Cynaropicrin is a sesquiterpene lactone which can inhibit tumor necrosis factor (TNF-α) release with IC₅₀s of 8.24 and 3.18 μM for murine and human macrophage cells, respectively. Cynaropicrin also inhibits the increase of cartilage degradation factor (MMP13) and suppresses NF-κB signaling. IC50 & Target: IC50: 8.24 μM (TNF-α of murine), 3.18 μM (TNF-α of human)^[1]
MMP13, NF-κB^[2] In Vitro: Cynaropicrin strongly inhibits lipopolysaccharide-induced TNF-α release from either murine or human macrophage cells in a dose-dependent manner with the IC₅₀ values of 8.24 and 3.18 μM, respectively. Cynaropicrin shows significant inhibitory effects toward all mitogenic signals with the IC₅₀ values of 1.20 (concanavalin A), 1.02 (phytohemagglutinin) and 0.90 μM (lipopolysaccharide), respectively. Cynaropicrin suppresses CTLL-2 cell proliferation in a dose-dependent manner and the 50% inhibitory concentration (IC₅₀) of Cynaropicrin for CTLL-2 cell growth is 0.91 μM^[1]. The increased mRNA expression of MMP13 induced by TNF-α is similarly inhibited in a concentration-dependent manner by Cynaropicrin. The increased mRNA expression of HIF-2α induced by IL-1β in SW1353 is inhibited in a concentration-dependent manner by Cynaropicrin^[2].