Potent alpha-glucosidase inhibitors purified from the red alga Grateloupia elliptica.

Diabetes mellitus is a most serious and chronic disease whose incidence rates are increasing with incidences of obesity and aging of the general population over the world. One therapeutic approach for decreasing postprandial hyperglycemia is to retard absorption of glucose by inhibition of alpha-glucosidase. Two bromophenols, 2,4,6-tribromophenol and 2,4-dibromophenol, were purified from the red alga Grateloupia elliptica. IC(50) values of 2,4,6-tribromophenol and 2,4-dibromophenol were 60.3 and 110.4 microM against Saccharomyces cerevisiae alpha-glucosidase, and 130.3 and 230.3 microM against Bacillus stearothermophilus alpha-glucosidase, respectively. In addition, both mildly inhibited rat-intestinal sucrase (IC(50) of 4.2 and 3.6mM) and rat-intestinal maltase (IC(50) of 5.0 and 4.8mM). Therefore, bromophenols of G. elliptica have potential as natural nutraceuticals to prevent diabetes mellitus because of their high alpha-glucosidase inhibitory activity.