Deglycosylation of stilbene glucoside compounds improves inhibition of 3-hydroxy-3-methylglutaryl coenzyme a reductase and squalene synthase activities

Abstract

The glycosylated stilbenes mulberroside A and rhapontin were converted to their aglycones (oxyresveratrol and rhapontigenin) by enzymatic transformation. Rhapontin, rhapontigenin, mulberroside A, oxyresveratrol-3-O-glucoside, and oxyresveratrol showed inhibitory activities against 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase and squalene synthase, which are key enzymes in the cholesterol biosynthesis pathway. Aglycones showed stronger inhibitory activities than their glycosylated counterparts, and methoxylated stilbenes were stronger inhibitors of both enzymes than non-methoxylated stilbenes. The inhibitory activities of the stilbene compounds were significantly different from that of a negative control group (p < 0.05).