To study the biological activities and chemical constituents of Siraitia grosvenorii roots,the crude extracts of S.grosvenorii roots were loaded to HPD-100 column and eluted by gradient methanol-water solutions to obtain Fr1,Fr2,Fr3 and Fr4 fractions.Traditional separation methods and reversed-phase preparative chromatography techniques were used for separation and purifica-tion,and ESI-MS and NMR were used for identifying their structure.α-glycosidase and HepG2 tu-mor cell inhibition activity of different polar parts and partical compounds were determined.The re-sults indicate that Fr4 has the highest α-glycosidase and HepG2 tumor cell inhibition activity.Four compounds were isolated from Fr4,and their structures were identified as dihydrocucurbitacin E,cu-curbitacin E,dihydroisocucurbitacin B-25-acetate and cucurbitacin B,and they are isolated from S.grosvenorii for the first time.