Abstract: OBJECTIVE To synthesize caudatin-β-D-glucoside and determine its antitumor activity. METHODS The target compound caudatin-β-D-glucoside was synthesized from caudatin by reaction with tetra-O-actyl-D-glucosyl bromide catalyzed by CdCO₃ and then deprotection in CH₃ONa/CH₃OH. The antitumor activity was studied by MTT method. RESULTS Caudatin-β-D-glucoside was synthesized and characterized by 1H-NMR and ¹³C-NMR spetra. CONCLUSION Preliminary pharmacological result shows that the inhibitory effect of caudatin-tetra-O-actyl-D-glucoside on rat glioma cell C₆ is higher than that of caudatin while caudatin-β-D-glucoside shows similar activity to caudatin.