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Esculetin

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Chemical Structure| 305-01-1 同义名 : 秦皮乙素;二羟基香豆素;6,7-二羟基香豆素 ;Cichorigenin;Aesculetin;NSC 26428;CCRIS 7065;Asculetine;NSC 26427;6,7-Dihydroxycoumarin
CAS号 : 305-01-1
货号 : A155662
分子式 : C9H6O4
纯度 : 98%
分子量 : 178.142
MDL号 : MFCD00006874
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(673.62 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • lipoxygenase
描述 Lipoxygenases are a family of iron-containing enzymes that catalyze the formation of hydroperoxides from polyunsaturated fatty acids. Esculetin is an inhibitor of both 5- and 12-lipoxygenases with ID50 values of 4 and 2.5 μM, respectively[3]. It shows inhibitory effect on platelet lipoxygenase and platelet cyclooxygenase with respective IC50 values of 0.65 and 0.45 μM[4]. Treatment of colon cancer cells with esculetin (20-80 μMol/L) for 24h effectively suppressed TOP-luciferase activity in a dose-dependent manner. In HCT116, HCT15, and DLD1 colon cancer cells, 24h- treatment of esculetin at the doses of 20 - 80 μM substantially inhibited the protein levels of c-Myc and cyclin D1, but had no effect on the expressions of β-catenin or Tcf. Consistently, the mRNA levels of c-myc and cyclin D1 in esculetin-treated human colon cancer cells was downregulated compared to control group. Moreover, esculetin at 20 - 80 μM decreased the viability of colon cancer cells, and significantly repressed anchorage-independent cell growth in a dose-dependent manner. In athymic nude mice, intraperitoneal injection of esculetin at 20 and 100 mg/kg (3 times per week) for 2 weeks suppressed HCT116 tumor size by 44% and 64%, respectively, compared to vehicle-treated group[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

5.61mL

1.12mL

0.56mL

28.07mL

5.61mL

2.81mL

56.13mL

11.23mL

5.61mL
参考文献

[1]Wang J, Lu ML, et al. Esculetin, a coumarin derivative, exerts in vitro and in vivo antiproliferative activity against hepatocellular carcinoma by initiating a mitochondrial-dependent apoptosis pathway. Braz J Med Biol Res. 2015 Mar;48(3):245-53.

[2]Park SS, Park SK, et al. Esculetin inhibits cell proliferation through the Ras/ERK1/2 pathway in human colon cancer cells. Oncol Rep. 2011 Jan;25(1):223-30.

[3]Neichi T, Koshihara Y, Murota S. Inhibitory effect of esculetin on 5-lipoxygenase and leukotriene biosynthesis. Biochim Biophys Acta. 1983 Aug 29;753(1):130-2. PMID: 6411127.

[4]Sekiya K, Okuda H, Arichi S. Selective inhibition of platelet lipoxygenase by esculetin. Biochim Biophys Acta. 1982 Oct 14;713(1):68-72. PMID: 6814494.

[5]Lee SY, Lim TG, Chen H, Jung SK, Lee HJ, Lee MH, Kim DJ, Shin A, Lee KW, Bode AM, Surh YJ, Dong Z. Esculetin suppresses proliferation of human colon cancer cells by directly targeting β-catenin. Cancer Prev Res (Phila). 2013 Dec;6(12):1356-64. doi: 10.1158/1940-6207.CAPR-13-0241. Epub 2013 Oct 8. PMID: 24104353; PMCID: PMC3885338.