紫草素

紫草素，(+)-Shikonin，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。更多视频请关注视频号【艾维缔】。哔哩哔哩【IVDSHOW】。抖音【军哥聊表观】。

关键词

紫草素

所属分类

抑制剂

目录号

T1125

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紫草素，(+)-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。

生物活性

产品描述	(+)-Shikonin (Anchusa acid) is a natural product, a TMEM16A chloride channel inhibitor (IC50=6.5 μM) and selective PKM2 inhibitor. Shikonin exhibits antitumor, anti-inflammatory and wound healing activities.
靶点活性	TMEM16A (Cl- channel):6.5 μM, PKM2 (FBP absence):0.3 μM, PKM2 (FBP presence):0.8 μM
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]
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].
别名	紫草素, NSC 252844, Isoarnebin 4, C.I. 75535, Anchusa acid, Alkanna Red, (R)-(+)-Shikonin, (+)-Shikonin

化学信息

分子量	288.30
分子式	C₁₆H₁₆O₅
CAS No.	517-89-5
Smiles	CC(C)=CC[C@@H](O)C1=CC(=O)c2c(O)ccc(O)c2C1=O
密度	1.373g/cm3

产品组分

内容	型号	规格	储存温度
紫草素	T1125-01	1mg	-20°C
紫草素	T1125-02	5mg	-20°C
紫草素	T1125-03	10mg	-20°C
紫草素	T1125-04	25mg	-20°C
紫草素	T1125-05	50mg	-20°C
紫草素	T1125-06	100mg	-20°C
紫草素	T1125-07	200mg	-20°C
紫草素	T1125-08	500mg	-20°C
操作手册	1	1	常温

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FAQ
1.Zhang FY, et al. Shikonin Inhibits the Migration and Invasion of Human Glioblastoma Cells by Targeting Phosphorylated β-Catenin and Phosphorylated PI3K/Akt: A Potential Mechanism for the Anti-Glioma Efficacy of a Traditional Chinese Herbal Medicine. Int J Mol Sci. 2015 Oct 9;16(10):23823-48.

2.Huang B, et al. Shikonin ameliorated mice colitis by inhibiting dimerization and tetramerization of PKM2 in macrophages. Front Pharmacol. 2022 Aug 17;13:926945.

3.Zhao X, et al. Shikonin Inhibits Tumor Growth in Mice by Suppressing Pyruvate Kinase M2-mediated Aerobic Glycolysis. Sci Rep. 2018 Sep 28;8(1):14517.

4.Zhang F Y, Hu Y, Que Z Y, et al. Shikonin inhibits the migration and invasion of human glioblastoma cells by targeting phosphorylated β-catenin and phosphorylated PI3K/Akt: a potential mechanism for the anti-glioma efficacy of a traditional Chinese herbal medicine[J]. International journal of molecular sciences, 2015, 16(10): 23823-23848.

5.Fu D, Shang X, Ni Z, et al. Shikonin inhibits inflammation and chondrocyte apoptosis by regulation of the PI3K/Akt signaling pathway in a rat model of osteoarthritis[J]. Experimental and therapeutic medicine, 2016, 12(4): 2735-2740.

6.Zhang FY, et al. Shikonin Inhibits the Migration and Invasion of Human Glioblastoma Cells by Targeting Phosphorylated β-Catenin and Phosphorylated PI3K/Akt: A Potential Mechanism for the Anti-Glioma Efficacy of a Traditional Chinese Herbal Medicine. Int J Mol Sci. 2015 Oct 9;16(10):23823-48.

7.Jiang Y et al. Shikonin Inhibits Intestinal Calcium-Activated Chloride Channels and Prevents Rotaviral Diarrhea. Front Pharmacol. 2016 Aug 23;7:270.