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CAS No.: 305-01-1

七叶亭 Catalog No. CSN12630

Synonyms: 秦皮乙素

Esculetin is a naturally occuring 5-lipoxygenase and 12-Lipoxygenase inhibitor with IC50 values of ID50 values of 4 and 2.5 µM, respectively.

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实验方案

技术信息

生物活性

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].
动物研究
剂量
Rat: 10 mg/kg, 50 mg/kg^[3] (p.o.); 1.25 mg/kg - 20 mg/kg^[4] (i.p.) Mice: 6 mg/kg^[5] (p.o.)

给药途径
p.o., i.p.
参考文献

动物研究
剂量	Rat: 10 mg/kg, 50 mg/kg^[3] (p.o.); 1.25 mg/kg - 20 mg/kg^[4] (i.p.) Mice: 6 mg/kg^[5] (p.o.)
给药途径	p.o., i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 5.6135 mL
- 28.0676 mL
- 56.1352 mL
- 5 mM
- 1.1227 mL
- 5.6135 mL
- 11.2270 mL
- 10 mM
- 0.5614 mL
- 2.8068 mL
- 5.6135 mL

技术信息

CAS号

305-01-1

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C9H6O4

运输

蓝冰

分子量

178.14

别名

秦皮乙素

溶解度

DMSO	35.0 mg/mL (196.5 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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