CITCO inhibits growth and expansion of brain tumour stem cells (BTSCs) and has an EC50 of 49 nM over pregnane X receptor (PXR), and no activity on other nuclear receptors. CITCO is an imidazothiazole derivative and it also is a selective Constitutive androstane receptor (CAR) agonist.
CITCO (intraperitoneal; on days 22, 24, 26, 30 and 36) with 25 μg results a significant decrease in tumour growth, which further decreases to an undetectable level after treatment with 100 μg CITCO. Animal model: Six-to eight-week-old male athymic nude mice. Dosage: 25 or 100 μg. Administration: Intraperitoneal; on days 22, 24, 26, 30 and 36. Result: Decreased tumour growth.
In Vitro
CITCO (1-50 μM; 48 hours) results in a dose-dependent inhibition of viable cell count and proliferation in both T98G and U87MG glioma and BTSCs. CITCO (2.5, 5 μM; 48 hours) induces cell cycle arrest differentially in different BTSCs in culture, but not in normal astrocytes. CITCO (2.5-10 μM; 48 hours) induces apoptosis in BTSCs in culture in dose dependently, but not in normal astrocytes. CITCO (0-25 μM; 48 hours) causes the T98G and U87MG glioma and BTSCs expressing very low levels of CAR protein that increased significantly. Cell Proliferation Assay Cell line: T98G, U87MG, DB29 and DB33 human glioma cells, astrocytes. Concentration: 1, 2.5, 5, 10, 25, 50 μM Incubation time: 48 hours. Result: Resulted in a dose-dependent inhibition of viable cell count and proliferation. Cell Cycle Analysis Cell line: The T98G, U87MG, DB29 and DB33 glioma cells. Concentration: 2.5, 5 μM Incubation time: 48 hours. Result: Induced cell cycle arrest differentially in different BTSCs in culture. Apoptosis Analysis Cell line: The T98G, U87MG, DB29 and DB33 glioma cells. Concentration: 2.5, 5 or 10 μM Incubation time: 48 hours. Result: Increased the levels of Annexin V-positive apoptotic cells in dose dependently. Western blot analysis. Cell line: T98G, U87MG, DB29 and DB33 glioma cells. Concentration: 0 to 25 μM. Incubation time: 48 hours. Result: The T98G, U87MG glioma and BTSCs expressed very low levels of CAR protein that increased significantly.
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