Semi-Synthesis of Caudatin Glycosides and Study on their Antiproliferative Activities

Four Caudatin glycosides were synthesized from Caudatin by reaction with tetra-O-actyl-D-glycosyl bromide catalyzed by CdCO3 and tested in vitro for their antiproliferative activities against human lung cancer A549, human prostate cancer PC3, human liver cancer BEL-7402 and human gastric cancer SGC-7901 cells. The IC50 values indicated that the inhibitory effect of Caudatin-tetra-O-actyl-D-glycosides was superior or comparable to Caudatin against most of the tested cells, worthy of further investigation. Keywords: Antiproliferative activities, Caudatin, C21 steroidal glycosides, Glycosyl bromide, In vitro, Semi-Synthesis, Cynanchum auriculatum Royle ex Wight, 3β-hydroxyl group, aglycon, 14-O-isopropylidene-Caudatin (1)