Antitumor Activity of Ten bufadienolides on Hela Cells and Its Structure-Activty Relationship

Objective:To investigate the growth inhibitory effect of bufadienolides on Hela cell line and the relationship between their structures and antitumor activity.Method: The modified MTT assay was adopted to measure the inhibitory effect of bufadienolides at different concentrations and chemical structures on Hela cells,and analysed the relationship between their chemical structures and cytotoxicity.Results:Ten bufadienolides could inhibit the proliferation of Hela cells effectively,and their sequence of cytotoxicities on Hela cells showed BulBtlArgHelTelDebCtlCbgGtlRbg.It indicated that the chemical structure of A-type nucleus with 14-epoxy was significantly lower than that of B-type nucleus which with 14-hydroxy.Similarly,among the same nucleus structures,the compounds with only one hydroxy of acetyl group of bufadienolides could enhance their cytotoxicity.Conclusion: The bufadienolides has an inhibitory effect on proliferation of Hela cell line,and their cytotoxicities show obvious concentration dependent manners and structure-activty relationship.