Abstract:Objective:To prepare acylated derivatives of mangiferin, and then to evaluate their anti-inflammatory activity. Method: Mangiferin was respectively reacted with acetic anhydride, propionic anhydride and butyric anhydride to produce acylated-derivatives. Swelling of mice ear and permeability of mice celiac capillary were used to evaluate the anti-inflammatory activity. Result: 3 compounds were confirmed: (a) 7,2',3',4',6'-penta-acetyl-mangiferin(PAM), (b) 3,6,7,2',3',4',6'-hepta-propionyl-mangiferin(HPM), (c) 3,6,7,2',3',4'-hexa-butyryl-mangiferin(HBM). Mangiferin's high and medium dose group (1.0, 0.5 mmol·kg-1), PAM's high and medium dose group (0.25, 0.125 mmol·kg-1), HPM's high, medium and low dose group (0.25, 0.125, 0.063 mmol·kg-1) and HBM's high, medium and low dose group (0.25, 0.125, 0.063 mmol·kg-1) could significantly inhibit the ear swelling and permeability of celiac capillary in mice, showing obvious anti-inflammatory effect. Conclusion: PAM, HPM and HBM were novel compounds and were reported for the first time.Acylated derivatives have stronger anti-inflammatory activity than their parent compound mangiferin.