Rullia tuberosa L. is used for treatment of diabetes mellitus, antiinflammation, etc. However, its hypoglycaemic and anti inflammatory activities has not been investigated so far. In the present study, the a-glucosidase inhibitory, anti inflammatory activities of the extract of this plant were investigated. Our results showed that the crude extract as well as ethyl acetate and methanol fractions showed a-glucosidase inhibitory activity with IC50 of 15.84, 4.73 and 8.27 mg/ml, respectively. In addition, the hexane and ethyl acetate fractions are capable of inhibiting LPS-induced NO production with IC50 of 17.41 and 23.95 mg/mL, respectively. From the ethyl acetate and methanol fractions, eight compounds, including isobargaptol 5-O-b-D-glucopyranoside (1), syringaresinol (2), catechin (3), pulmatin (4), stigmast-4-en-3-on (4), verbascoside (5), hydroxymethylfurfural (6), rutin (7), and homoplantaginin (8) were extracted and isolated. Their chemical structures were elucidated by spectroscopic method including MS, 1 D and 2 D- NMR and comparison with the literature values.