The clove ellagitannins and their related polygalloylglucoses inhibited mal
tase activity of rat intestinal alpha -glucosidases. The structure-activity
relationship study of those galloylglucoses, varying the extent of galloyl
ation on the glucose core, with the ellagitannins, indicated that an increa
sing number of galloyl units in the molecule lead to an increase in the inh
ibitory activity. Penta-O-galloyl-beta -D-glucose, with five galloyl groups
showed the highest inhibitory activity. On the other hand, hexahydroxydiph
enoyl units contained in the ellagitannins had little effect on the activit
y. After separation of maltase-glucoamglaas and sucrase-isomaltase complexe
s from the crude mixture of the rat alpha -glucosidases, the inhibitory act
ivities of the galloylglucose derivatives against each complex were examine
d. The inhibitory influence on the maltase-glucoamylase complex was more po
tent than on the sucrase-isomaltase complex.