产品说明书
Piperlongumine
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同义名 : | Piplartine;PPLGM |
| CAS号 : | 20069-09-4 | |
| 货号 : | A250732 | |
| 分子式 : | C17H19NO5 | |
| 纯度 : | 99%+ | |
| 分子量 : | 317.337 | |
| MDL号 : | MFCD00075706 | |
| 存储条件： |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(330.88 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
IP 2% DMSO+2% Tween80+40% PEG300+water 6 mg/mL clear PO 0.5% CMC-Na 50 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
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| 描述 | Reactive Oxygen Species (ROS) can induce small molecules that use the altered redox state in cancer cells that will be more vulnerable than normal cells to agents with high levels of ROS as well as antioxidant enzymes. Piperlongumine(PL), a natural alkaloid from Piper longum L, can increase the level of ROS and selectively kills cancer cells, which is also a TrxR1 inhibitor with suppressive activity against gastric cancer and a novel inhibitor of CRM1 as well as an inhibitor of PI3K/Akt/mTOR in human breast cancer cells. The average IC50 value of piperlongumine in different cell types is about 5μM. Piperlongumine with concentration range of 0.1–20 μM induced a concentration and time-dependent decrease in the viability of PANC-1, MIA PaCa-2, and BxPC-3, with IC50 values of 4.2, 4.6, and 4.2 μM, respectively at 72 h. MIA PaCa-2 and BxPC-3 cells were particularly sensitive to piperlongumine, and no cells survived for the 5 and 10 μM treatments. PANC-1, MIA PaCa-2, and BxPC-3 cells treated with 10 μM PPLGM for 6 h followed by staining for 30 min, the production of ROS in all three cell lines increased. Three ovarian cancer cell lines A2780, OVCAR3, and SKOV3 and human embryonic kidney cell line HEK293T were treated with either DMSO or PL range from 1 to 100 μM for 72 hr, the IC50 values of PL afer 72 hr exposure were 6.18 μM, 6.20 μM, and 8.20 μM in A2780, OVCAR3, and SKOV3, respectively while it is 60.23 μM to HEK293T. In addition, PL treatment mostly induced apoptosis in OVCAR3 cells. OVCAR3 cells treated with PL (3 μM and 10 μM for 24 hr and 48 hr) showed that the subG1 and G2/M groups were dose- and time dependently increased. Furthermore, HepG2 cells were treated with 2 mM of PL to determine its ability to activate AMPK. PL increased Thr172 phosphorylation and led to a dose-dependent increase in phosphorylation of AMPK and acetyl-CoA carboxylase. | ||
| 作用机制 | Piperlongumine can induce cell autophagy and cell death, inhibit cell proliferation and survival. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| A375 cells | Proliferation assay | 72 h | Antiproliferative activity against human A375 cells after 72 hrs by MTT assay, EC50=6.17 μM | 25826398 | |
| A549 cells | Proliferation assay | 72 h | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, EC50=12.2 μM | 25826398 | |
| HaCaT cells | Proliferation assay | 72 h | Antiproliferative activity against human HaCaT cells after 72 hrs by MTT assay, EC50=4.46 μM | 25826398 | |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.15mL 0.63mL 0.32mL |
15.76mL 3.15mL 1.58mL |
31.51mL 6.30mL 3.15mL |
