In the present study, the antioxidant and antiplasmodial activities of bergenin was compared with its natural derivative 11-O-galloylbergenin for the first time. Both compounds were isolated from Bergenia ligulata. 11-O-galloylbergenin was found to be very active in in-vitro antioxidant assay as compared to bergenin, which was found to be almost inactive. The EC50 values of 11-O-galloylbergenin were 7.45±0.2 μg/mL and 5.39±0.28 μg/mL in DPPH antioxidant assay and reducing power assay respectively, while IC50 value for antiplasmodial assay of both compounds were less than 2.5 μM. Interestingly, in the total antioxidant phosphomolybdate assay, 11-O-galloylbergenin was found more potent (CAHT: 940.04±115.30) as compared to α-tocopherol (CAHT: 552.4±27.91).