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CAS No. : 5610-40-2
MCE 国际站:(-)-Securinine
产品活性:(-)-Securinine 是一种植物来源的生物碱,也是一种 GABAA 受体拮抗剂。
研究领域:Membrane Transporter/Ion Channel | Neuronal Signaling
作用靶点:GABA Receptor
结构分类:生物碱 | 吡啶类生物碱
来源:植物 | 大戟科 | 一叶萩
In Vitro: (-)-Securinine is a major plant-derived alkaloid and also a GABAA receptor antagonist. (-)-Securinine is significantly potent on HeLa cells growth inhibition with IC50 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 Vivo: 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.
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