中文同义词:
一叶秋碱 , 来源于叶底珠;一叶秋碱 ,一叶萩碱(标准品);SECURININE 一叶萩碱;一叶萩碱、一叶秋碱;一叶秋碱 ,一叶萩碱;叶底珠碱;一叶碱;硝酸一叶秋碱
英文同义词:
SECURAN-11-ONE;SECURININE;(-)-securinin;securinan-11-one;(-)-SECURININE;securinin;Securinan-11-on;SECURININE(RG)
相关类别:
中草药成分;原料药;中间体;植物提取物;植提;标准品，对照品;中药对照品;Heterocycles;Intermediates Fine Chemicals;Pharmaceuticals;天然产物;对照品;标准品;植提标准品;精细化工;标准品-对照品;对照品-中药对照品;生物碱;标准品 -中药标准品
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)
酸度系数(pKa)
8.29±0.20(Predicted)
旋光性 (optical activity)
[α]/D -980 to -1015 (C=1, MeOH)
生物活性
(-)-Securinine 是一种植物来源的生物碱，也是一种 GABAA 受体拮抗剂。
靶点
Target Value
GABA receptor
()
体外研究
(-)-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.
体内研究
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
抗菌活性；对中枢神经系统有兴奋作用；抗肿瘤作用
