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Inhibitory action of novel aromatic diamine compound on lipopolysaccharide-induced nuclear translocation of NF-kappaB without affecting IkappaB degradation.
FEBS Letters ( IF 3.0 ) Pub Date : 2004 Jul 30 , DOI: 10.1016/j.febslet.2004.06.056
Hyun-Mo Shin , Min-Hee Kim , Byung Hak Kim , Sang-Hun Jung , Yeong Shik Kim , Hye Ji Park , Jin Tae Hong , Kyung Rak Min , Youngsoo Kim

4-Methyl-N1-(3-phenyl-propyl)-benzene-1,2-diamine (JSH-23) is a novel chemically synthetic compound. The aromatic diamine JSH-23 compound exhibited inhibitory effect with an IC(50) value of 7.1 microM on nuclear factor (NF)-kappaB transcriptional activity in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7, and interfered LPS-induced nuclear translocation of NF-kappaB without affecting IkappaB degradation. This mechanism of action is very rare for controlling NF-kappaB activation. Furthermore, the compound inhibited not only LPS-induced expressions of tumor necrosis factor-alpha, interleukin (IL)-1beta, IL-6 and inducible nitric oxide synthase and cyclooxygenase-2 but also LPS-induced apoptosis of the RAW 264.7 cells.

中文翻译:

新型芳香族二胺化合物对脂多糖诱导的NF-κB核转运的抑制作用,而不会影响IkappaB的降解。

4-甲基-N1-(3-苯基-丙基)-苯-1,2-二胺(JSH-23)是新型的化学合成化合物。芳香族二胺JSH-23化合物对脂多糖(LPS)刺激的巨噬细胞RAW 264.7中的核因子(NF)-kappaB转录活性具有7.1 microM的IC(50)值的抑制作用,并干扰LPS诱导的NF核转运-kappaB,而不会影响IkappaB的降解。这种作用机制对于控制NF-κB激活非常罕见。此外,该化合物不仅抑制LPS诱导的肿瘤坏死因子-α,白介素(IL)-1beta,IL-6和诱导型一氧化氮合酶和环加氧酶2的表达,而且还抑制LPS诱导的RAW 264.7细胞凋亡。
更新日期:2017-01-31
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