紫草素 T1125

Product Introduction
Bioactivity


英文名: Shikonin

描述: Shikonin (Anchusa acid) 属于天然产物，是一种 TMEM16A 氯离子通道抑制剂 (IC50=6.5 μM) 和选择性 PKM2 抑制剂。Shikonin 具有抗肿瘤、抗炎和伤口愈合活性。

细胞实验: U87 and U251 cells are seeded into 96-well plates at a density of 1×104 cells per well in standard DMEM and incubated for 24 h under standard conditions (37°C and 5% CO2). Then the medium is replaced with either blank, serum-free DMEM or DMEM containing Shikonin at concentrations of 2.5, 5, and 7.5 μM. The total volume in each well is 200 μL. Finally, the plates are shaken softly and the optical density is recorded at 570 nm (OD570) using a plate reader. At least three independent experiments are performed[4].

动物实验: Healthy male Sprague-Dawley rats (n=30; 8 to 10-weeks old, 250 to 300 g) are used in this study. Rats were randomly assigned to three groups: Sham-operated group (n=10), osteoarthritis model group (n=10) and Shikonin-treated group (n=10). In the sham-operated group, the right knee joint of the anesthetized rat is only exposed under sterile conditions, and the rats are treated with 0.1 ml/100 g physiological saline (i.p.). In the osteoarthritis model group, osteoarthritis model rats were treated with 0.1 ml/100 g physiological saline (i.p.). In the Shikonin-treated group, osteoarthritis model rats are treated with 10 mg/kg Shikonin (i.p.) once daily for 4 days after osteoarthritis modeling[5].

体外活性: 方法：人胶质瘤细胞 U87 和 U251 用 Shikonin (2.5-7.5 μmol/L) 处理 12-72 h，使用 CCK-8 方法检测细胞活力。结果：Shikonin 以时间和剂量依赖的方式抑制 U87 和 U251 细胞的增殖。[1]方法：巨噬细胞 RAW264.7 用 Shikonin (0.5-2 μM) 预处理 1 h，然后用 LPS (250 ng/mL) 和 IFN-γ (100 ng/mL) 处理 24 h，使用 RT-qPCR 和 ELISA 检测炎症因子水平。结果：在 LPS+IFN-γ 模拟的 RAW264.7 细胞中，IL-1β、IL-6 和 TNF-α 的 mRNA 和蛋白表达均降低。[2]

体内活性: 方法：为研究对小鼠结肠炎的疗效，将 Shikonin (6.125-25 mg/kg) 灌胃给药给 DSS 诱导的 Balb/c 小鼠结肠炎模型，每天一次，持续七天。结果：Shikonin 减轻了 DSS 诱导的小鼠结肠炎的总体症状，并减轻了结肠损伤。[2]方法：为检测体内抗肿瘤活性，将 Shikonin (0.1-10 mg/kg) 腹腔注射给携带人黑色素瘤 B16 的 SCID 小鼠，每天一次，持续九天。结果：Shikonin 处理以剂量依赖的方式抑制 SCID 小鼠中的 B16 细胞生长。[3]

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

溶解度: DMSO : 57 mg/mL
H2O : Insoluble
Ethanol : 13 mg/mL(45.1 mM)


关键字: Inhibitor | Nuclear factor-kappaB | inhibit | TNFR | Human immunodeficiency virus | HIV | Cl? Channels | Isoarnebin-4 | TNF Receptor | Pyruvate Kinase | Isoarnebin4 | Tumor Necrosis Factor Receptor | Nuclear factor-κB | NSC-252844 | Shikonin | Chloride Channel | NF-κB | NSC252844

相关产品: SPD304 | Gentianine | C25-140 | AX-024 hydrochloride | Apremilast | Nepetoidin B | Caulophyllogenin | 6,4'-Dihydroxy-7-methoxyflavanone | Bacoside A | Cynaropicrin

相关库: Anti-Prostate Cancer Compound Library | Anti-Breast Cancer Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Kinase Inhibitor Library | Traditional Chinese Medicine Monomer Library | Cuproptosis Compound Library | Tibetan medicine Compound Library | Glycolysis 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