| Description | Scutellarin (Scutellarein-7-glucuronide), an active flavone isolated from Scutellaria baicalensis, can inhibit RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts, and down-regulate the STAT3/Girdin/Akt signaling in HCC cells. |
| In vitro | Scutellarin 处理明显以剂量依赖的方式降低了HepG2细胞的活性。在体外，它还抑制了HCC细胞的迁移和侵袭。Scutellarin 处理显著减少了HCC细胞中STAT3和肌动蛋白丝的桥梁(Girdin)表达、STAT3和Akt的磷酸化。STAT3过表达的引入恢复了Scutellarin 降低的Girdin表达、Akt激活、HCC细胞的迁移和侵袭。此外，Girdin过表达的诱导完全消除了Scutellarin 对HCC细胞Akt磷酸化、迁移和侵袭的抑制作用。Scutellarin 通过下调STAT3/Girdin/Akt信号通路抑制HCC细胞体内外的转移、迁移和侵袭[1]。Scutellarin 选择性增强了Akt磷酸化[2]。Scutellarin 作为一种潜在的治疗剂，它不仅可以抑制微胶质细胞的活化，从而改善神经炎症，还可以增强星形胶质细胞反应。通过上调包括神经营养因子在内的表达，Scutellarin 放大了星形胶质细胞的反应，显示其神经保护作用。值得注意的是，Scutellarin 对反应性星形胶质细胞的影响是通过激活的微胶质细胞介导的，支持两种胶质细胞类型之间的功能性“交流”[3]。Scutellarin 能够抑制RANKL介导的成骨细胞形成、成骨细胞的骨吸收功能以及特定成骨细胞基因（耐酸性磷酸酶（TRAP）、猫酶K、c-Fos、NFATc1）的表达水平。进一步的研究表明，Scutellarin 能够抑制RANKL介导的MAPK和NF-κB信号通路，包括JNK1/2、p38、ERK1/2和IκBα的磷酸化[5]。 |
| In vivo | Scutellarin (50 mg/kg/day) significantly mitigates the lung and intrahepatic metastasis of HCC tumors in vivo. The numbers of lung and intrahepatic metastatic tumors in the scutellarin-treated group are significantly less compared to the controls[1]. The rats treated with Scutellarin display a significant alleviation in neurobehavioral deficits compared to the SAH group. Scutellarin enhanced eNOS expression compared with SAH rats[4]. |
| Cell experiments | HepG2 cells (1×105/well) are cultured in 96-well plates and treated in triplicate with scutellarin at concentrations of 5, 10, 20, 30, and 100 μM or vehicle alone for 24 h. The cellular viability is tested by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, and is expressed as a percentage of proliferation versus controls. |
| Synonyms | 黄岑素, 野黄芩苷, Breviscapin, Breviscapinun, Breviscapine, Scutellarein-7-glucuronide |
| molecular weight | 462.36 |
| Molecular formula | C21H18O12 |
| CAS | 27740-01-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50mg/mL(108.14 mM) |
| References | 1. Ke Y, et al. Scutellarin suppresses migration and invasion of human hepatocellular carcinoma by inhibiting the STAT3/Girdin/Akt activity. Biochem Biophys Res Commun. 2016 Dec 18. pii: S0006-291X(16)32174-X. 2. Yang LL, et al. Differential regulation of baicalin and scutellarin on AMPK and Akt in promoting adipose cell glucose disposal. Biochim Biophys Acta. 2016 Nov 27;1863(2):598-606. 3. Wu CY, et al. Scutellarin attenuates microglia-mediated neuroinflammation and promotes astrogliosis in cerebral ischemia - a therapeutic consideration. Curr Med Chem. 2016 Nov 18. [Epub ahead of print] 4. Li Q, et al. Scutellarin attenuates vasospasm through the Erk5-KLF2-eNOS pathway after subarachnoid hemorrhage in rats. J Clin Neurosci. 2016 Dec;34:264-270. 5. Zhao, S., Sun, Y., Li, X., Wang, J., Yan, L., & Zhang, Z. et al. (2016). Scutellarin inhibits RANKL-mediated osteoclastogenesis and titanium particle-induced osteolysis via suppression of NF-κB and MAPK signaling pathway. International Immunopharmacology, 40, 458-465. doi: 10.1016/j.intimp.2016.09.031 6. Chinnasamy S, Selvaraj G, Selvaraj C, et al. Combining in silico and in vitro approaches to identification of potent inhibitor against phospholipase A2 (PLA2)[J]. International Journal of Biological Macromolecules. 2020, 144: 53-66 |