Omtriptolide, triptolide purified from the Chinese herb, is a water-soluble derivative prodrug.

Triptolide is a traditional Chinese medicine. It also has anti-inflammatory, antiproliferative, and proapoptotic properties[1].

Omtriptolide effectively reduces fibrosis in groups treated with bleomycin, either when administered concurrently or five days post-treatment. It significantly diminishes in vivo expansion of both CD4+Vbeta3+ and CD8+Vbeta3+ T cells (alloreactive T cells in this context) in the spleen by 64.09% and 34.02%, respectively, particularly during the logarithmic expansion phase (day 3 post-transplantation). Additionally, it notably decreases the population of myofibroblasts in the bleomycin-treated cohorts. In a cisplatin-induced acute kidney injury (AKI) mouse model, Omtriptolide substantially lowers blood urea nitrogen (BUN), serum creatinine levels, and acute tubular necrosis (ATN) scores, while slightly increasing the tubular apoptosis score, indicating a protective role against AKI. This protection correlates with a reduction in p-ERK activity, operating independently of MKP-1 and pro-inflammatory cytokines[1]. Furthermore, Omtriptolide alleviates airway obliteration and curtails the aggregation of inflammatory cells, suggesting potential preventive or therapeutic applications for obliterative airway diseases post-lung transplantation, as demonstrated in a mouse heterotopic tracheal allograft model[2][3][4].