Triterpenoid alkaloids are one of the most important classes that have been studied. Buxus alkaloids are such a type of triterpenoid alkaloids of cycloartenol skeleton with a degraded C-20 side chain, and with the nitrogen containing substituents at C-3 and/or C-20. 219 Buxus alkaloids have been reported so far. This review article focuses on the structural characters, plant sources and biological activities of Buxus alkaloids. This review includes anti-myocardial ischemia, inhibition of acetyl- and butyryl-cholinesterases, cytotoxicity and antibacterial activities. The biological activities, mechanisms and structure modifications of cyclovirobuxine D (CVB-D) are also described.