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Cirsium setosum ( C. setosum ) has a potential antihyperglycemic effect, but it is unclear what bioactive components play a key role. According to the α -glucosidase inhibition activity, three new taraxastane-type triterpenoids of 3 β -hydroxy-30-hydroperoxy-20-taraxastene ( 1 ), 3 β -hydroxy-22 α -methoxy-20-taraxastene ( 2 ), and 30-nor-3 β ,22 α -dihydroxy-20-taraxastene ( 3 ), as well as five known taraxastane triterpenoids of 3 β ,22-dihydroxy-20-taraxastene ( 4 ), 20-taraxastene-3,22-dione ( 5 ), 3 β -acetoxy-20-taraxasten-22-one ( 6 ), 3 β -hydroxy-20-taraxasten-22-one ( 7 ), and 30-nor-3 β -hydroxy-20-taraxastene ( 8 ) were obtained from the petroleum ether-soluble portion of the ethanol extract from C. setosum . All chemical structures of the compounds were elucidated by spectroscopic data analysis and compared with literature data. Compounds 4 - 8 were identified for the first time from this plant, and compounds 1 , 2 , 4, and 7 exhibited more potent α -glucosidase inhibitory activity-with IC 50 values of 18.34 ± 1.27, 26.98 ± 0.89, 17.49 ± 1.42, and 22.67 ± 0.25 μM, respectively-than acarbose did (positive control, IC 50 42.52 ± 0.32 μM).

Bioassay-Guided Isolation of Triterpenoids as α-Glucosidase Inhibitors from Cirsium setosum