Periplogenin

Periplogenin is a cardenolide and an active metabolite of periplocin that has been found in P. graeca and has diverse biological activities.^1,2,3 It reduces the activity of porcine Na⁺/K⁺ ATPase when used at concentrations of 0.3 or 0.6 ?M.¹ Periplogenin induces apoptosis in U937 and PC3 prostate cancer cells, as well as inhibits the proliferation of these cells (EC₅₀s = 1.41 and 1.2 ?M, respectively), when used at concentrations of 0.1 or 0.2 ?M. It increases the production of reactive oxygen species (ROS) and induces necroptosis in HaCaT keratinocytes when used at a concentration of 2 ?g/ml.³ Topical application of periplogenin reduces ear thickness in a mouse model of psoriasis induced by phorbol 12-myristate 13-acetate .

1.Bloise, E., Braca, A., De Tommasi, N., et al.Pro-apoptotic and cytostatic activity of naturally occurring cardenolidesCancer Chemother. Pharmacol.64(4)793-802(2009) 2.He, J., Bo, F., Tu, Y., et al.A validated LC-MS/MS assay for the simultaneous determination of periplocin and its two metabolites, periplocymarin and periplogenin in rat plasma: Application to a pharmacokinetic studyJ. Pharm. Biomed. Anal.114292-295(2015) 3.Zhang, W.-J., Song, Z.-B., Bao, Y.-L., et al.Periplogenin induces necroptotic cell death through oxidative stress in HaCaT cells and ameliorates skin lesions in the TPA- and IMQ-induced psoriasis-like mouse modelsBiochem. Pharmacol.10566-79(2016)