuronal differentiation marker.