Abstract:Seven compounds were isolated from the ethanolic extract of twigs and leaves of Kopsia hainanensis Tsiang. On the basis of spectral data (NMR, MS, IR, etc.), their structures were identified as kopsinine (1), tubotaiwine (2), dihydrodehydrodiconiferyl alcohol (3), β-amyrin (4), ursolic acid (5), 2 α,3β-dihydroxyursolic acid (6), and β-sitosterol (7). Compounds 3-7 were isolated from K. hainanensis for the first time. Antibacterial activities assayed by paper disk diffusion method, the result showed that compounds 1-3, and 5 had inhibitory activities against methicillin-resistant Staphylococcus aureus (MRSA), and compound 2 exhibits inhibitory effect on Staphylococcus aureus. Cytotoxic activity assay demonstrated that compound 5 showed cytotoxic activities towards chronic myelogenous leukemia (K562), human gastric carcinoma (SGC-7901), and human hepatoma (SMMC-7721) cell lines.