Phillygenin (Phillygenol)

Phillygenin is a lignan that has been found in F. fructus and has diverse biological activities.^1,2,3,4 It scavenges peroxide and 2,2-diphenyl-1-picrylhydrazyl radicals in cell-free assays (IC₅₀s = 10.5 and 19.1 ?M, respectively).¹ Phillygenin (25-200 ?g/ml) inhibits LPS-induced production of IL-1β, IL-6, TNF-α, and the fibrosis markers collagen I and α-SMA in LX-2 hepatic stellate cells.² It inhibits the growth of SH-1-V1 esophageal cancer cells (IC₅₀ = 6 ?M), as well as induces the production of reactive oxygen species (ROS) and apoptosis in the same cells.³ Phillygenin (15 mg/kg) reduces tumor volume in an SH-1-V1 mouse xenograft model. It also reduces serum levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), superoxide dismutase (SOD), and malondialdehyde (MDA) and prevents hepatic necrosis in a mouse model of carbon tetrachloride-induced liver injury.⁴

1.Hung, C.-Y., Tsai, Y.-C., and Li, K.-Y.Phenolic antioxidants isolated from the flowers of Osmanthus fragransMolecules17(9)10724-10737(2012) 2.Krausz, L.T., Bianchini, R., Ronchetti, S., et al.GITR-GITRL system, a novel player in shock and inflammationScientificWorldJournal7533-566(2007) 3.He, J., Wei, W., Yang, Q., et al.Phillygenin exerts in vitro and in vivo antitumor effects in drug-resistant human esophageal cancer cells by inducing mitochondrial-mediated apoptosis, ROS generation, and inhibition of the nuclear factor lappa B NF-κB signalling pathwayMed. Sci. Monit.25739-745(2019) 4.Song, W., Wu, J., Yu, L., et al.Evaluation of the pharmacokinetics and hepatoprotective effects of phillygenin in mouseBiomed. Res. Int.7964318(2018)