Yangonin Blocks Tumor Necrosis Factor-α-Induced Nuclear Factor-κB-Dependent Transcription by Inhibiting the Transactivation Potential of the RelA/p65 Subunit
The nuclear factor-κB (NF-κB) transcription factors control many physiological processes including inflammation, immunity, and apoptosis. In our search for NF-κB inhibitors from natural resources, we identified yangonin from Piper methysticum as an inhibitor of NF-κB activation. In the present study...
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Elsevier,
2012-01-01T00:00:00Z.
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| 001 | doaj_8a8e4d46e231438d9c673334d3d26511 | ||
| 042 | |a dc | ||
| 100 | 1 | 0 | |a Juan Ma |e author |
| 700 | 1 | 0 | |a He Liang |e author |
| 700 | 1 | 0 | |a Hong Ri Jin |e author |
| 700 | 1 | 0 | |a Nguyen Tien Dat |e author |
| 700 | 1 | 0 | |a Shan Yu Zhang |e author |
| 700 | 1 | 0 | |a Ying Zi Jiang |e author |
| 700 | 1 | 0 | |a Ji Xing Nan |e author |
| 700 | 1 | 0 | |a Donghao Li |e author |
| 700 | 1 | 0 | |a Xue Wu |e author |
| 700 | 1 | 0 | |a Jung Joon Lee |e author |
| 700 | 1 | 0 | |a Xuejun Jin |e author |
| 245 | 0 | 0 | |a Yangonin Blocks Tumor Necrosis Factor-α-Induced Nuclear Factor-κB-Dependent Transcription by Inhibiting the Transactivation Potential of the RelA/p65 Subunit |
| 260 | |b Elsevier, |c 2012-01-01T00:00:00Z. | ||
| 500 | |a 1347-8613 | ||
| 500 | |a 10.1254/jphs.11215FP | ||
| 520 | |a The nuclear factor-κB (NF-κB) transcription factors control many physiological processes including inflammation, immunity, and apoptosis. In our search for NF-κB inhibitors from natural resources, we identified yangonin from Piper methysticum as an inhibitor of NF-κB activation. In the present study, we demonstrate that yangonin potently inhibits NF-κB activation through suppression of the transcriptional activity of the RelA/p65 subunit of NF-κB. This compound significantly inhibited the induced expression of the NF-κB-reporter gene. However, this compound did not interfere with tumor necrosis factor-α (TNF-α)-induced inhibitor of κBα (IκBα) degradation, p65 nuclear translocation, and DNA-binding activity of NF-κB. Further analysis revealed that yangonin inhibited not only the induced NF-κB activation by overexpression of RelA/p65, but also transactivation activity of RelA/p65. Moreover, yangonin did not inhibit TNF-α-induced activation of p38, but it significantly impaired activation of extracellular signal-regulated kinase 1/2 and stress-activated protein kinase/c-Jun NH2-terminal kinase. We also demonstrated that pretreatment of cells with this compound prevented TNF-α-induced expression of NF-κB target genes, such as interleukin 6, interleukin 8, monocyte chemotactic protein 1, cyclooxygenase-2 and inducible nitric oxide. Taken together, yangonin could be a valuable candidate for the intervention of NF-κB-dependent pathological conditions such as inflammation. Keywords:: yangonin, nuclear factor-κB (NF-κB), RelA/p65, transactivation, inflammation | ||
| 546 | |a EN | ||
| 690 | |a Therapeutics. Pharmacology | ||
| 690 | |a RM1-950 | ||
| 655 | 7 | |a article |2 local | |
| 786 | 0 | |n Journal of Pharmacological Sciences, Vol 118, Iss 4, Pp 447-454 (2012) | |
| 787 | 0 | |n http://www.sciencedirect.com/science/article/pii/S1347861319305389 | |
| 787 | 0 | |n https://doaj.org/toc/1347-8613 | |
| 856 | 4 | 1 | |u https://doaj.org/article/8a8e4d46e231438d9c673334d3d26511 |z Connect to this object online. |