A lignan with anti-inflammatory and anticancer activities
Magnolin is a lignan originally found in M. fargesii that has anti-inflammatory and anticancer activities.1 It inhibits LPS-induced nitric oxide (NO) production in BV-2 cells (IC50 = 20.5 ?M).2 Magnolin inhibits ERK1 and ERK2 (IC50s = 87 and 16.5 nM, respectively) and EGF-induced NF-κB transactivation activity when used at concentrations of 30 and 60 ?M.3 It suppresses migration of JB6 C141 cells in a concentration-dependent manner and decreases markers of epithelial-to-mesenchymal transition (EMT) in A549 cells. Magnolin decreases phosphorylation of Akt, increases caspase-3 levels, and upregulates p53 and p21 in PC3 and DU145 prostate cancer cells.4 It inhibits proliferation, halts the cell cycle, and induces apoptosis in PC3 and DU145 cells when used at concentrations of 50 and 100 ?M. Magnolin also reduces tumor growth and increases apoptosis of tumor cells in a PC3 prostate cancer mouse xenograft model when administered at a dose of 50 ?mol/kg.
1.Kakisawa, H., Kusumi, T., Hsu, H.-Y., et al.Structures of lignans of Magnolia fargesiiBull. Chem. Soc. Jpn.43(11)3631-3631(1970) 2.Kim, J.Y., Lim, H.J., Lee, D.Y., et al.In vitro anti-inflammatory activity of lignans isolated from Magnolia fargesiiBioorg. Med. Chem. Lett.19(3)937-940(2009) 3.Lee, C.-J., Lee, M.-H., Yoo, S.-M., et al.Magnolin inhibits cell migration and invasion by targeting the ERKs/RSK2 signaling pathwayBMC Cancer15:576(2015) 4.Huang, Y., Zou, X., Zhang, X., et al.Magnolin inhibits prostate cancer cell growth in vitro and in vivoBiomed Pharmacother.87714-720(2017)
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Cell experiment: |
JB6 Cl41 (7×104), A549 (7×104) and NCI-H1975 (7×104) cells, and RSK2+/+ (7×104) and RSK2-/- (7×104) MEFs are seeded into culture-inserts and cultured overnight. The cells are treated with mitomycin-C (10 μg/mL) for 2 h, and the culture-inserts are removed to offer a cell-free gap. The cells are treated with the indicated doses of Magnolin (15, 30, and 60 μM) either in the presence or absence of EGF for 12 or 24 h, and cell migration is observed under a light microscope. The migrated area is measured using the Image J computer software program. To measure the Magnolin effect on cancer cell invasion, a matrigel-coated invasion chamber is used. Briefly, A549 or NCI-H1975 (2.5×104) cells are seeded into an insert chamber with FBS-free media supplemented with the indicated doses of Magnolin(15, 30, and 60 μM), and cultured in 24-well plates supplemented with complete media for the appropriate time period. The cells are fixed with 4 % formaldehyde, permeabilized with methanol and stained with crystal violet. The stained cells are observed under a light microscope and those that have migrated are counted[1]. |
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参考文献: [1]. Lee CJ, et al. Magnolin inhibits cell migration and invasion by targeting the ERKs/RSK2 signaling pathway. BMC Cancer. 2015 Aug 8;15:576. |
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