ASBI (APP-Selective BACE inhibitors) represent a novel class of candidate therapeutic agents for Alzheimer’s disease. A systematic approach was used to identify ASBIs and to evaluate their in vivo ability to modulate APP processing selectively. We identified a bioflavonoid nutritional supplement, galangin, as a molecular lead that acts as an ASBI in cell models, and have shown that increasing brain levels of this bioflavonoid through a pro-drug approach leads to reduction of Aβ42 in an Alzheimer’s disease mouse model. Given that even a partial specific reduction of BACE could have dramatic effects on plaque load, this bioflavonoid and its pro-drug became object of interest for further evaluation. We are in the process of testing new delivery approaches of galangin to the brain in the AD mouse model, these results will be discussed. Our study indicates that a bioflavonoid has the ability to bind APP and inhibit the BACE cleavage of APP and APLP2, thus suggesting that they may be APP /APLP2-selective BACE inhibitors.

Natural product galangin is an APP-Selective BACE inhibitor and is a potential agent to treat Alzheimer’s disease

251st National Meeting (2016)

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