The fresh rhizomes of Angiopteris evecta Hoffm. were extracted subsequently with organic solvents including methanol, hexane and ethyl acetate, respectively. Each crude extract was isolated and purified using column chromatography to obtain four compounds. The structures of these compounds were characterized using their physical and chemical properties, spectral data and x-ray crystallographic analysis. Four compounds were Succinic acid (1), Angiopteroside (4-O-beta-D-Glucopyranosyl-L-thero-2-hexen-5-olide) monohydrate (2), D-(+)-glucose (3) and a mixture of beta-sitosterol and stigmasterol (4). This research indicated the first report of compound 2 in Angiopteris evecta Hoffm. The compound 2 was tested for cytotoxic activity against cancer cell lines. The result indicated that compound 2 showed low activity. Moreover, compound 2 was found to inhibit HIV-1 reverse transcriptase.