CAS |
No.92-61-5 |
中文名称 |
东莨菪内酯(10mM in DMSO,无菌) |
英文名称 |
Scopoletin(10mM in DMSO,Sterile) |
分子式 |
C10H8O4 |
分子量 |
192.17 |
溶解性 |
请根据自己的实验要求使用。 |
外观(性状) |
无菌溶液 |
储存条件 |
Stroe at -20℃,6 months. |
靶点 |
AChE |
通路 |
Neuronal Signaling |
背景说明 |
Scopoletin 是一种乙酰胆碱酯酶 (AChE) 抑制剂。 |
生物活性 |
Scopoletin is an inhibitor of acetylcholinesterase (AChE).[1-2] |
In Vitro |
Scopoletin (SCT) 被确定为乙酰胆碱酯酶 (AChE) 的推定抑制剂。Scopoletin 增强 K+ 刺激的大鼠额叶皮质突触体 ACh 释放,显示出钟形剂量效应曲线 (Emax:4 μM)[1]。Scopoletin 通过诱导 PC3 细胞凋亡来抑制 PC3 增殖。Scopoletin抑制PC3、PAA (人肺癌细胞)、Hela 细胞增殖的 IC50 分别为 (157±25)、(154±51)、(294±100) mg/L。Scopoletin 诱导显著的时间和浓度依赖性 PC3 细胞增殖抑制。Scopoletin 以浓度依赖性方式降低 PC3 细胞中的蛋白质含量和酸性磷酸酶活性 (ACP) 水平。光镜、荧光显微镜、透射电镜观察 Scopoletin 处理后的细胞,显示出典型的细胞凋亡形态学变化。Scopoletin 0、100、200、400 mg/L 时细胞凋亡率分别为 0.3%、2.1%、9.3%、35%,东莨菪素处理后 G2 期细胞明显减少[2]。 |
In Vivo |
Scopoletin (2 μg,icv) 增加 T 迷宫交替并改善东莨菪碱诱导的胆碱能缺陷小鼠的新物体识别。 Scopoletin 还可以减少 15-18 个月大的小鼠(2 mg/kg sc)的对象记忆中与年龄相关的缺陷。 注射 2 μg Scopoletin 的小鼠表现出 71.3±2.5% 的交替率增加[1]。 |
细胞实验 |
PC3 cells (5×107/L) 1 mL in exponential growth are seeded into four 24-well plates. The plates are incubated at 37°C in a humidified 5% CO2 atmospbee. After 24h, Scopoletin 33, 66, 133, 266, and 533 mg/L are added to wells (3 wells for each concentration for each plate). For control cells (3 wells foreach plate),only DMEM was added. The plates are incubated continually. The viable cells are counted by hemocytometer every day in the frist 4 d by Trypan blue dye exclusion method[2]. |
动物实验 |
Mice[1]C56BL/6N male, 4-6-month-old and 16-18-month-old mice are used in the behavioral studies. The mice are housed in groups of four in cages at constant humidity (50-55%) and temperature (22±1°C) on a 12:12 h light/dark cycle (7:00–19:00 h), with food and water ad libitum. Younger mice (4-6 months) are implanted with i.c.v. cannulas for application of Scopolamine (SCOP) and Scopoletin. The aged mice are injected with Scopoletin by the s.c. route. Experiments are conducted between 8:00 and 16:00 h. Mice with i.c.v. cannulas are randomly divided into four experimental groups: vehicle; SCOP 20 μg; Scopoletin 2 μg; and SCOP 20 μg plus Scopoletin 2 μg. The drugs are applied in 1 μL of vehicle solution (SCOP: saline, Scopoletin: 3 DMSO: 7 sterile water). I.c.v. injections are carried out 15 min before the start of the tests. Aged mice obtained Scopoletin s.c. 30 min prior to object memory test (vehicle: 1 DMSO: 1 EtOH, diluted with olive oil as required)[1]. |
数据来源文献 |
[1]. Hornick A, et al. The coumarin Scopoletin potentiates acetylcholine release from synaptosomes, amplifies hippocampal long-term potentiation and ameliorates anticholinergic- and age-impaired memory. Neuroscience. 2011 Dec 1;197:280-92. [2]. Liu XL, et al. Effect of Scopoletin on PC3 cell proliferation and apoptosis. Acta Pharmacol Sin. 2001 Oct;22(10):929-33. |
规格 |
1ml |
单位 |
瓶 |