Nerve growth factor-induced Bα (Nur77) is an orphan nuclear receptor overexpressed in colon tumors. DIM-C-pPhOCH3 is a Nur77 agonist. It inhibited RKO cell growth at 24-, 48-, and 72-h post-treatment at a concentration of 10μmol/L. PARP cleavage was observed in RKO cells treated with 12.5μmol/L DIM-C-pPhOCH3 for 48 hours. Treatment with 12.5μmol/L DIM-C-pPhOCH3 for 48 hours also induced the expression of TRAIL protein in RKO cells. DIM-C-pPhOCH3 at a concentration of 12.5 μmol/L also induced the gene expression of PDCD1, CSE, and ATF3 in RKO cells 6 hours after exposure. DIM-C-pPhOCH3 treatment at 12.5 μmol/L induced apoptosis (PARP cleavage) in RKO, SW480, HCT-116, and HT-29 cells at 24-h post-treatment but not in HCT-15 cells. In athymic nude mice bearing RKO cell xenografts, oral administration of DIM-C-pPhOCH3 at a dosage of 25 mg/kg/d for 21 days significantly inhibited tumor growth compared with corn oil-treated controls[2].
DIM-C-pPhOCH3 细胞实验
Cell Line
Concentration
Treated Time
Description
References
L3.6pl pancreatic cancer cells
10 µM
18 hours
DIM-C-pPhOCH3 induces p21 mRNA levels
Mol Cancer Res. 2009 Jul;7(7):1169-78.
A549 cells
14.29±2.30 µM (IC50)
24 hours
Evaluate the cytotoxicity of C-DIM-5 on A549 cells, showing an IC50 value of 14.29±2.30 μM at 24 hours.
Eur J Pharm Sci. 2013 Oct 9;50(2):227-41.
Panc1 pancreatic cancer cells
5 or 10 µM
24 hours
DIM-C-pPhOCH3 induces p21 protein levels
Mol Cancer Res. 2009 Jul;7(7):1169-78.
DIM-C-pPhOCH3 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Nude mice
A549 cell metastatic lung tumor model
Inhalation
0.440 mg/kg
Alternate days for 4 weeks
Evaluate the antitumor activity of C-DIM-5 on metastatic lung tumors, showing significant inhibition of tumor growth and metastasis.
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