Five new aspidofractinine-type alkaloids, kopsiahainins A–E (1–5), were isolated from a 80% EtOH extract of the leaves and stems of Kopsia hainanensis. Structural elucidation of all the compounds were performed by spectral methods such as 1D- and 2D-NMR, IR, UV, and HR-ESI-MS. Alkaloids 3 and 4 exhibited some cytotoxic activity against all of six tested tumor cell lines (BGC-823, HepG2, MCF-7, SGC-7901, SK-MEL-2, and SK-OV-3) with IC50 values of 7.3–9.5 μM and 9.2–10.6 μM, respectively. © 2017 Elsevier B.V.