Inhibition of phospholipase Cγ1 by the prenylated flavonoids from Sophora flavescens

Abstract

The effect on the phospholipase Cγ1 activity of eleven prenylated flavonoids from Sophorn flavescens was investigated. These flavonoids exhibited relatively strong inhibitory activity with IC50 values ranged from 7.5 x 10-6M to 35 x 10-6 M with the exception of kushenol H (4) (IC50 value; > 5.3 x 10-4M). The presence of C3-OH resulted in a significant diminution of activity and the configuration of C3-OH is likely to be another factor influencing the activity. In addition, hydration of the C-4'''-C-5''' double bond of the lavandulyl side chain caused complete loss of activity. These data suggest that the presence and configuration of C3-OH are related to the inhibitory activity and the lavandulyl side chain is also important for high inhibitory activity against PLCγ1.