tcsc0018584 (-) -Securinine

(-)-Securinine is plant-derived alkaloid and also a GABA_A receptor antagonist.

IC50 & Target: GABA_A receptor^[1]

In Vitro: (-)-Securinine is a major plant-derived alkaloid and also a GABA_A 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^[1].

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^[2].