Piperlongumine 是一种来自 Piper longum L. 的天然生物碱，具有抗炎、抗菌、抗血管生成、抗氧化、抗肿瘤和抗糖尿病等活性。它选择性地杀死癌细胞并增强活性氧的水平。它具有抗心肌纤维化的作用，通过抑制 ERK1/2 信号通路抑制肌成纤维细胞的转化。

Piperlongumine is a natural alkaloid from Piper longum L. It selectively kills cancer cells and strengthens the level of reactive oxygen species (ROS).

Piperlongumine is a known ROS inducer which could induce pancreatic cancer cell death in cell culture[1] As a thromboxane A(2) receptor antagonist, Piperlongumine inhibits platelet aggregation. [2] Piperlongumine also promotes autophagy via inhibition of Akt/mTOR signalling and mediates cancer cell death. [3]

Piperlongumine (50 mg/kg i.p.) causes in vivo growth inhibition of tumor cells without leading to major changes in the biochemical, hematological and histopathological parameters. [4]

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.

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)

20069-09-4

C17H19NO5

317.341

PPLGM;Piplartine;荜茇酰胺

DMSO:31.7 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years