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Morusin

CAS No. : 62596-29-6

MCE 站：Morusin

产品活性：Morusin是从M. australis分离的去乙烯基化黄酮，具有抗肿瘤，抗氧化，抗菌等各种生物活性。Morusin可抑制 NF-κB 和 STAT3 的活性。

研究领域：NF-κB  |  Stem Cell/Wnt  |  JAK/STAT Signaling  |  Anti-infection

作用靶点：NF-κB  |  STAT  |  Bacterial

In Vitro: Morusin exhibits a dose- and time-dependent inhibitory effect on murine and human breast cancer cells. IC₅₀ is 9.48 μg/mL for normal mammary epithelial cells (MCF-10A); 2.03 and 1.87 μg/mL for murine breast cancer cells (4 T1 and EMT6); and 2.71 and 3.86 μg/mL for human breast cancer cells (MCF-7 and MDA-MB-231), respectively, the maximal inhibition of cell growth (>80 %) is obtained at 8 μg/mL. The apoptotic cells in morusin treated breast cancer cells are increased significantly in a dose-dependent manner. Morusin significantly inhibits the growth and clonogenicity of human colorectal cancer HT-29 cells. Morusin also inhibits the phosphorylation of IKK-α, IKK-βand IκB-β, increases expression of IκB-α, and suppresses nuclear translocation of NF-κB and its DNA binding activity. Dephosphorylation of NF-κB upstream regulators PI3K, Akt and PDK1 is also displayed. In addition, activation of caspase-8, change of mitochondrial membrane potential, release of cytochrome c and Smac/DIABLO, and activation of caspase-9 and -3 are observed at the early time point. Downregulation in the expression of Ku70 and XIAP is exhibited afterward. Morusin suppresses viability of prostate cancer cells, but little effect in normal human prostate epithelial cells. Morusin also reduces STAT3 activity by inhibiting its phosphorylation, nuclear accumulation, and DNA binding activity. In addition, morusin down-regulated expression of STAT3 target genes encoding Bcl-xL, Bcl-2, Survivin, c-Myc and Cyclin D1. It induces apoptosis in human prostate cancer cells by reducing STAT3 activity.

In Vivo: Morusin retards the growth of breast cancer significantly. Mean tumor weight of the control mice is 1.14±0.30 g, and those of the mice administrated with 5 and 10 mg/kg of morusin are 0.61±0.23 and 0.41±0.10 g, respectively, tumor inhibitory rates are 46.5 %, and 64.1 %, respectively.

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