Hispidulin

Hispidulin is a natural flavone with a broad spectrum of biological activities. Hispidulin is a Pim-1 inhibitor with an IC₅₀ of 2.71 μM. IC50 & Target: IC50: 2.71 μM (Pim-1)^[1] In Vitro: Hispidulin induces cell death in a dose- and time-dependent manner in HepG2 cells. Hispidulin induces apoptosis through mitochondrial dysfunction, which is characterized by decreased Bcl-2/Bax ratio, disrupted mitochondrial membrane potential and increased release of cytochrome C and activated capase-3^[2]. In Vivo: Hispidulin shows significant inhibitory effect on mice tumor size^[2]. Hispidulin treatment effectively prevents ovariectomy-induced body weight loss and attenuates ovariectomy-induced bone loss. Hispidulin treatment also decreases trabecular spacing in ovariectomy mice^[3]. Intraperitoneally administering hispidulin(10 or 50mg/ kg) to rats 30 min before intraperitoneally injecting kainic acid (15mg/kg) increases seizure latency and decreases seizure score. In addition, hispidulin substantially attenuates kainic acid-induced hippocampal neuronal cell death, and this protective effect is accompanied by the suppression of microglial activation and the production of proinflammatory cytokines such as interleukin-1β, interleukin-6, and tumor necrosis factor-α in the hippocampus^[4].