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一叶萩碱
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CAS号:5610-40-2 | 英文名称:Securinine
分子式 C13H15NO2
分子量 217
EINECS号 694-738-6
MDL MFCD00867422
Smiles
InChIKey
乙二醇化学百科
基本信息
中文名称 一叶秋碱
英文名称 SECURININE
CAS号 5610-40-2
分子式 C13H15NO2
分子量 217.26
EINECS号 694-738-6
物化性质
熔点 140-1420C
比旋光度 D20 -1042° (c = 1 in alc)
沸点 357.82°C (rough estimate)
密度 1.30±0.1 g/cm3 (20 ºC 760 Torr)
折射率 1.5300 (estimate)
溶解度 二甲基亚砜:≥25mg/mL
形态 粉末
酸度系数(pKa) 8.29±0.20(Predicted)
颜色 粘黄色
旋光性 (optical activity) [α]/D -980 to -1015 (C=1, MeOH)
安全信息
危险品标志 T,Xn
危险类别码 23/24/25-22
安全说明 36/37/39-45
WGK Germany 3
RTECS号 VS4115000
生产及用途
(-)-Securinine 是一种植物来源的生物碱,也是一种 GABAA 受体拮抗剂。
TargetValue
GABA receptor
()

(-)-Securinine is a major plant-derived alkaloid and also a GABA A receptor antagonist. (-)-Securinine is significantly potent on HeLa cells growth inhibition with IC 50 values of 7.02±0.52 μg/mL (32.3 μM). (-)-Securinine induces apoptosis in a dose-dependent manner in the tested cells, increases the percentage of ROS positive cells and depolarized cells as well as stimulates the activity of ERK1/2, caspase-9 and -3/7. (-)-Securinine also induces cell cycle arrest in S phase. Real-time PCR analysis shows high expression of tumor necrosis factor receptor superfamily (TNFRSF) genes in the cells stimulated with (-)-Securinine.

In this tumor model, tumor growth is significantly impaired with (-)-Securinine treatment indicating that (-)-Securinine has potential as an Acute Myeloid Leukemia (AML) therapeutic. (-)-Securinine treated mice (n=5 mice, bilateral tumors), exhibit an average of more than 75% smaller tumors than vehicle treated mice at the end of the study period.

化学性质 
黄色结晶粉末,可溶于甲醇、乙醇、DMSO等有机溶剂,来源于大戟科植物叶底珠的嫩枝叶或根,叶下珠。
用途 
中枢神经系统兴奋药。
用途 
抗菌活性;对中枢神经系统有兴奋作用;抗肿瘤作用
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