Troglitazone

Troglitazone is a selective agonist of peroxisome proliferator-activated receptor γ (PPARγ; EC₅₀s = 0.78 and 0.55 μM for the mouse and human receptors, respectively, in a transactivation assay).¹ It is selective for PPARγ over PPARα and PPARδ, at which it is inactive at concentrations up to 10 μM. Troglitazone (500 mg/kg twice per day) exhibits antihyperglycemic and antihyperlipidemic properties in Zucker diabetic fatty rats, reducing plasma glucose and triglyceride levels by 61 and 87% respectively.² It also induces cell cycle arrest at the G₁ phase in SK-HEP-1 and Hep3B hepatocellular carcinoma cells when used at a concentration of 10 μM and increases apoptosis in these cells at concentrations of 30 μM and higher.³

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1. Willson, T.M., Brown, P.J., Sternbach, D.D., et al. The PPARs: From orphan receptors to drug discovery. J. Med. Chem. 43(4), 527-550 (2000).

2. Henke, B.R., Blanchard, S.G., Brackeen, M.F., et al. N-(2-Benzoylphenyl)-L-tyrosine PPARγ agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents. J. Med. Chem. 41(25), 5020-5036 (1998).

3. Yoshizawa, K., Cioca, D.P., Kawa, S., et al. Peroxisome proliferator-activated receptor γ ligand troglitazone induces cell cycle arrest and apoptosis of hepatocellular carcinoma cell lines. Cancer 95(10), 2243-2251 (2002).

Soriano-Castell, D., Currais, A., and Maher, P. Defining a pharmacological inhibitor fingerprint for oxytosis/ferroptosis. Free Radic. Biol. Med. S0891-5849(21), (2021).

Malaviya, A., and Sylvester, P.W. Synergistic antiproliferative effects of combined g-tocotrienol and PPARg antagonist treatment are mediated through PPARg-independent mechanisms in breast cancer cells. PPAR Res. 2014(439146), (2014).

Baumgartner, L., Sosa, S., Atanasov, A.G., et al. Lignan derivatives from Krameria lappacea roots inhibit acute inflammation in vivo and pro-inflammatory mediators in vitro. J. Nat. Prod. 74(8), 1779-1786 (2011).