Methanol extract from
Arctium lappa L. showed an inhibitory activity of α-glucosidase. The methanol extract was re-extracted with ethyl acetate and water. The ethyl acetate extract showed inhibitory activity. The inhibitory compound was isolated from the ethyl acetate extract and identified as sitosterol-β -D-glucopyranoside (
1) by EI-MS, FAB-MS, IR,
1H and
13C NMR spectroscopy. Compound
1 inhibited 97.3% of α-glucosidase activity at a concentration of 200.0 μ mol/mL, and the ID
50 (50% inhibition dose) value was 30 μ mol/mL. In addition, the inhibitory compounds from the ethyl acetate extract were also identified as methyl palmitate (
2), methyl linoleate (
3) and methyl linoleneate (
4) by GC-MS analysis. Compound
2-
4 inhibited 73.4%, 66.5% and 68.5% of α-glucosidase activity at a concentration of 200 μ mol/mL, and the ID
50 values were 52.8, 47.5 and 46.7 μ mol/mL. To research the structure-activity relationship, methyl steareate (
5), methyl oleate (
6), palmitic acid (
7), linoleic acid (
8), linolenic acid (
9), stearic acid (
10) and oleic acid (
11) were also assayed.
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