Shikonin is an inhibitor of TMEM16A chloride channel with IC50 of 6.5 μM, it's a natural product isolated and purified from the roots of Lithosperraum erythrorhizon Sieb. et Zucc..
Shikonin is the major bioactive chemical component of Lithospermum erythrorhizon (Purple Cromwell) roots. It shows anticancer activity both in vitro and in vivo. At low concentration, shikonin induced apoptosis in various kinds of cell lines of different origins, including M10 (Mammary epithelial cells), EC109, EC9706 (Esophageal cancer,Esophageal epithelial cells), HCT116, SW620 (Colon cancer), A549 (Lung adenocarcinoma), AGS (Gastric cancer), 8505C8305C, FTC133, BCPAP, TPC1C643IHH4, K (Thyroid cancer) and Htori (Immortalized thyroid epithelial cells), etc.. However, at high concentrations shikonin induced necroptosis in various cancer cell lines. The mode of action of shikonin is associated with cell cycle, glycolysis, metastasis, DNA damage, inflammation, angiogenesis, epigenetics, autophagy or ferroxitosis. In vivo studies showed that shikonin exhibited anti-tumor effects through chemoprevention, cell death or other mechanisms in xenograft, carcinogen-induced, orthotopic or allograft cancer models. Shikonin is also used as a PKM2 inhibitor. Inhibition of PKM2 by shikonin re-sensitized the cisplatin resistant T24 cells and killed the T24 cisplatin resistant cells by inducing necroptosis at concentration of 0.4μM. Recent study found that shikonin showed inhibition effect on 2019-nCoV.
Shikonin 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
8-MG-BA cell
Growth inhibition assay
Inhibition of human 8-MG-BA cell growth in a cell viability assay, IC50=85.56 nM
SANGER
A101D cell
Growth inhibition assay
Inhibition of human A101D cell growth in a cell viability assay, IC50=0.712 nM
SANGER
A204 cell
Growth inhibition assay
Inhibition of human A204 cell growth in a cell viability assay, IC50=0.12654 μM
SANGER
A253 cell
Growth inhibition assay
Inhibition of human A253 cell growth in a cell viability assay, IC50=7.49 nM
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