Triptolide is a diterpenoid triepoxide, a major bioactive component isolated from the traditional Chinese medicinal plant *Tripterygium wilfordii* (Thunder God Vine). It is characterized by a unique and complex oxygenated diterpene skeleton containing three epoxide groups, which are critical for its potent biological activity. Its primary and most researched application is in the field of medicine, particularly as a lead compound for developing novel anti-inflammatory and immunosuppressive agents. Triptolide exerts its effects through multiple mechanisms, including the inhibition of nuclear factor-kappa B (NF-κB) signaling and suppression of pro-inflammatory cytokine production. This makes it a promising candidate for treating autoimmune diseases such as rheumatoid arthritis, lupus, and psoriasis. Furthermore, significant research focuses on its potent anti-tumor activities against various cancer cell lines. Despite its therapeutic potential, triptolide has a narrow therapeutic window and is associated with significant toxicity, including hepatotoxicity and reproductive toxicity, which has limited its direct clinical application. Current research is heavily directed towards synthesizing analogs and prodrugs to improve its safety profile while retaining efficacy, positioning it firmly as a valuable natural product-derived pharmaceutical agent and a chemical probe for biological studies.