| Description | Piperlongumine (Piplartine) is an alkaloid natural product with anti-tumor, anti-inflammatory, anti-oxidant, anti-angiogenic and other biological activities. Piperlongumine enhances the level of ROS and induces apoptosis in tumor cells. |
| In vitro | 方法：7 株人骨髓瘤细胞系用 Piperlongumine 处理 48 h，使用 CCK-8 assay 检测细胞活力。结果：Piperlongumine 孵育 48 h 以剂量依赖的方式抑制 MM 细胞生长，IC50 值范围为 1-5 µM。[1]方法：人乳腺癌细胞系 MCF-7 用 Piperlongumine (10-20 µM) 处理 24 h，使用 Flow cytometry 检测细胞周期。结果：与对照组相比，G2/M 期的细胞分布显著增加了 5.56% (10 µM) 和 11.07% (20 µM)。Piperlongumine 在细胞周期中通过 G2/M 阻滞抑制细胞增殖。[2] |
| In vivo | 方法：为研究抗肿瘤活性，将 Piperlongumine (50 mg/kg，10% DMSO and 10% Tween 80 in water) 腹腔注射给携带 NCI-H929 异种移植物的裸鼠，每周五次，持续三周。结果：用 Piperlongumine 治疗的小鼠显示出肿瘤生长延迟，cleaved caspase-3 水平增加，p-STAT3 水平降低。[1] |
| Cell experiments | MCF-7 and 786-O cells are incubated with various PL concentrations for 48h. Cell proliferation is analysed by CellTiter Blue assay. Effective doses (ED) are calculated using XLift, Microsoft Excel add-in. (Only for Reference) |
| Synonyms | PPLGM, 荜茇酰胺, Piplartine |
| molecular weight | 317.34 |
| Molecular formula | C17H19NO5 |
| CAS | 20069-09-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 16.67 mg/mL (52.52 mM), Sonication is recommended. |
| References | 1. Yao Y, et al. Piperlongumine induces apoptosis and reduces bortezomib resistance by inhibiting STAT3 in multiple myeloma cells. Oncotarget. 2016 Nov 8;7(45):73497-73508. 2. Jeong CH, et al. Piperlongumine Induces Cell Cycle Arrest via Reactive Oxygen Species Accumulation and IKKβ Suppression in Human Breast Cancer Cells. Antioxidants (Basel). 2019 Nov 14;8(11):553. 3. Ryu J, et al. Nat Prod Res. 2014, 28(22), 2040-2043. 4. Bezerra DP, et al. J Appl Toxicol. 2008, 28(5), 599-607. 5. Zou P, et al. Cancer Lett. 2016, 375(1):114-26. 6. Wu X, e,t al. Piperlongumine inhibits angiotensin II-induced extracellular matrix expression in cardiac fibroblasts. J Cell Biochem. 2018 Dec;119(12):10358-10364 |
| Kinase | MEK Kinase Assay: Kinase inactive murine ERK2 (mERK2) K52A/T183A is affinity purified from Escherichia coli expressed using the pET21a vector. MEK1 kinase activity is determined using mERK2 K52A T183A as the substrate. Recombinant MEK1 enzyme (5 nM) is first activated by 0.02 unit or 1.5 nM of RAF1 in the presence of 25 mM HEPES (pH 7.8), 1 mM MgCl2, 50 mM NaCl, 0.2 mM EDTA, and 50 μM ATP for 30 minutes at 25 °C. The reactions are initiated by adding 2 μM of mERK2K52A T183A and 2.5 μCi [γ-33P] ATP in a total volume of 20 μL. The MEK2 kinase activity is determined similarly except that activation by RAF1 is not needed and 11 nM of MEK2 enzyme (active) are used in the assays.Kinase profiling is performed by Invitrogen using their Select Screen Kinase Profiling Service. The Z'-LYTE biochemical assay is used. RDEA119 is assayed in quadruplicate at 10 μM against 205 kinases. |