(-)-Arctigenin

Semi-synthetic. Soluble in DMSO (20mg/ml) or DMF (20mg/ml). Slightly soluble in ethanol or methanol (both ~1mg/ml). Insoluble in water. Aglycone metabolite of (-)-Arctiin (AG-CN2-0532), isolated from Arctium lappa. Multifunctional natural compound with antioxidant, antibacterial, anti-inflammatory, antidiabetic, neuroprotective, antiproliferative and antiviral activities. Natural agonist of the PP2A that has potent renoprotective effects in type 1 and type 2 diabetic animal models. Inhibits adipogenesis through AMPK induction. Modulator of peroxisome proliferator-activated receptor gamma (PPARgamma). Inhibits LPS-induced iNOS expression via inhibition of IkappaBalpha phosphorylation and p65 nuclear translocation. Inhibits NLRP3 in a SIRT1-dependent manner. HIV-1 integrase/replication inhibitor in vitro. Potently inhibits MKK1 (MEK1). Blocks the activation of Akt induced by glucose starvation in pancreatic cancer PANC-1 cells. Also dissipates the mitochondrial membrane potential by inhibition of the mitochondrial complexes II and IV. Selectively kills only the OXPHOS-dependent PANC-1 cells. Possibly useful in immunometabolism research. Shown to induce cell cycle arrest, autophagy and apoptosis in several cancer cell lines and having chemosensitizing properties.