An [alpha]-glucosidase inhibitor, SKG-3, was isolated from the fruiting bodies of Ganoderma lucidum and its physico-chemical properties were characterized. It was a highly specific and effective reversible inhibitor of [alpha]-glucosidase. It showed very potent inhibitory activity against [alpha]-glucosidase with an IC_50 value of 4.6 mg/ml, but no activity for any other glycosidases tested. Enzyme activity could be recovered upon dialysis, thus providing evidence for the reversibility of the inhibition. A Lineweaver-Burk plot indicated that the SKG-3 inhibition of [alpha]-glucosidase was competitive.