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Novel chrysin derivatives as hidden multifunctional agents for anti-Alzheimer's disease: design, synthesis and in vitro evaluation by Chang Liu; Xiaodi Kou; Xi Wang; Jianhua Wu; Aihong Yang; Rui Shen is a Pharmacology, Toxicology and Pharmaceutics article available to read on EtoBox.

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Alzheimer's disease (AD) is the most common type of dementia, the exact etiology of the disease has not been known yet. The use of single-target drugs limits the efficacy of drugs and has certain side effects. In this study, the ‘hidden’ multi-target strategy was used in combination with chrysin's metal chelating site and rivastigmine's anti-cholinesterase pharmacophore to form an ester, which improves the hydrophobicity and protects the phenolic hydroxyl group at the same time. Four derivatives (1-4) were synthesized as the hidden multifunctional agents for AD therapy. Most of the compounds displayed good activities of anti-cholinesterase, antioxidant, appropriate blood brain barrier (BBB) penetration and certain inhibitory activity of β-amyloid (Aβ) aggregation. Compound 3 was demonstrated as the highest selective butyrylcholinesterase (BuChE) inhibitor and targeted both the catalytic active site (CAS) and the peripheral anion site (PAS). And it could be hydrolyzed by BuChE to release chrysin with good ability to chelate Cu2+ and Fe2+. At the same time, phenol fragment can exert its good antioxidant effect. Overall, these findings demonstrated that compound 3 might be considered

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Author

Chang Liu; Xiaodi Kou; Xi Wang; Jianhua Wu; Aihong Yang; Rui Shen

Publisher

Elsevier BV

Published

2021

Language

EN

Field

Pharmacology, Toxicology and Pharmaceutics (Life Sciences)