Eight known secondary metabolites were isolated from the methanolic extract of the whole plant of Astragalus lycius Boiss. They were identified as 5,5′-dihydroxy-3′-methoxy-isoflavone-7-O-β-D-glucoside (1), genistin (2), sissotrin (3), 5,4′-dimethoxy-isoflavone-7-O-β-D-glucopyranoside (4), (7S,8R)-5-methoxydehydrodiconiferyl alcohol-4-O-β-D-glucopyranoside (5), 4-O-lariciresinol-glucoside (6), 2-phenylethyl-β-D-glucopyranoside (7) and β-sitosterol-3-O-β-D-glucopyranoside (8) by spectroscopic methods including 1H- and 13C-NMR and HR-MS experiments, and by comparison with literature values. Compounds 1–7 are reported for the first time from Astragalus taxa. All of the compounds were tested for their cytotoxic activities against a number of cancer cell lines. Among them, only 6 exhibited significant activity against human colon carcinoma (HT-29) at 2.69 μM concentration.
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