Piperlongumine

Piperlongumine is an alkaloid that has been found in P. longum and has anticancer and antioxidant activities.^1,2,3 It binds to glutathione (GSH) and inhibits the protein-protein interaction between glutathione and glutathione S-transferase pi 1 (GSTP1), an enzyme that is often overexpressed in cancer cells.³ Piperlongumine reduces the viability of A549 and NCI H460 cells (IC₅₀s = 14.91 and 13.72 µM, respectively).¹ It also induces apoptosis and inhibits the DNA binding activity of NF-κB in A549 and NCI H460 cells. Piperlongumine (2.5 and 5 mg/kg twice per week) reduces tumor growth in an A549 mouse xenograft model. It also reduces plasma glucose levels, as well as plasma and pancreatic levels of thiobarbituric acid reactive substances (TBARS) and lipid hydroperoxides in a rat model of diabetes induced by streptozotocin (Item No. 13104).²

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1. Zheng, J., Son, D.J., Gu, S.M., et al. Piperlongumine inhibits lung tumor growth via inhibition of nuclear factor kappa B signaling pathway. Sci. Rep. 6, 26357 (2016).

2. Xu, P., Xiao, J., and Chi, S. Piperlongumine attenuates oxidative stress, inflammatory, and apoptosis through modulating the GLUT-2/4 and AKT signaling pathway in streptozotocin-induced diabetic rats. J. Biochem. Mol. Toxicol. 35(6), 1-12 (2021).

3. Harshbarger, W., Gondi, S., Ficarro, S.B., et al. Structural and biochemical analyses reveal the mechanism of glutathione S-transferase pi 1 inhibition by the anti-cancer compound piperlongumine. The Journal of Biological Chemisty 292(1), 112-120 (2017).