The petroleum ether extract of Heracleum platytaenium afforded 8 furocoumarins (psoralen, bergapten, xanthotoxin, pimpinellin, isopimpinellin, sphondin, byakangelicin, and heraclenol) and the methanol extract of H. platytaenium gave only 1 glycosylated dihydrofurocoumarin, apterin. In addition, stigmasterol was also obtained from petroleum ether extract. Structure identification of the isolated compounds has been achieved by using spectroscopic methods, namely 1D and 2D NMR experiments and mass spectral analyses. The antioxidant activity of the extracts and pure compounds was investigated by 2 methods, including DPPH free radical scavenging activity and lipid peroxidation inhibitory activity by beta-carotene-linoleic acid assays. The anticholinesterase activity of petroleum ether and methanol extracts of the plant and the isolated furocoumarins was investigated against acetylcholinesterase and butyrylcholinesterase enzymes by the Ellman method in vitro.