"目录号: HY-13719

NF-κBStem Cell/Wnt-

Oleandrin（一种毒性强心苷）在各种培养的细胞系（U937，SKOV3，人上皮细胞和T细胞）中抑制NF-κB活性，在PC3细胞系培养中诱导程序性细胞死亡中的。

NF-κBβ-catenin

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生物活性

Description

Oleandrin (a toxic cardiac glycoside of N. oleander L.) inhibits the activity of NF-κB in various cultured cell lines (U937, CaOV3, human epithelial cells and T cells) as well as it induces programmed cell death in PC3 cell line culture. Target: NF-κBin vitro: Oleandrin inhibits proliferation of tumor cells and inhibits the excretion of fibroblast growth factor-2 (FGF-2) through membrane interaction and through inhibition of the Na, K-ATPase pump. In PANC-1 cells (human pancreatic cancer cell line), cell death occurs not through apoptosis, but rather through autophagy and it has been noticed that Oleandrin at low nanomolar concentrations potently inhibited cell proliferation associated with induction of a profound G(2)/M cell cycle arrest. Inhibition of cell cycle is not accompanied by any significant sub G1 accumulation of cells, suggesting a non-apoptotic mechanism of Oleandrin. [1] Oleandrin suppresses the activity of Wnt/β-catenin signaling pathway. Oleandrin downregulates the target gene expression of the Wnt/β-catenin pathway at both the mRNA and protein levels. Oleandrin inhibits the protein expression of β-catenin and reduces its nuclear localization. In addition, Oleandrin suppresses the activities of MMP-2 and MMP-9. Oleandrin also induces apoptosis in human leukemia cells through the dephosphorylation of Akt and expression of Fas L, as well as by altering the membrane fluidity. [2]in vivo: Oleandrin has lipophilic property and it can be easily absorbed in the gastrointestinal tract after oral dosing. Oleandrin is metabolized into oleandrigenin in mice.  Oleandrin is rapidly absorbed after oral dosing (Cmax at 20 min) although the elimination half-life is longer (2.3 ± 0.5 h) than that after i.v. dosing (0.4 ± 0.1 h).  In mouse studies, Oleandrin rapidly accumulates in brain tissue as it can pass through the blood-brain barrier. [1]

References

[1].Kumar A, et al. Oleandrin: A cardiac glycosides with potent cytotoxicity. Pharmacogn Rev. 2013 Jul;7(14):131-9.