Abstract:Four new monoterpene rhamnosides, graphiumisides A–D (1–4), along with four known steroid compounds (5–8) were isolated from the fermentation extract of animal‐derived endophytic fungus, Graphium sp. GD‐11. The chemical structures of all compounds were elucidated using 1D and 2D NMR, HRESIMS spectroscopic analyses, and other spectroscopic methods. Compounds 1–4 exhibit a distinctive structure connected by one p‐menthane type monoterpene and one L‐rhamnose. This is the first report of monoterpene glycosides from Graphium sp. All compounds (1–8) were tested for cytotoxic activities against four cancer cell lines (HepG2, SMMC7721, SW480, and A549), and only compound 1 showed weak anti‐tumor activity against SMMC7721 cells.