Euphorbia fischeriana Steud is an essential oriental folk medicine used for healing cancer, edema and tuberculosis. Recently, its anticancer activitity has attracted more attention. A volume of research has indicated that diterpenoids are the major anticancer active constituents from this medicinal herb. In this review, we aimed to provide a summary of the promising anticancer diterpenoids from this plant; many diterpenoids mentioned in this article are newly discovered diterpenoids. According to the carbon skeleton and substituents, they can be classified into eight subtypes: ent-abietane, daphnane, tigliane, ingenane, ent-atisane, ent-rosane, ent-kaurane, and lathyrane. Futhermore, their key anticancer mechanisms and protein targets of these compounds will be discussed. These natural diterpenoids could provide a reservoir for drug discovery.

Diterpenoids are the focus of natural product drug discovery because of their great structural diversity and pronounced biological activities. Euphorbia fischeriana Steud is a Chinese traditional medicinal herb for curing edema, ascites, and cancer. This plant contains rich diterpenoids. Based on the carbon skeleton and substituents, it can be classified into thirteen subtypes: ent-abietane, daphnane, tigliane, ingenane, ent-atisane, ent-rosane, ent-kaurene, ent-kaurane, secotigliane, lathyrane, ent-pimarene, isopimarene and dimeric. In this paper, we reviewed the chemical structures and biological activities of 90 diterpenoids isolated from this medicinal herb. We hope that this work can serve as a reference for further research of these diterpenoids and lay the foundation for drug discovery.