Andrographolide (Andro) 穿心莲内酯是通过共价修饰 p50 的半胱氨酸 62 来影响 NF-κB 活性的小拮抗剂。Andrographolide (Andro) 穿心莲内酯是一种双环二萜内酯,主要由穿心莲 (Andrographis paniculate) 产生。Andrographolide (Andro) 穿心莲内酯抑制刺激的内皮细胞中 NF-κB 的活化,降低细胞粘附分子 E-选择素的表达,阻止 E-选择素介导的白细胞粘附,但对 IκBα 降解,p50 和 p65 核转位没有影
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Andrographolide (Andro) is a small antagonist for NF-κB activation by covalent modifying reduced cysteine 62 of p50. Andrographolide is a bicyclic diterpenoid lactone mainly produced from the plant Andrographis (Andrographis paniculate).Andrographolide suppresses the activation of NF-κB in stimulated endothelial cells, which reduces the expression of cell adhesion molecule E-selectin and prevents E-selectin-mediated leukocyte adhesion, but has no effect on IκBα degradation, p50 and p65 nuclear translocation[1].
Andrographolide (15 μM; 12 hours) inhibited the luciferase activities induced by TNF-α in a time-dependent manner with an IC50 of 10 μM[1]. Cell Proliferation Assay[1] Cell Line: 293 cells
[1]. Xia YF, et al. Andrographolide attenuates inflammation by inhibition of NF-kappa B activation through covalent modification of reduced cysteine 62 of p50. J Immunol. 2004 Sep 15;173(6):4207-17.
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