The purpose of this study was to explore the acylation of panaxadiol,prepare its derivatives,and evaluated the relaxation activity of the prepared panaxadiol acylates on the isolated thoracic aorta of SD rats.The 3-hydroxyl group of panaxadiol saponins was modified and reacted with acyl chloride reagent to prepare its derivatives.After its structure was identified by nuclear magnetic resonance(NMR),the relaxing activity of rat thoracic aorta was determined by Wire Myograph System DMT vascular tension tester.The results showed that the 10 acylated derivatives of panaxadiol were new compounds,among which compounds PD-3,4,7,9 and 10 had significant relaxing activity of thoracic aorta,which were worthy of further study.