The enzymatic regioselective acylation of resveratrol was achieved in organic solvents catalyzed by the lipase from Candida sp. 99-125 (CSL) under microwave irradiation. Influences of various reaction conditions have been studied. After selecting the optimum conditions [MTBE (20ml, a(w)=0.38), resveratrol (0.1mmol), vinyl acetate (1.0mmol) and CSL (100.0mg) under microwave irradiation (35 degrees C, 400 W)], CSL exhibited a satisfied enzyme activity (281 +/- 11mol/g/h) and yield of 75% for 4-O-acetyl- resveratrol could be obtained in about 4h when performing the reaction on a 25-fold-larger scale. [GRAPHICS] Schematic illustration of the enzymatic regioselective acylation of resveratrol catalyzed by the lipase from Candida sp. 99-125 (CSL) under microwave irradiation.