American Chemical Society
mp0c00677_si_001.pdf (1.7 MB)

A Glycosylated Prodrug to Attenuate Neuroinflammation and Improve Cognitive Deficits in Alzheimer’s Disease Transgenic Mice

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journal contribution
posted on 2020-11-26, 13:33 authored by Mingeun Kim, Min Hee Park, Geewoo Nam, Misun Lee, Juhye Kang, Im-Sook Song, Min-Koo Choi, Hee Kyung Jin, Jae-sung Bae, Mi Hee Lim
We report a prodrug, Glu-DAPPD, to overcome the shortcomings of an anti-neuroinflammatory molecule, N,N′-diacetyl-p-phenylenediamine (DAPPD), in biological applicability for potential therapeutic applications. We suspect that Glu-DAPPD can release DAPPD through endogenous enzymatic bioconversion. Consequently, Glu-DAPPD exhibits in vivo efficacies in alleviating neuroinflammation, reducing amyloid-β aggregate accumulation, and improving cognitive function in Alzheimer’s disease transgenic mice. Our studies demonstrate that the prodrug approach is suitable and effective toward developing drug candidates against neurodegeneration.