| 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 |
| 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) |
| 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 |
| Target | Value |
|
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.