Hispidulin是存在于豚草中的一种黄酮，是Pim-1抑制剂，IC50值为2.71 μM。

Hispidulin, a natural flavone with a broad spectrum of biological activities, is a Pim-1 inhibitor (IC50: 2.71 μM).

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 caspase-3 [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].

HepG2 cells are treated with different concentrations of hispidulin (50, 100, 200 μM) for 24, 48 and 72 h. Following treatment, cells are further incubated with MTT reagents at 37°C for 4 h before DMSO is added, to dissolve formazan crystals, and absorbance is measured at 570 nm in a microplate reader [2].

The tumor is established in mice. Mice are treated with DMSO or Hispidulin at a dosage of 10, 20 or 40 mg/kg/day for 35 days. The body weight of tumor-bearing mice is recorded every week and tumor volume is calculated [2].

1447-88-7

C16H12O6

300.266

DMSO:60 mg/mL (199.82 mM),Need ultrasonic
H2O:Insoluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years