Background:

DIM-C-pPhOCH3 is a Nur77 agonist. Nerve growth factor-induced Bα (NGFI-Bα, Nur77) is an orphan nuclear receptor.

DIM-C-pPhOCH3 decreases survival and induces apoptosis in RKO colon cancer cells, and this is accompanied by induction of tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) protein. DIM-C-pPhOCH3 also induces Nur77-independent apoptosis. DIM-C-pPhOCH3 (10 μM) inhibits cell growth after treatment for 24, 48, or 72 h, and the maximum inhibitory response is observed after 72 h, where there is considerable cell detachment and dead cells. The growth-inhibitory effects observed for DIM-C-pPhOCH3 after 72 h are also accompanied by several markers of apoptosis, including PARP cleavage and cleavage of caspase-3, caspase-9, and caspase-8. PARP cleavage is also observed after treatment of RKO cells for 48 h with DIM-C-pPhOCH3[1].

DIM-C-pPhOCH3 (25 mg/kg/d) also inhibits tumor growth in athymic nude mice bearing RKO cell xenografts. The effects of DIM-C-pPhOCH3 (25 mg/kg/d) on colon tumor growth are also investigated in athymic nude mice bearing RKO cell xenografts. Treatment with the DIM-C-pPhOCH3 significantly decreases tumor volumes and final tumor weights compared with corn oil controls[1].

[1]. Cho SD, et al. Nur77 agonists induce proapoptotic genes and responses in colon cancer cells through nuclear receptor-dependent and nuclear receptor-independent pathways. Cancer Res. 2007 Jan 15;67(2):674-83.