摘要

Methanolic extracts from the medicinal parts of 50 traditional Chinese herbs were tested in screening experiments for rat intestinal alpha-glucosidase. The methanolic extract from flower buds of Tussilago farfara L. (Compositae) showed the highest maltase inhibitory activity, with maltose as a substrate. Enzyme assay-guided fractionation of this extract afforded. 3,4-dicaffeoylquinic acid (1), 3,5-dicaffeoyl-quinic acid (2), 4,5-dicaffeoylquinic acid (3) and rutin (4), and the structures of these compounds were elucidated on the basis of MS and NMR data analyses. Compounds 1, 2 and 3 showed comparative maltase inhibitory activities, and the IC50 values were 0.91 mM, 0.90 mM and 0.89 mM, respectively. Comparison of the activities of 1-3, chlorogenic acid (5), quinic acid (6) and caffeic acid (7) suggested that the number of caffeoyl groups attached to a quinic acid core were important for the potency. Rutin (4) showed moderate activity and inhibited 41 % of maltase activity at a concentration of 1 mM. This is the first report on mammalian alpha-glucosidase inhibition of T farfara and the isolation of 1, 2 and 3 from this herb species. These results suggest a use of the extract of T farfara for antidiabetes.