Synthesis of gypsogenin and gypsogenic acid derivatives with antitumor activity by damaging cell membranes
Forty-five gypsogenin and gypsogenic acid derivatives were synthesized and screened for their cytotoxic activities. Their structures were established using IR, 1H NMR, 13C NMR, and LC-MS spectroscopic data. These compounds were submitted to an extensive biological testing. In the MTT assays nearly all the compounds displayed good cytotoxicity in the low μΜ range for several human tumor cell lines (A549, MC3-8, TE-1, HepG-2 and MCF-7). The preliminary bioassay test suggested that most of these gypsogenin and gypsogenic acid derivatives showed different degrees of antitumor activities. In particular, some compounds posed moderate antitumor activity. They were shown to destroy the cell membranes and increase its permeability, which lead to the outflow of intracellular nucleic acid.