Synthesis and cytotoxic activities of ardipusilloside I derivatives / 中草药

ABSTRACT

Objective: To seek novel compounds with better antineoplastic activities by modifying the structure of ardipusilloside I (ADS I) isolated from Ardisia pusilla. Methods: A series of ADS I derivatives were synthesized through oxidation, reduction, and condensation on C-30 aldehyde group, and the antineoplastic activities of these compounds against nine kinds of human cancer cells were evaluated by MTT assay. Results: Four derivatives a, b, d, and c were respectively named as hydrogenated ardipusilloside I, ardipusilloside I oxide, ardipusilloside 4-benzyl-3-thiosemicarbazide, ardipusilloside methyl hydrazinecarbodithioate. Compound a and c had lower IC50 than the lead compound on nine kinds of human cancer cells (P < 0.05), which indicated that they could enhance the antineoplastic activities when compared with ADS I. Four derivatives of ADS I were synthesized, among which compounds a and c had lower IC50 than the lead compound (P < 0.05). Conclusion: Through structural modification of ADS I, the antineoplastic activities are enhanced.