Inhibition of proteasome activity by anthocyanins and anthocyanidins

Recent reports have demonstrated multiple benefits associated with the consumption of berry fruits, including a decreased vulnerability to oxidative stress, reduced ischemic brain damage, protection of neurons from stroke-induced damage and the reversal of age-related changes in brain and behaviour. Berry fruits contain high amounts of anthocyanins, which play a major role as free radical scavengers. The present study addresses proteasome inhibition as a further mechanism by which anthocyanins and their aglycons, the anthocyanidins, may exert health-promoting effects. HL-60 cells were incubated with 19 test substances and inhibition of the chymotrypsin-like enzyme activity was determined in a chemiluminescent assay. Anthocyanins and their aglycons achieved IC50 values ranging from 7.8 mu M for kaempferidinidin and pelargonidin, to 32.4 mu M for delphiniclin. Thus proteasome inhibitory properties of anthocyanins may contribute to their known anticarcinogenic, antioxidative, anti-inflammatory and neuroprotective activities, rationalizing dietary supplementations with anthocyanins in the prevention and treatment of chronic diseases, including neurodegenerative disorders. (C) 2008 Elsevier Inc. All rights reserved.