野黄芩苷 T2789

Product Introduction
Bioactivity


英文名: Scutellarin

描述: Scutellarin (Scutellarein-7-glucuronide) 是从黄芩中分离的黄酮，可抑制破骨细胞中 RANKL 介导的 MAPK 和 NF-κB 信号通路，并下调 HCC 细胞中的 STAT3/Girdin/Akt 信号通路。

细胞实验: 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.

体外活性: 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]。

体内活性: 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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: 5% DMSO+95% Saline : 2.5 mg/mL (5.41 mM, suspension)
DMSO : 50mg/mL(108.14 mM)


关键字: PKB | Inhibitor | inhibit | HIV | Protein kinase B | Human immunodeficiency virus | Akt | Scutellarin | STAT

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相关库: Anti-Breast Cancer Compound Library | Anti-Cancer Compound Library | Inhibitor Library | Kinase Inhibitor Library | Anti-virus Traditional Chinese Medicine Monomer Library | Traditional Chinese Medicine Monomer Library | Autophagy Compound Library | Metabolism Compound Library | Anti-infective Natural Product Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途