(-)-Securinine
(Synonyms: 一叶秋碱) 目录号 : GC30889
An alkaloid
Cas No.:5610-40-2
Sample solution is provided at 25 µL, 10mM.
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(–)-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)
Kinase experiment: | The cells are seeded in 12-well plates (1×105/well) and treated with (-)-Securinine at concentrations of 1.0 to 50.0 μg/mL. The control cells are exposed to DMSO at a concentration of 0.5% (v/v). After 6 h and 24 h of exposure, the activity of caspase-9 is measured by Caspase-Glo 9 Assay Kit and Glomax Multi+ Detection System, according to the manufacturer’s instruction. The activity of caspase-3/7 is assessed after 24 h of exposure the cells to (-)-Securinine. Then the cells are harvested and prepared using Muse Caspase-3/7 Assay Kit according with the manufacturer’s protocol. The stained cells are analyzed by Muse Cell Analyzer. The experiments are performed at least in three independent repeats[1]. |
Cell experiment: | The viability of the cells is determined by MTT assay. HeLa cells are seeded in 96-well plates at a density of 5×103 cells/well and treated for 24 h with (-)-Securinine in the concentration range of 1.0 to 20.0 μg/mL. The maximal concentrations of the solvents used in all the MTT experiments are 5.0% (v/v) and 1.0% (v/v) for methanol and DMSO, respectively. The absorption of the obtained formazan solution is measured with a plate reader. The viability results are presented as IC50 mean values of at least three independent experiments[1]. |
Animal experiment: | 6 week old female nude mice are used and injected bilaterally s.c. with 10×106 HL-60 cells. (-)-Securinine treatment is started 10 days after tumor cell injection. Palpable tumors are present for the established tumor model prior to initiating drug treatment. 15 mg/kg of (-)-Securinine or vehicle (30 µL of DMSO and 70 µL of water) are injected i.p. 2 or 3 times a day for 5 days followed by once a day for two days. This injection schedule is repeated for two additional weeks[2]. |
References: [1]. Stefanowicz-Hajduk J, et al. Securinine from Phyllanthus glaucus Induces Cell Cycle Arrest and Apoptosis in Human Cervical Cancer HeLa Cells. PLoS One. 2016 Oct 28;11(10):e0165372. | |
| Cas No. | 5610-40-2 | SDF | |
| 别名 | 一叶秋碱 | ||
| Canonical SMILES | O=C(O1)C=C2[C@@]13[C@](CCCC4)([H])N4[C@](C3)([H])C=C2 | ||
| 分子式 | C13H15NO2 | 分子量 | 217.26 |
| 溶解度 | DMSO : 2 mg/mL (9.21 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.6028 mL | 23.0139 mL | 46.0278 mL |
| 5 mM | 0.9206 mL | 4.6028 mL | 9.2056 mL |
| 10 mM | 0.4603 mL | 2.3014 mL | 4.6028 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet