Abstract: Triptolide (TP) is a kind of natural triepoxide diterpenoid, isolated from Chinese medical herb Tripterygium wilfordii Hook F. As one of the primary biologically active ingredients, TP possesses various and potent pharmacological effects such as anti-inflammatory, immunosuppressive and anti-tumor properties. Here, we focus on the mechanisms of actions of TP in anti-tumor effects, the toxicity and the possible solutions in toxicity attenuation by compatibility. This review may provide reference for the clinical development of TP as well as its related derivatives.