A bioassay-guided fractionation and chemical investigation of the trunk of Berberis koreana led to the isolation and identification of three new triterpenoids, 2α,3α,19α-trihydroxy-urs-12-en-24-formyl-28-oic acid (1), 2α,3β,21α-trihydroxy-urs-12-en-28-oic acid (2), and 3β-acetyloxy-1-oxo-olean-12-en-28-oic acid (3), along with seven known triterpenoids (4–10). The structures of these new compounds were determined through spectral analysis, including extensive 2D-NMR data. The new compounds 1–3 showed significant cytotoxicity against the A549, SK-OV-3, SK-MEL-2, and HCT-15 human tumor cell lines with IC50 values ranging from 7.17 to 48.73 µM.
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