Aim: To study the bufadienolides in the Chinese traditional drug "Ch'an Su" and their cytotoxic activity.
Method: Various chromatographic techniques were used to isolate the constituents, and their structures were elucidated through physical and spectroscopic data.
Results: Twenty compounds were isolated, and eighteen were evaluated in vitro for their cytotoxic activity against A-549 and K-562 cells.
Conclusion: Compound 1 (bufalin 3β-acrylic ester) was a new bufadienolide and exhibited the most potent activity against the two tumor cell lines with IC50 values of 7.16 and 6.83 nmol · L(-1). The relationships between structure and activity are discussed.
Keywords: Bufalin 3β-acrylic ester; Cytotoxicity; New bufadienolide; “Ch'an Su”.
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