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 inhibits fibrosis in the bleomycin group when given the same day or 5 days after bleomycin. Omtriptolide inhibits in vivo both CD4+Vbeta3+ and CD8+Vbeta3+ T cell (alloreactive T cells in this model) expansion in the spleen by 64.09 and 34.02%, respectively, at the time when Vbeta3+ cell expansion is in the logarithmic phase (day 3 after transplantation). Omtriptolide also markedly reduces the number of myofibroblasts in the bleomycin treatment group. Omtriptolide causes a significant decrease in blood urea nitrogen (BUN), serum creatinine, and acute tubular necrosis (ATN) score, and a nonsignificant increase in tubular apoptosis score in AKI, in a mouse model of cisplatin-induced AKI. The protection of Omtriptolide against AKI is associated with a decrease in p-ERK and is independent of MKP-1 and proinflammatory cytokines[1]. Omtriptolide attenuates airway obliteration and inhibits the accumulation of inflammatory cells, and therefore may have preventive or therapeutic benefits for patients with obliterative airway disease following lung transplantation, in a mouse heterotopic tracheal allograft model of obliterative airway disease [2][3][4].