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Resveratrol was glucosylated to its 3- and 4'-β-glucosides by the glucosyltransferase PaGT3 from Phytolacca americana expressed in Bacillus subtilis. PaGT3 glucosylated pterostilbene to its 4'-β-glucoside. Piceatannol was converted into its 4'-β-glucoside by PaGT3. Resveratrol 3-β-glucoside showed the inhibitory action of adhesion, migration, and invasion of KB cells. The resveratrol 3-β-glucoside would act as a chemopreventive agent against KB cells. Piceatannol 4'-β-glucoside showed the strongest inhibitory activity among the glycosides toward histamine release from rat peritoneal mast cells. The 4'-β-glucoside of piceatannol would be a potential therapeutic agent for allergic disease. Pterostilbene 4'-β-glucoside showed high phosphodiesterase (PDE) inhibitory activity. The 4'-β-glucoside of pterostilbene could be a potential chemopreventive agent for Alzheimer’s disease.
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