Objective To study the chemical constituents and pharmacological activities of acylation products of acid hydrolysis of Panax notoginseng saponins and to find active substances. Methods Under acidic condition， Panax notoginseng saponins were hydrolyzed to obtain the acylation products. The compounds were isolated and purified by silica gel column chromatography and recrystallization， and the structures of the acylated products were identified by NMR， and study the antitumor activity and vasodilation activity of the products. Results After acid hydrolysis， seven acylated products were obtained， three compounds have some antitumor activity， one compound has some vasodilation of rat brain. Conclusions Acylated derivatives of sapogenins of Panax notoginseng saponins have certain pharmacological activity and were worthy of further study.