Triptolide is a diterpenoid epoxide originally found in Tripterygium that exhibits anticancer chemotherapeutic, anti-angiogenic, antinociceptive, anti-inflammatory, anti-fibrotic, and immunosuppressive activities. Triptolide induces apoptosis and decreases β-catenin expression in breast cancer cells. In cellular and animal models of pancreatic cancer, triptolide inhibits cell proliferation and xenograft growth, downregulates expression of COX-2 and VEGF, and suppresses cell migration and tube formation. In animal models, chronic administration of triptolide decreases activation of glial cells and phosphorylation of MAPKs, suppressing neuropathic pain. Additionally, triptolide decreases expression of IL-17 and STAT3 and suppresses neutrophil migration, displaying hepatoprotective benefit in animal models of liver ischemia/reperfusion injury. Triptolide also prevents the development of cardiac fibrosis and improves cardiac function in animal models of chronic heart failure.