Description |
Quercetagetin (6-Hydroxyquercetin) is the major flavonoid isolated from Citrus unshiu (C. unshiu) peel[3]. Quercetagetin is a moderately potent and selective, cell-permeable pim-1 kinase inhibitor (IC50, 0.34 μM)[1]. Anti-inflammatory and anticancer properties.
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Target |
PIM1:0.34 μM (IC50)
PIM2:3.45 μM (IC50)
RSK2:2.82 μM (IC50)
PKA:21.2 μM (IC50)
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In Vitro |
Quercetagetin also inhibits PIM2, PKA, and RSK2 with IC50s of 3.45, 21.2, and 2.82 µM, respectively. Quercetagetin inhibits PIM1 activity in intact RWPE2 prostate cancer cells in a dose-dependent manner (ED50, 5.5 μM). Furthermore Quercetagetin inhibits the activity of the Aurora-A kinase (IC50, ~4 μM). When pim-1-expressing cells were treated with Quercetagetin, p-BAD(S112) levels were markedly reduced in proportion to the concentration of Quercetagetin. Half-maximal inhibition occurred at 5.5 μM extracellular concentration[1]. Quercetagetin shows strong 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical-scavenging activity (IC50 7.89 μM) but much lower hydroxyl radical-scavenging activity (IC50 203.82 μM). Furthermore, Quercetagetin significantly reduces ROS in Vero cells and shows a strong protective effect against hydrogen peroxide-induced DNA damage[3].
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In Vivo |
Quercetagetin significantly inhibits UVB-induced skin cancer development. Topical application of 4 or 20 nmol of Quercetagetin to mouse skin reduces tumor incidence by 32.0% and 46.7%, respectively[2].
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Cell Assay |
RWPE2 cells are treated with Quercetagetin (0-12.5 μM) for up to 72 h. Cell number is measured by crystal violet staining and read at 570 nm[1].
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Animal Admin |
Mice[2] UVB-induced skin tumorigenesis SKH-1 hairless mouse model are treated with topical application of 4 or 20 nmol of Quercetagetin. At the end of the study, the dimensions of each tumor in each mouse are recorded. Tumor volume is calculated[2].
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Density | 1.912 g/cm3 |
Boiling Point | 732.4ºC at 760 mmHg |
Flash Point | 280.3ºC |
Exact Mass | 318.03800 |
PSA | 151.59000 |
LogP | 1.69360 |
Storage condition | 2-8℃ |