Alpinetin, a composition of Alpinia katsumadai Hayata, has been reported to have a number of biological properties, such as antibacterial, antitumor and other important therapeutic activities.[1-2]
In Vitro
Alpinetin markedly inhibits the LPS- induced TNF-α, IL-6 and IL-1β production both in vitro and vivo. Furthermore, alpinetin blocks the phosphorylation of IκBα protein, p65, p38 and extracellular signal-regulated kinase (ERK) in LPS stimulated RAW 264.7 cells[1]. Alpinetin can suppress the proliferation and invasiveness of GSCs and induce apoptosis in GSCs[2].
In Vivo
Alpinetin attenuates lung histopathologic changes in mouse models[1].The anti-tumor activity of alpinetin was further confirmed in an animal model. Collectively, targeting of GSC by alpinetin is an effective strategy for glioma therapy.[2]
SMILES
O=C1C[C@@H](C2=CC=CC=C2)OC3=CC(O)=CC(OC)=C13
靶点
UCK2
动物实验
Cell viability is evaluated by MTT assay. Briefly, 100 μl cells are plated at a density of 4×105 cells/ml in 96-well plates in a 37 ℃, 5% CO2 incubator for 1 h. Then the cells are treated with 50 μl of alpinetin of different concentrations (0-300 μg/ml) for 1 h, followed by stimulation with 50 μl LPS (4 μg/ml). The total volume of each well is 200 μl, and the concentrations of Alpinetin and LPS are four times diluted finally. After 18 h of LPS stimulation, 20 μl MTT (5 mg/ml) is added to each well, and the cells are further incubated for an additional 4 h. The supernatant is removed and the formation of formazan is resolved with 150 μl/well of DMSO. The optical density is measured at 570 nm on a microplate reader.[1]
细胞实验
Animal Models: Male BALB/c mice; Dosages: 50 mg/kg; Administration: i.p.[1]
数据来源文献
[1] Huo M, et al. Int Immunopharmacol. 2012, 12(1):241-8. [2] Wang J, et al. Tumour Biol. 2016, 37(7):9243-8.