Cytotoxic steroidal saponins from Ophiopogon japonicus

Four new steroidal saponins, named ophiopogonin P–S (1–4), together with eleven known ones (5–15) were isolated from the tuberous roots of Ophiopogon japonicus. Their structures were elucidated by spectroscopic and chemical analysis. Compounds 2–15 were evaluated for their cytotoxic activity against five human tumor cell lines (HepG2, HLE, BEL7402, BEL7403 and Hela). Compounds 2, 5, 6, 8 and 9 were cytotoxic for all cell lines tested. Compounds 7, 11 and 15 showed selective cytotoxicity against some of the cell lines. The structure–activity relationship of these compounds was discussed.

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► Fifteen steroidal saponins (1–15) were isolated from Ophiopogon japonicus.
► Compounds 1–4 were new compounds.
► The cytotoxicity of compounds 2–15 were tested on five human tumor cell lines.
► The structure–activity relationship of these compounds was discussed.