| Description | Hispidulin, a natural flavone with a broad spectrum of biological activities, is a Pim-1 inhibitor (IC50: 2.71 μM). |
| In vitro | Hispidulin在HepG2细胞中以剂量依赖和时间依赖的方式诱导细胞死亡。Hispidulin通过线粒体功能障碍诱导细胞凋亡，表现为Bcl-2/Bax比率下降、线粒体膜电位破坏以及细胞色素C释放增加和caspase-3激活[2]。 |
| In vivo | Hispidulin治疗有效预防去卵巢引起的体重减轻，并减轻去卵巢引起的骨质流失。Hispidulin治疗还减少了去卵巢小鼠的小梁间隙[3]。在腹腔内给予大鼠Hispidulin（10或50mg/kg）30分钟后，再腹腔内注射海因酸（15mg/kg），可以延长发作潜伏期，降低发作评分。此外，Hispidulin显著减轻海因酸引起的海马神经元细胞死亡，这种保护效果伴随着海马中微胶质激活的抑制以及诸如白细胞介素-1β、白细胞介素-6和肿瘤坏死因子-α等促炎细胞因子产生的抑制[4]。 |
| Cell experiments | 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]. |
| Animal experiments | 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]. |
| Target activity | Pim1:2.71 μM |
| Synonyms | Dinatin |
| molecular weight | 300.26 |
| Molecular formula | C16H12O6 |
| CAS | 1447-88-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: Insoluble DMSO: 60 mg/mL (199.82 mM), Sonication is recommended. |
| References | 1. Chao SW, et al. Total Synthesis of Hispidulin and the Structural Basis for Its Inhibition of Proto-oncogene KinasePim-1. J Nat Prod. 2015 Aug 28;78(8):1969-76. 2. Gao H, et al. Hispidulin induces apoptosis through mitochondrial dysfunction and inhibition of P13k/Akt signalling pathway in HepG2 cancer cells. Cell Biochem Biophys. 2014 May;69(1):27-34. 3. Zhou R, et al. Hispidulin exerts anti-osteoporotic activity in ovariectomized mice via activating AMPK signaling pathway. Cell Biochem Biophys. 2014 Jun;69(2):311-7. 4. Lin TY, et al. Protective effect of hispidulin on kainic acid-induced seizures and neurotoxicity in rats. Eur J Pharmacol. 2015 May 15;755:6-15. |