TY - JOUR AB - The nuclear factor-κB (NF-κB) transcription factors control many physiological processes including inflammation, immunity, apoptosis and angiogenesis. In our search for NF-κB inhibitors from natural resources, we identified baicalein from Scutellaria baicalensis as an inhibitor of NF-κB activation. As examined by the NF-κB luciferase reporter assay, we found that baicalein suppressed TNF-α-induced NF-κB activation in a dose-dependent manner. It also inhibited TNF-α-induced nuclear translocation of p65 through inhibition of phosphorylation and degradation of IκBα. Furthermore, baicalein blocked the TNF-α-induced expression of NF-κB target genes involved in anti-apoptosis (cIAP-1, cIAP-2, FLIP and BCL-2), proliferation (COX-2, cyclin D1 and c-Myc), invasion (MMP‑9), angiogenesis (VEGF) and major inflammatory cytokines (IL-8 and MCP1). The flow cytometric analysis indicated that baicalein potentiated TNF-α-induced apoptosis and induced G1 phase arrest in HeLa cells. Moreover, baicalein significantly blocked activation of p38, extracellular signal-regulated kinase 1/2 (ERK1/2). Our results imply that baicalein could be a lead compound for the modulation of inflammatory diseases as well as certain cancers in which inhibition of NF-κB activity may be desirable. AD - Key Laboratory of Natural Resources of Changbai Mountain and Functional Molecules, Ministry of Education, Molecular Cancer Research Center, College of Pharmacy, Yanbian University, Yanji, Jilin 133002, P.R. China AU - Li,Junbo AU - Ma,Juan AU - Wang,Ke,Si AU - Mi,Chunliu AU - Wang,Zhe AU - Piao,Lian,Xun AU - Xu,Guang,Hua AU - Li,Xuezheng AU - Lee,Jung,Joon AU - Jin,Xuejun DA - 2016/11/01 DO - 10.3892/or.2016.5108 EP - 2776 IS - 5 JO - Oncol Rep KW - baicalein nuclear factor-κB IκBα inflammation cancer PY - 2016 SN - 1021-335X 1791-2431 SP - 2771 ST - Baicalein inhibits TNF-α-induced NF-κB activation and expression of NF-κB-regulated target gene products T2 - Oncology Reports TI - Baicalein inhibits TNF-α-induced NF-κB activation and expression of NF-κB-regulated target gene products UR - https://doi.org/10.3892/or.2016.5108 VL - 36 ER -