The methylene chloride-methanol (1:1) extract of the air-dried aerial parts of Magnolia grandiflora was fractionated and separated to obtain the isolated compounds by different chromatographic techniques. Structures of the isolated compounds were determined on the basis of the extensive spectroscopic analysis, including 1D and 2D NMR and compared with the literature data. Three secondary metabolites were isolated from Magnolia grandiflora in this study. Of which two sesquiterpenoidal compounds; parthenolide (1) and 1,10-epoxy-parthenolide (2), together with an aromatic compound identified as threo-4-hydroxyphenyl propane-7,8-diol, 7-O-ethylether (3), which firstly isolated from the genus Magnolia. Our study aims to further phytochemical investigation of M. grandiflora to discover more secondary metabolites characterized with wide range of therapeutic values.