Bivalent ligands incorporating curcumin and diosgenin as multifunctional compounds against Alzheimer's disease.

ABSTRACT: In an effort to combat the multifaceted nature of Alzheimer's disease (AD) progression, a series of multifunctional, bivalent compounds containing curcumin and diosgenin were designed, synthesized, and biologically characterized. Screening results in MC65 neuroblastoma cells established that compound 38 with a spacer length of 17 atoms exhibited the highest protective potency with an EC50 of 111.7 ± 9.0 nM. A reduction in protective activity was observed as spacer length was increased up to 28 atoms and there is a clear structural preference for attachment to the methylene carbon between the two carbonyl moieties of curcumin. Further study suggested that antioxidative ability and inhibitory effects on amyloid-β oligomer (AβO) formation may contribute to the neuroprotective outcomes. Additi

SUBMITTER: Chojnacki JE 

PROVIDER: S-EPMC4641451 | biostudies-literature | 2015 Nov

REPOSITORIES: biostudies-literature