(–)-Securinine is an alkaloid originally isolated from S. suffructicosa.1 It reduces proliferation of SW480 colon adenocarcinoma cells in a dose- and time-dependent manner via increased Beclin 1 expression and induction of autophagy.2 It decreases viability of HL-60 leukemia cells (IC50s = 47.88, 23.85, and 18.87 μM at 24, 48, and 72 hours post-treatment, respectively).3 It also induces cell cycle arrest at the G1/S phase and decreases PI3K, Akt, and mTOR gene expression in a dose-dependent manner. (–)-Securinine inhibits GABA and GABA-activated benzodiazepine binding to rat brain membranes (IC50s = 57 and 101 μM, respectively).1 In vivo, (–)-securinine (5.2 mg/kg) induces clonic and tonic convulsions in mice, an effect that is reversed by administration of GABA.4
1.Beutler, J.A., Karbon, E.W., Brubaker, A.N., et al.Securinine alkaloids: A new class of GABA receptor antagonistBrain Res.330(1)135-140(1985) 2.Xia, Y.-H., Chang, C.-R., Yao, S.-Y., et al.L-securinine induced the human colon cancer SW480 cell autophagy and its molecular mechanismFitoterapia82(8)1258-1264(2011) 3.Han, S., Zhang, G., Li, M., et al.L-securinine induces apoptosis in the human promyelocytic leukemia cell line HL-60 and influences the expression of genes involved in the PI3K/AKT/mTOR signaling pathwayOncol. Rep.31(5)2245-2251(2014) 4.Tao, S.-C., Peng, J.-Z., and Lu, M.-W.Central convulsive action of l-securinineZhongguo Yao Li Xue Bao.7(1)9-12(1986)