Shikonin is an inhibitor of TMEM16A chloride channel with IC50 of 6.5 uM.
Shikonin is a naphthoquinone extracted from the root of Lithospermum erythrorhizon, and has been reported to suppress allergic airway inflammation in mice. In this study, shikonin (0.5, 2 or 4mg/kg) was given intraperitoneally to ovalbumin (OVA)-challenged BALB/c mice. We found that the pathological airway remodeling of asthmatic mice was alleviated by shikonin, and the infiltrated inflammatory cells and collagen deposition in their lungs were reduced. Furthermore, the abnormal activation of extracellular signal-regulated kinase (ERK)/nuclear factor-κB (NF-κB) pathway and the elevation of matrix metalloproteinase 9 (MMP9) in the lung of asthmatic mice were suppressed by shikonin. The inactivation of NF-κB by shikonin was at least in part via inhibiting IκBα activation. In vitro, the treatment of shikonin inhibited the platelet-derived growth factor (PDGF)-induced proliferation of primary airway smooth muscle cells (ASMCs), and induced a G0/G1 arrest in these cells.
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Chen, X., et al. 2003. Antimicrob. Agents Chemother. 47: 2810-2816.
[2] Nigorikawa, K., et al. 2006. Mol. Pharmacol. 70: 1143-1149.
[3] Kim, Y.O., et al. 2010. Korean J. Physiol. Pharmacol. 14: 199-204.
分子式 C16H16O5 |
分子量 288.30 |
CAS号 517-89-5 |
储存方式 -20 ℃长期冷藏储存。冰袋运输 |
溶剂(常温) |
DMSO 54 mg/mL |
Water <1 mg/mL |
Ethanol 20 mg/mL |
体内溶解度
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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