In vitro: Troglitazone significantly inhibits cell growth by cell cycle arrest and apoptotic cell death. Troglitazone also downregulates surface expression of CD97, a novel dedifferentiation marker, in FTC-133 cells and upregulated sodium iodide symporter (NIS) mRNA in TPC-1 and FTC-133 cells. Troglitazone, a PPARγ agonist, induces antiproliferation and redifferentiation in thyroid cancer cell lines. Troglitazone induces Erk phosphorylation in human prostate cancer cells via a PPARγ-independent signaling pathway. TGZ(Troglitazone) up-regulates nitric oxide synthesis, induces the p53 pathway, inhibits cholesterol biosynthesis, induces p21 cyclin-dependent kinase inhibitor, has antioxidant function, and activates extracellular signal-regulated protein kinase (ERK) in a PPARγ-independent manner. TGZ induces Egr-1 expression by transcriptional and post-transcriptional regulation. Egr-1 induction by TGZ results in the increase of binding affinity and transactivation of the promoter containing Egr-1 consensus sequences, thereby possibly inducing other anti-tumorigenic proteins. In vivo: Troglitazone is an effective antidiabetic drug with a fundamentally new mechanism of action. However, within a year after its widespread use, individual cases of liver injury and failure are reported. TGZ significantly inhibits tumor growth of human colorectal cancer cells (HCT-116), human breast cancer cells (MCF-7), and human prostate cancer cells (PC-3) in immunodeficient mice. Troglitazone attenuates pancreatic damage and inflammation in experimental chronic pancreatitis.
|Cell lines||Thyroid cancer cell lines TPC-1, FTC-133, FTC-236, FTC-238, XTC-1 and ARO82-1 cell lines|
|Preparation method||Growth experiments are done in a 96-well plate in hexaplicate. Cells at 85%-100% confluency are harvested with 1×Trypsin/EDTA solution and seeded into a 96-well plate at 3-5×103 cells per well depending upon growth rate and maintained in 200 μL H5 medium in a humidified incubator. After 24 hours, cells are incubated with different concentrations of troglitazone and the media was changed daily. Colorometric dimethyl-thiazol-diphenyltetrazolium bromide (MTT) proliferation assays are performed at 0, 2, 4, and 6 days after treatment. MTT (400 μg/mL) is added to each well and incubated for 3 hours. It is solubilized with 0.04 N HCl/iso-propanol/3% SDS and incubated for 1 hour. The optical densities in the 96-well plates are determined using an enzyme-linked immunosorbent assay (ELISA) microplate reader at 595 nm/620 nm.|
|Concentrations||5, 10, 20, 40 μM|
|Incubation time||0, 2, 4, and 6 days|
|Animal models||C57BL/6 mice|
|Dosages||0.2% (with chow)|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||88 mg/mL in DMSO|
Cancer drug troglitazone stimulates the growth and response of renal cells to hypoxia inducible factors.
Taub M Biochem Biophys Res Commun. 2016 Mar 11;471(3):342-7. PMID: 26869517.
Troglitazone Stimulates Cancer Cell Uptake of 18F-FDG by Suppressing Mitochondrial Respiration and Augments Sensitivity to Glucose Restriction.
Moon SH, et al. J Nucl Med. 2016 Jan;57(1):129-35. PMID: 26449833.
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