Abstract: The Ladizabalaceae is a relatively primitive small family in the Dicotyledoneae. It is composed mainly of monotypic and oligotypic genera and is distributed mainly in eastern Asia. There are 29 species of 7 genera in China, some of which are used as traditional herbs. Based on the brief summary of taxonomic and chemical research results, the present paper discusses the chemotaxonomy of this family. It is noticed that oleanane triterpenoidal saponins are characteristic constituents of this family and have taxonomic significance. The distribution of triterpenoidal saponins in the plants of Ladizabalaceae suggests the phylogenetic relation between Lardizabalaceae and Ranunculoideae of Ranunculaceae. Moreover, the oxidative level of triterpenoidal aglycone may also imply evolutionary relations among the genera of the family.