Rutin (quercetin-3-O-rutinoside) is a multifunctional natural flavonoid glycoside with profound effects on the various cellular functions under pathological conditions. Due to the ability of rutin and/or its metabolites to cross the blood brain barrier, it has also been shown to modify the cognitive and various behavioral symptoms of neurodegenerative diseases. In this review, its therapeutic potential for Alzheimer's disease (AD) is evaluated through appraisal of current literatures relevant to the various cellular and molecular targets of the disease. Among the most relevant mechanisms involved are effect on amyloid beta (Aβ) processing, aggregation and action; alteration of the oxidant-antioxidant balance associated with neuronal cell loss; removing the inflammatory component of neurodegeneration, etc. The effect of rutin resulting from its physicochemical features related to effects like metal chelation and bioavailability are also discussed.