β-Amyloid aggregation induced by human acetylcholinesterase: inhibition studies

Synthesis and Multitarget Biological Profiling of a Novel Family of Rhein Derivatives As Disease-Modifying Anti-Alzheimer Agents

“…The inhibitory activity of these hybrids and the parent rhein and huprine Y against the AChE-induced aggregation of Aβ40 was assessed using a thioflavin T-based fluorescent method. 49 Rhein-huprine hybrids exhibited a significant inhibitory activity against the AChE-induced Aβ40 aggregation, exhibiting percentages of inhibition ranging from 29 to 52% at a 100 μM concentration, which are clearly superior to that found for the AChE's CAS inhibitor huprine Y, 4 (Table 1). These activities are similar to those reported for other families of dual binding site AChEIs, 40,[50][51][52][53][54][55] even though more potent inhibitors of the AChE-induced Aβ40 aggregation have been described.…”

“…AChE-Induced Aβ40 Aggregation Inhibition Assay. 49 Thioflavin T(Basic Yellow 1), human recombinant AChE lyophilized powder, and 1,1,1,3,3,3-hexafluoro-2-propanol (HFIP)…”

Thioflavin-S Staining of Bacterial Inclusion Bodies for the Fast, Simple, and Inexpensive Screening of Amyloid Aggregation Inhibitors

“…Usually, the screening of inhibitors of A aggregation is carried out in vitro using expensive synthetic peptides and thioflavin-T (Th-T)-based fluorometric assays involving a variety of experimental conditions [18][19][20][21][22]. Even in vitro, A aggregation itself is a difficult process to study, inasmuch as it is highly sensitive to a number of factors including purity and experimental conditions such as solvents or buffers used or mixing conditions [16].…”

Study of the interaction of Huperzia saururus Lycopodium alkaloids with the acetylcholinesterase enzyme

“…a dual-site inhibitor) were able to prevent the aggregating activity of AChE toward A as well as the hydrolysis of acetylcholine. [18] Therefore, inhibitors with the dual-site binding mode have recently been presented as a new therapeutic option. [6] Page 4 of 23 A c c e p t e d M a n u s c r i p t Figure 1.…”