Norartocarpetin is a tyrosinase inhibitor. Norartocarpetin has strong tyrosinase inhibitory activity with an IC 50 value of 0.47 μM. Norartocarpetin as an antibrowning agent can be used for the research of food systems. Norartocarpetin also has a significant anticancer activity in lung carcinoma cells (NCI-H460) with an IC 50 value of 22 μM. Norartocarpetin has antiproliferative effects are mediated via targeting Ras/Raf/MAPK signalling pathway, mitochondrial mediated apoptosis , S-phase cell cycle arrest and suppression of cell migration and invasion in human lung carcinoma cells
In Vitro
Norartocarpetin has strong mushroom tyrosinase inhibitory activity with an IC 50 value of 0.47 μM. Norartocarpetin (0-100 μM; 48 h) leds to dose-dependent cytotoxic effects in NCI-H460 cells and MRC-9 cells with IC 50 values of 22 μM and 85 μM, respectively. Norartocarpetin (0, 11, 22, and 44 μM; 24 h) led to blockade of Ras/Raf/MAPK signalling pathway. Norartocarpetin (0, 11, 22, and 44 μM, 24 h) induced the apoptosis of the human lung carcinoma cells (NCI-H460). Norartocarpetin (0, 11, 22, and 44 μM) leds to S-phase cell cycle arrest. Norartocarpetin (22 μM; 24 h) leds to dose-dependent suppression of cell invasion. Norartocarpetin (0, 11, 22, and 44 μM, 24 h) leds to significant inhibition of cell migration. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: MRC-9 (normal fibroblast lung cells) and NCI-H460 (human lung cancer cells) Concentration: 0, 3.12, 6.25, 12.5, 25, 50, and 100 μM (first dissolved in DMSO at 1.0 mg/mL and then diluted to different concentrations using DMSO, 30 μL, 20min) Incubation Time: 48 h Result: Repressed the viability of NCI-H460 cells in a dose-dependent manner. Western Blot AnalysisCell Line: MRC-9 and NCI-H460 cells Concentration: 0, 11, 22, and 44 μM Incubation Time: 24 h Result: Significantly reduced the expression of p-RAS, p-RAF and p-P38 and unchanged the expressions of RAS, RAF and P38. Apoptosis AnalysisCell Line: MRC-9 and NCI-H460 cells Concentration: 0. 11, 22 and 44 μM Incubation Time: 24 h Result: Led to dose-dependent apoptosis and induced DNA damage. Cell Cycle AnalysisCell Line: MRC-9 and NCI-H460 cells Concentration: 0, 11, 22, and 44 μM Incubation Time: Result: Showed increase of S-phase cells and the percentage of S-phase NCI-H460 LC cells was 30%, 40%, 55% and 70% at 0, 11, 22 and 44 μM concentrations, respectively. Cell Invasion AssayMRC-9 and NCI-H460 cells Cell Line: MRC-9 and NCI-H460 cells Concentration: 22 μM Incubation Time: 24 h Result: Significantly reducted (from 100% to about 40%) in the invasion of NCI-H460 human LC cells. Cell Migration AssayCell Line: MRC-9 and NCI-H460 cells Concentration: 0, 11, 22, and 44 μM Incubation Time: 24 h Result: Decreased remarkably the cell invasion in NCI-H460 LC cells in a concentration- dependent manner.
Form:Solid
IC50& Target:IC50: 0.47 μM (tyrosinase), IC50: 22 μM (NCI-H460 cells),85 μM (MRC-9 cells)
