About two hundred Daphniphyllum alkaloids have so far been isolated from thirteen species of the genus Daphniphyllum. This comprehensive review summarizes all the research into the isolation and structure elucidation of these alkaloids reported since investigations began in 1996. The structures of the Daphniphyllum alkaloids are classified based on six Daphniphyllum alkaloids (daphniphylline, secodaphniphylline, yuzurimine, daphnilactone A, daphnilactone B and yuzurine); these are also a number of newly found skeletons. The biosynthetic pathways, total syntheses, and bioactivities of the Daphniphyllum alkaloids are also described.