[Inhibition of protein kinase C by stilbenoids]

The effect of 15 stilbenoids on protein kinase C (PKC) was studied in order to search for naturally occurring PKC inhibitors. All these compounds were isolated from Chinese medicines. Three oligomeric Stilbenes from Caragana sinica, alpha-viniferin, kobophenol A and miyabenol C, were shown to intensely inhibit the activity of partially purified rat brain PKC with IC50 values of 62.5, 52.0, and 27.5 mumol.L-1, respectively. Kinetic analyses revealed that that inhibition was noncompetitive. The Other compounds also showed the effect. Monomer Stilbenes exhibited PKC inhibitory activity at higher mumol.L-1 concentrations than oligomeric Stilbenes. Whenever they are methylated or acetylated perfectly, the inhibition weakens or disappears.