Troglitazone

Troglitazone is a potent and selective activator of peroxisome proliferator-activated receptor-γ (PPARγ) with EC50 = 0.55 and 0.78 µM for human and mouse, respectively. Troglitazone does not inhibit PPARα or PPARδ at up to 10 µM (Willson et al.). Troglitazone causes cell cycle arrest at phase G1, inducing caspase-dependent apoptosis in both HeLa and hepatocellular carcinoma cell lines (Yoshizawa et al.; Chang et al.).

DIFFERENTIATION

• Stimulates adipogenesis in 3T3-L1 cells (Jeong & Yoon).
• Inhibits macrophage differentiation (Chen Y et al.).

METABOLISM

• Exerts potent glucose-lowering effects in insulin-resistant diabetic animals and in non-insulin-dependent (type II) human diabetic subjects (Lee & Olefsky).

CANCER RESEARCH

• Inhibits growth and induces apoptosis in non-small cell lung carcinoma, bladder cancer, cervical cancer, and prostate cancer cells (Chen H-M et al.; Santha et al.; Satoh et al.; Yan et al.).
• Promotes cytostatic effects in MDA-MB-231 and MCF-7 breast cancer cell lines (Berthe et al.)